PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 33694335-0 2021 Successful management of familial hemophagocytic lymphohistiocytosis by the JAK 1/2 inhibitor ruxolitinib. ruxolitinib 94-105 Janus kinase 1 Homo sapiens 76-83 33534941-9 2021 Poly(I:C)-induced CCL5 production occurred via the TLR3-IRF3 and IFNAR/JAK1-phosphoinositide 3-kinase (PI3K) pathways, but not the IFNAR/JAK1-STATs pathway. Poly I-C 0-9 Janus kinase 1 Homo sapiens 71-75 33534941-12 2021 The JAK1/2 inhibitor, ruxolitinib, was demonstrated to more effectively decrease CCL5 production in BEAS-2B cells than fluticasone propionate. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 4-10 33534941-12 2021 The JAK1/2 inhibitor, ruxolitinib, was demonstrated to more effectively decrease CCL5 production in BEAS-2B cells than fluticasone propionate. Fluticasone 119-141 Janus kinase 1 Homo sapiens 4-10 33745126-4 2021 CIM activates complement cascade and increased monocyte infiltration in the soleus muscle, which was ameliorated by JAK1/2 inhibition, leading to reduced muscle degeneration and improved muscle force. cim 0-3 Janus kinase 1 Homo sapiens 116-122 34042156-0 2021 Randomized Controlled Trial Substudy of Cell-specific Mechanisms of Janus Kinase 1 Inhibition With Upadacitinib in the Crohn"s Disease Intestinal Mucosa: Analysis From the CELEST Study. upadacitinib 99-111 Janus kinase 1 Homo sapiens 68-82 34042156-2 2021 We aimed to provide mechanistic insights into the JAK1-selective inhibitor upadacitinib through a transcriptomics substudy on biopsies from patients with Crohn"s disease from CELEST. upadacitinib 75-87 Janus kinase 1 Homo sapiens 50-54 34054304-3 2021 Methods: In this study, we characterized a JAK1-specific inhibitor, LW402, on biochemical and human whole-blood assays. lw402 68-73 Janus kinase 1 Homo sapiens 43-47 34052462-0 2021 The JAK Inhibitor Tofacitinib Inhibits Structural Damage in Osteoarthritis by Modulating JAK1/TNF-alpha/IL-6 Signaling Through Mir-149-5p. tofacitinib 18-29 Janus kinase 1 Homo sapiens 89-93 34052462-10 2021 CONCLUSION: We show for the first time that tofacitinib suppresses the expression level of JAK1/TNF-alpha/IL-6 by upregulating miR-149-5p level. tofacitinib 44-55 Janus kinase 1 Homo sapiens 91-95 34052462-11 2021 Our findings revealed the functional association between proinflammatory JAK1/TNF-alpha/IL-6 signaling and ACs development and highlight the therapeutic potential of tofacitinib in OA. tofacitinib 166-177 Janus kinase 1 Homo sapiens 73-77 34023851-1 2021 JAK1/2 inhibitor ruxolitinib (RUX) is approved in patients with myelofibrosis but the impact of pretreatment with RUX on outcome after allogeneic hematopoietic stem cell transplantation (HSCT) remains to be determined. ruxolitinib 17-28 Janus kinase 1 Homo sapiens 0-6 34023851-1 2021 JAK1/2 inhibitor ruxolitinib (RUX) is approved in patients with myelofibrosis but the impact of pretreatment with RUX on outcome after allogeneic hematopoietic stem cell transplantation (HSCT) remains to be determined. ruxolitinib 30-33 Janus kinase 1 Homo sapiens 0-6 34054304-6 2021 Results: LW402 exhibited potent nanomolar activity against JAK1 and showed a 45-fold selectivity for inhibition of JAK1- over JAK2-dependent signaling induced by either IL6 or GM-CSF in human whole-blood assays. lw402 9-14 Janus kinase 1 Homo sapiens 59-63 34054304-6 2021 Results: LW402 exhibited potent nanomolar activity against JAK1 and showed a 45-fold selectivity for inhibition of JAK1- over JAK2-dependent signaling induced by either IL6 or GM-CSF in human whole-blood assays. lw402 9-14 Janus kinase 1 Homo sapiens 115-119 33595362-14 2021 Pre-incubation with the JAK1 inhibitor filgotinib ameliorated the barrier dysfunction induced by IL-28A. GLPG0634 39-49 Janus kinase 1 Homo sapiens 24-28 34023008-1 2021 BACKGROUND: Upadacitinib is an oral Janus kinase (JAK) inhibitor with greater inhibitory potency for JAK1 than JAK2, JAK3, and tyrosine kinase 2. upadacitinib 12-24 Janus kinase 1 Homo sapiens 101-105 34023009-2 2021 Upadacitinib is an oral Janus kinase (JAK) inhibitor with greater inhibitory potency for JAK1 than JAK2, JAK3, or tyrosine kinase 2 that is being tested for atopic dermatitis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 89-93 34008179-1 2021 Tofacitinib is a JAK1/3 inhibitor used off-label to treat alopecia areata (AA). tofacitinib 0-11 Janus kinase 1 Homo sapiens 17-23 33727040-6 2021 Meanwhile, polarized M2 macrophages enhance 5-FU resistance in tumor cells by secreting CCL8 and activating phosphorylation of JAK1/STAT3 signaling pathway. Fluorouracil 44-48 Janus kinase 1 Homo sapiens 127-131 33982267-2 2021 A cream formulation of ruxolitinib, a potent selective JAK1/JAK2 inhibitor, was developed for topical delivery. ruxolitinib 23-34 Janus kinase 1 Homo sapiens 55-59 34016786-8 2021 Then ruxolitinib was selected to perform molecular docking simulations with ANGPT2, FGF7, NT5E, CSF3R, JAK1, JAK2, JAK3, TYK2. ruxolitinib 5-16 Janus kinase 1 Homo sapiens 103-107 34025783-2 2021 We evaluated real-life efficacy and safety of Baricitinib, an oral selective JAK1-2 inhibitor, in RA patients using clinical, clinimetric, and US assessments. baricitinib 46-57 Janus kinase 1 Homo sapiens 77-83 33950225-1 2021 Upadacitinib and filgotinib, two JAK1 selective drugs have undergone extensive phase III clinical trials in RA and have demonstrated rapid improvements in disease activity, function and patient reported outcomes. upadacitinib 0-12 Janus kinase 1 Homo sapiens 33-37 33950225-1 2021 Upadacitinib and filgotinib, two JAK1 selective drugs have undergone extensive phase III clinical trials in RA and have demonstrated rapid improvements in disease activity, function and patient reported outcomes. GLPG0634 17-27 Janus kinase 1 Homo sapiens 33-37 33950226-5 2021 Tofacitinib, a JAK1 inhibitor, is now licensed for use in the induction and maintenance of ulcerative colitis and there are a large number of molecules currently under investigation. tofacitinib 0-11 Janus kinase 1 Homo sapiens 15-19 33950228-4 2021 With this proposal, early phase trials of selective JAK1 inhibitors, namely upadacitinib, filgotinib and itacitinib, were initiated in recent years to identify the efficacy and adverse effects of these agents and to define their potential role in treatment of inflammatory and autoimmune diseases. upadacitinib 76-88 Janus kinase 1 Homo sapiens 52-56 33950228-4 2021 With this proposal, early phase trials of selective JAK1 inhibitors, namely upadacitinib, filgotinib and itacitinib, were initiated in recent years to identify the efficacy and adverse effects of these agents and to define their potential role in treatment of inflammatory and autoimmune diseases. GLPG0634 90-100 Janus kinase 1 Homo sapiens 52-56 33950228-4 2021 With this proposal, early phase trials of selective JAK1 inhibitors, namely upadacitinib, filgotinib and itacitinib, were initiated in recent years to identify the efficacy and adverse effects of these agents and to define their potential role in treatment of inflammatory and autoimmune diseases. INCB039110 105-115 Janus kinase 1 Homo sapiens 52-56 33950228-5 2021 Early phase (Phase I-II) studies of upadacitinib and filgotinib provided evidence for efficacy and safety of the selective JAK1 inhibitors in refractory populations of RA patients and allowed informed selection of the appropriate dose by balancing the optimal benefit-risk profile for further evaluation in the later successfully performed Phase III trials. upadacitinib 36-48 Janus kinase 1 Homo sapiens 123-127 33950228-5 2021 Early phase (Phase I-II) studies of upadacitinib and filgotinib provided evidence for efficacy and safety of the selective JAK1 inhibitors in refractory populations of RA patients and allowed informed selection of the appropriate dose by balancing the optimal benefit-risk profile for further evaluation in the later successfully performed Phase III trials. GLPG0634 53-63 Janus kinase 1 Homo sapiens 123-127 33950230-2 2021 JAK1 selective drugs, upadacitinib and filgotinib, have broadly come with the same overarching safety recommendations as other immunosuppressive drugs for RA: caution is needed regarding infection risk; monitoring for laboratory abnormalities, including lipids and muscle enzymes, is indicated. upadacitinib 22-34 Janus kinase 1 Homo sapiens 0-4 33950230-2 2021 JAK1 selective drugs, upadacitinib and filgotinib, have broadly come with the same overarching safety recommendations as other immunosuppressive drugs for RA: caution is needed regarding infection risk; monitoring for laboratory abnormalities, including lipids and muscle enzymes, is indicated. GLPG0634 39-49 Janus kinase 1 Homo sapiens 0-4 33950231-2 2021 Newer generations of Jak inhibitors, like upadacitinib and filgotinib, target Jak 1 selectively with the aim of maximizing efficacy and to improve safety. upadacitinib 42-54 Janus kinase 1 Homo sapiens 78-83 33950231-2 2021 Newer generations of Jak inhibitors, like upadacitinib and filgotinib, target Jak 1 selectively with the aim of maximizing efficacy and to improve safety. GLPG0634 59-69 Janus kinase 1 Homo sapiens 78-83 33755884-1 2021 INTRODUCTION: In the phase 2 CELEST study, positive efficacy results were obtained with the Janus kinase 1 inhibitor upadacitinib for adult patients with moderate to severe Crohn"s disease. upadacitinib 117-129 Janus kinase 1 Homo sapiens 92-106 33585999-0 2021 Phase I study of JAK1/2 inhibitor ruxolitinib with weekly paclitaxel for the treatment of HER2-negative metastatic breast cancer. ruxolitinib 34-45 Janus kinase 1 Homo sapiens 17-23 33337992-1 2021 OBJECTIVES: Baricitinib is a Janus-kinase (JAK) 1/2 inhibitor, approved for the treatment of moderate-to-severe rheumatoid arthritis (RA) patients with inadequate response to conventional synthetic disease-modifying anti-rheumatic drugs (csDMARDs). baricitinib 12-23 Janus kinase 1 Homo sapiens 29-51 33585999-2 2021 Ruxolitinib is an orally bioavailable JAK1/2 inhibitor. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-44 33667986-12 2021 Our results suggest that improved stability and abnormal accumulation of Tregs in tumor microenvironment is IL-10/JAK1/STAT5 signal pathway-dependent and provide a novel approach for improving the efficiency of anti-tumor immunotherapy. tregs 73-78 Janus kinase 1 Homo sapiens 114-118 33527177-3 2021 Upadacitinib is a once-daily, oral Janus kinase (JAK) inhibitor with increased selectivity for JAK1 over JAK2, JAK3, and tyrosine kinase 2. upadacitinib 0-12 Janus kinase 1 Homo sapiens 95-99 33523540-3 2021 The JAK1/2 inhibitor ruxolitinib has recently gained attention as a treatment option for HLH due to its broad cytokine-modulating abilities and safety profile. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 33156550-1 2021 Upadacitinib is a selective Janus Kinase 1 inhibitor, which was recently approved for treatment of rheumatoid arthritis (RA) and is currently being evaluated for treatment of several other autoimmune diseases, including atopic dermatitis (AD). upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 33792103-5 2021 Therapies include hydroxyurea for cytoreduction, hypomethylating agents, and the JAK1/2 inhibitor ruxolitinib to address splenomegaly and constitutional symptoms. ruxolitinib 98-109 Janus kinase 1 Homo sapiens 81-87 33747209-0 2021 Ruxolitinib induces apoptosis of human colorectal cancer cells by downregulating the JAK1/2-STAT1-Mcl-1 axis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 85-91 32981124-2 2021 We report a case that demonstrated the efficacy and feasibility of ruxolitinib a JAK 1/2 inhibitor in the treatment of chronic steroid-refractory GVHD (SR-GVHD). ruxolitinib 67-78 Janus kinase 1 Homo sapiens 81-88 33747209-6 2021 Firstly, JAK1/2-STAT1 was identified as the target of ruxolitinib. ruxolitinib 54-65 Janus kinase 1 Homo sapiens 9-15 33747209-10 2021 Taken together, the results showed that ruxolitinib decreased JAK1/2-STAT1-Mcl-1 protein level and effectively suppressed CRC cell proliferation in vitro and in vivo. ruxolitinib 40-51 Janus kinase 1 Homo sapiens 62-68 33850568-0 2021 miR-20a-5p inhibits endometrial cancer progression by targeting janus kinase 1. mir-20a-5p 0-10 Janus kinase 1 Homo sapiens 64-78 33850568-4 2021 Whether miR-20a-5p could inhibit EC progression by targeting janus kinase 1 (Jak1) was subsequently investigated. mir-20a-5p 8-18 Janus kinase 1 Homo sapiens 61-75 33850568-4 2021 Whether miR-20a-5p could inhibit EC progression by targeting janus kinase 1 (Jak1) was subsequently investigated. mir-20a-5p 8-18 Janus kinase 1 Homo sapiens 77-81 32981124-2 2021 We report a case that demonstrated the efficacy and feasibility of ruxolitinib a JAK 1/2 inhibitor in the treatment of chronic steroid-refractory GVHD (SR-GVHD). Steroids 127-134 Janus kinase 1 Homo sapiens 81-88 33965175-1 2021 Ruxolitinib is a JAK2/JAK1 inhibitor that blocks the inflammatory JAK-STAT signaling pathway. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-26 33965175-1 2021 Ruxolitinib is a JAK2/JAK1 inhibitor that blocks the inflammatory JAK-STAT signaling pathway. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-20 33740386-0 2021 Filgotinib, a Novel JAK1-Preferential Inhibitor for the Treatment of Rheumatoid Arthritis: An Overview from Clinical Trials. GLPG0634 0-10 Janus kinase 1 Homo sapiens 20-24 33909185-3 2021 Upadacitinib, a JAK1 inhibitor, has also been evaluated in a phase III trial for its efficacy and safety in AS. upadacitinib 0-12 Janus kinase 1 Homo sapiens 16-20 33870531-1 2021 Baricitinib is a JAK1/2 inhibitor first approved for treating moderate to severe rheumatoid arthritis but later showed considerable efficacy in the control of exaggerated inflammatory responses that occur in a wide range of diseases. baricitinib 0-11 Janus kinase 1 Homo sapiens 17-23 33954282-1 2021 Even after development of the JAK1/JAK2 inhibitor ruxolitinib, myeloproliferative neoplasm (MPN) patients require novel therapeutic options. ruxolitinib 50-61 Janus kinase 1 Homo sapiens 30-34 33517393-9 2021 Interestingly, the STAT3 phosphorylation could be inhibited with ruxolitinib as well as tofacitinib, which are clinically approved JAK1 and JAK3 (to lesser extent JAK2 and JAK1) inhibitors, respectively. ruxolitinib 65-76 Janus kinase 1 Homo sapiens 172-176 33517393-9 2021 Interestingly, the STAT3 phosphorylation could be inhibited with ruxolitinib as well as tofacitinib, which are clinically approved JAK1 and JAK3 (to lesser extent JAK2 and JAK1) inhibitors, respectively. tofacitinib 88-99 Janus kinase 1 Homo sapiens 131-135 33517393-9 2021 Interestingly, the STAT3 phosphorylation could be inhibited with ruxolitinib as well as tofacitinib, which are clinically approved JAK1 and JAK3 (to lesser extent JAK2 and JAK1) inhibitors, respectively. tofacitinib 88-99 Janus kinase 1 Homo sapiens 172-176 33981229-0 2021 Ruxolitinib, a JAK1/2 Inhibitor, Ameliorates Cytokine Storm in Experimental Models of Hyperinflammation Syndrome. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 33740386-3 2021 Filgotinib has demonstrated preferential inhibition of JAK1-dependent cytokine signaling in in vitro assays. GLPG0634 0-10 Janus kinase 1 Homo sapiens 55-59 33936080-6 2021 To the best of our knowledge, this is the first case study depicting an SLE patient with refractory alopecia who experienced impressive hair regrowth with the JAK1/3 inhibitor tofacitinib therapy, which contributes to expanding the field of possible uses of tofacitinib in SLE patients with difficult-to-treat cutaneous involvement, including severe alopecia. tofacitinib 176-187 Janus kinase 1 Homo sapiens 159-165 33992887-4 2021 Similarly, preliminary studies have shown that JAK1/2 inhibitor treatment with ruxolitinib or baricitinib may decrease mortality by dampening the deadly cytokine storm, which - in addition to the virus itself - also contributes to multi-organ thrombosis and multi-organ failure. ruxolitinib 79-90 Janus kinase 1 Homo sapiens 47-53 33936080-6 2021 To the best of our knowledge, this is the first case study depicting an SLE patient with refractory alopecia who experienced impressive hair regrowth with the JAK1/3 inhibitor tofacitinib therapy, which contributes to expanding the field of possible uses of tofacitinib in SLE patients with difficult-to-treat cutaneous involvement, including severe alopecia. tofacitinib 258-269 Janus kinase 1 Homo sapiens 159-165 33992887-4 2021 Similarly, preliminary studies have shown that JAK1/2 inhibitor treatment with ruxolitinib or baricitinib may decrease mortality by dampening the deadly cytokine storm, which - in addition to the virus itself - also contributes to multi-organ thrombosis and multi-organ failure. baricitinib 94-105 Janus kinase 1 Homo sapiens 47-53 33847204-3 2021 Among these, Filgotinib (FIL) has been developed as Janus kinase1 (JAK1) selective inhibitor, specifically targeting key pro-inflammatory mediators in RA pathogenesis. GLPG0634 13-23 Janus kinase 1 Homo sapiens 52-65 33847204-3 2021 Among these, Filgotinib (FIL) has been developed as Janus kinase1 (JAK1) selective inhibitor, specifically targeting key pro-inflammatory mediators in RA pathogenesis. GLPG0634 13-23 Janus kinase 1 Homo sapiens 67-71 33830087-3 2021 We previously showed that therapeutic targeting of JAK/STAT pathways using the first-generation JAK1/2 inhibitor, ruxolitinib, and the pan-JAK inhibitor, tofacitinib, was highly effective in the treatment of human AA, as well as prevention and reversal of AA in the C3H/HeJ mouse model. ruxolitinib 114-125 Janus kinase 1 Homo sapiens 96-102 33845867-10 2021 INTERVENTION AND COMPARATOR: RUXOLITINIB (RUX) (14 days): An oral selective and potent inhibitor of Janus Associated Kinases (JAK1 and JAK2) and cell proliferation (Verstovek, 2010). ruxolitinib 29-40 Janus kinase 1 Homo sapiens 126-130 33845867-10 2021 INTERVENTION AND COMPARATOR: RUXOLITINIB (RUX) (14 days): An oral selective and potent inhibitor of Janus Associated Kinases (JAK1 and JAK2) and cell proliferation (Verstovek, 2010). ruxolitinib 29-32 Janus kinase 1 Homo sapiens 126-130 33827897-8 2021 Ruxolitinib, a JAK1/2 inhibitor, normalized interferon signature genes and all complement gene transcripts induced by SARS-CoV-2 in lung epithelial cell lines, but did not affect NF-kappaB-regulated genes. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 33222197-1 2021 Ruxolitinib (RUX), the first JAK1/JAK2 inhibitor approved for myelofibrosis (MF) therapy, has recently been associated with the occurrence of second primary malignancies (SPMs), mainly lymphomas and non-melanoma skin cancers (NMSCs). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 29-33 33222197-1 2021 Ruxolitinib (RUX), the first JAK1/JAK2 inhibitor approved for myelofibrosis (MF) therapy, has recently been associated with the occurrence of second primary malignancies (SPMs), mainly lymphomas and non-melanoma skin cancers (NMSCs). ruxolitinib 13-16 Janus kinase 1 Homo sapiens 29-33 33744327-3 2021 OBJECTIVE: To determine whether GDC-0214 reduces fractional exhaled nitric oxide (FeNO), a JAK1-dependent biomarker of airway inflammation, in patients with mild asthma. gdc-0214 32-40 Janus kinase 1 Homo sapiens 91-95 33795598-1 2022 BACKGROUND: Ruxolitinib, a JAK1/2 inhibitor, is used to treat chronic graft-versus-host-disease (cGVHD) in adult allogeneic hematopoietic stem cell transplant patients, but experience in children is limited, perhaps due to lack of pediatric dosing information. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 27-33 32989920-1 2021 Filgotinib (FIL) is a potent and selective JAK1 inhibitor in clinical development for treatment of severe inflammatory diseases. GLPG0634 0-10 Janus kinase 1 Homo sapiens 43-47 32989920-1 2021 Filgotinib (FIL) is a potent and selective JAK1 inhibitor in clinical development for treatment of severe inflammatory diseases. GLPG0634 12-15 Janus kinase 1 Homo sapiens 43-47 33423550-3 2021 Momelotinib (MMB) has been investigated in over 820 patients with MF and possesses a pharmacological and clinical profile differentiated from other JAKi by inhibition of JAK1, JAK2 and ACVR1. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 170-174 33423550-3 2021 Momelotinib (MMB) has been investigated in over 820 patients with MF and possesses a pharmacological and clinical profile differentiated from other JAKi by inhibition of JAK1, JAK2 and ACVR1. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 13-16 Janus kinase 1 Homo sapiens 170-174 32814839-0 2021 Compassionate use of JAK1/2 inhibitor ruxolitinib for severe COVID-19: a prospective observational study. ruxolitinib 38-49 Janus kinase 1 Homo sapiens 21-27 32814839-2 2021 Ruxolitinib is a JAK1/JAK2 inhibitor with potent anti-inflammatory properties. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-21 33741556-0 2021 JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib. GLPG0634 103-113 Janus kinase 1 Homo sapiens 0-3 33741556-0 2021 JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib. upadacitinib 115-127 Janus kinase 1 Homo sapiens 0-3 33741556-0 2021 JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib. tofacitinib 129-140 Janus kinase 1 Homo sapiens 0-3 33741556-0 2021 JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib. baricitinib 145-156 Janus kinase 1 Homo sapiens 0-3 33741556-7 2021 JAK1-dependent pathways (interferon (IFN)alpha/pSTAT5, interleukin (IL)-6/pSTAT1) were among the most potently inhibited by all JAKinibs in healthy and RA blood, with filgotinib exhibiting the greatest selectivity for JAK1 pathways. GLPG0634 167-177 Janus kinase 1 Homo sapiens 0-4 33741556-9 2021 Ex vivo pharmacodynamic data from phase 1 healthy volunteers clinically confirmed JAK1 selectivity of filgotinib. GLPG0634 102-112 Janus kinase 1 Homo sapiens 82-86 33741556-10 2021 CONCLUSION: Filgotinib inhibited JAK1-mediated signalling similarly to other JAKinibs, but with less inhibition of JAK2-dependent and JAK3-dependent pathways, providing a mechanistic rationale for its apparently differentiated efficacy:safety profile. GLPG0634 12-22 Janus kinase 1 Homo sapiens 33-37 33618802-5 2021 In this study, they show that inhibition of granzyme B with the Jak1/3 inhibitor, tofacitinib, is associated with decreased severity of cutaneous lesions without the attenuation of T helper type 1 signaling or parasite control. tofacitinib 82-93 Janus kinase 1 Homo sapiens 64-70 33662027-0 2021 Differential responses to folic acid in an established keloid fibroblast cell line are mediated by JAK1/2 and STAT3. Folic Acid 26-36 Janus kinase 1 Homo sapiens 99-105 33662027-5 2021 In healthy volunteer fibroblasts, folic acid exposure recapitulated the exaggerated closure and hyper-glycolytic state of keloid fibroblasts through JAK1/2- and STAT3-dependent pathways. Folic Acid 34-44 Janus kinase 1 Homo sapiens 149-155 32648334-1 2021 This phase 1 study characterized the effect of multiple doses of upadacitinib, an oral Janus kinase 1 selective inhibitor, on the pharmacokinetics of the cytochrome P450 (CYP) 2B6 substrate bupropion. upadacitinib 65-77 Janus kinase 1 Homo sapiens 87-101 32648334-1 2021 This phase 1 study characterized the effect of multiple doses of upadacitinib, an oral Janus kinase 1 selective inhibitor, on the pharmacokinetics of the cytochrome P450 (CYP) 2B6 substrate bupropion. Bupropion 190-199 Janus kinase 1 Homo sapiens 87-101 33693561-2 2022 Ruxolitinib, a Jak 1/2 inhibitor, reduces systemic inflammation for individuals without HIV and HIV reservoir markers ex vivo. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-22 33600915-1 2021 BACKGROUND: Baricitinib, an oral, selective Janus kinase (JAK)1/JAK2 inhibitor, is being studied for moderate-to-severe atopic dermatitis (AD) in adults. baricitinib 12-23 Janus kinase 1 Homo sapiens 44-63 33495807-11 2021 The inhibition of SOCS3 significantly activated JAK1/STAT3 signaling, as well as enhancing the levels of TNF-alpha, IL-6 and IL-1beta, and promoting apoptosis, which was reversed by the JAK1 inhibitor Tofacitinib. tofacitinib 201-212 Janus kinase 1 Homo sapiens 186-190 33598678-8 2021 Targeting JAK/STAT pathway with the JAK1/2 inhibitor ruxolitinib or HDAC with belinostat both independently increased dependence on BCL-2 but not MCL-1, thereby sensitizing T-PLL cells to venetoclax. ruxolitinib 53-64 Janus kinase 1 Homo sapiens 10-13 33598678-8 2021 Targeting JAK/STAT pathway with the JAK1/2 inhibitor ruxolitinib or HDAC with belinostat both independently increased dependence on BCL-2 but not MCL-1, thereby sensitizing T-PLL cells to venetoclax. ruxolitinib 53-64 Janus kinase 1 Homo sapiens 36-42 33598678-8 2021 Targeting JAK/STAT pathway with the JAK1/2 inhibitor ruxolitinib or HDAC with belinostat both independently increased dependence on BCL-2 but not MCL-1, thereby sensitizing T-PLL cells to venetoclax. belinostat 78-88 Janus kinase 1 Homo sapiens 10-13 33495807-11 2021 The inhibition of SOCS3 significantly activated JAK1/STAT3 signaling, as well as enhancing the levels of TNF-alpha, IL-6 and IL-1beta, and promoting apoptosis, which was reversed by the JAK1 inhibitor Tofacitinib. tofacitinib 201-212 Janus kinase 1 Homo sapiens 48-52 33658996-5 2020 Ruxolitinib cream is a potent and selective JAK1/2 inhibitor currently undergoing clinical evaluation in adults with mild-to-moderate AD (NCT03745638, NCT03920852 and NCT03745651). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 44-50 33586434-4 2022 Especially, compounds 15d and 15h potently inhibited JAK1/2/3 and HDAC1/6 and displayed antiproliferative and proapoptotic activities in triple-negative breast cancer cell lines. (1s)-1-(1-{3-[4-(1,3-Benzothiazol-2-Ylamino)phenoxy]pyrazin-2-Yl}piperidin-4-Yl)ethanol 30-33 Janus kinase 1 Homo sapiens 53-61 33587766-2 2021 (1) Tofacitinib is an effective oral JAK 1/3 inhibitor that can block IL-2, IL-7 and IL-6 and is reported as an option for alopecia areata treatment. tofacitinib 4-15 Janus kinase 1 Homo sapiens 37-44 33475190-9 2021 In addition, activation of the Jak1/Stat3 signaling pathway leads to high calcitriol levels and low parathyroid hormone production. Calcitriol 74-84 Janus kinase 1 Homo sapiens 31-35 33634982-0 2021 Arsenic trioxide induces differentiation of cancer stem cells in hepatocellular carcinoma through inhibition of LIF/JAK1/STAT3 and NF-kB signaling pathways synergistically. Arsenic Trioxide 0-16 Janus kinase 1 Homo sapiens 116-120 33634982-8 2021 Synergistic inhibition of the LIF/JAK1/STAT3 and NF-kB signaling pathways by ATO and 5-FU/cisplatin is a potential molecular mechanism underlying the differentiation effect. Arsenic Trioxide 77-80 Janus kinase 1 Homo sapiens 34-38 33634982-8 2021 Synergistic inhibition of the LIF/JAK1/STAT3 and NF-kB signaling pathways by ATO and 5-FU/cisplatin is a potential molecular mechanism underlying the differentiation effect. Fluorouracil 85-89 Janus kinase 1 Homo sapiens 34-38 33634982-8 2021 Synergistic inhibition of the LIF/JAK1/STAT3 and NF-kB signaling pathways by ATO and 5-FU/cisplatin is a potential molecular mechanism underlying the differentiation effect. Cisplatin 90-99 Janus kinase 1 Homo sapiens 34-38 33634982-9 2021 CONCLUSIONS: ATO induced the differentiation of HCC CSCs and potentiated the cytotoxic effects of 5-FU/cisplatin through synergistic inhibition of the LIF/JAK1/STAT3 and NF-kB signaling pathways. Arsenic Trioxide 13-16 Janus kinase 1 Homo sapiens 155-159 33634982-9 2021 CONCLUSIONS: ATO induced the differentiation of HCC CSCs and potentiated the cytotoxic effects of 5-FU/cisplatin through synergistic inhibition of the LIF/JAK1/STAT3 and NF-kB signaling pathways. Fluorouracil 98-102 Janus kinase 1 Homo sapiens 155-159 33634982-9 2021 CONCLUSIONS: ATO induced the differentiation of HCC CSCs and potentiated the cytotoxic effects of 5-FU/cisplatin through synergistic inhibition of the LIF/JAK1/STAT3 and NF-kB signaling pathways. Cisplatin 103-112 Janus kinase 1 Homo sapiens 155-159 31916502-0 2021 Molecular modeling studies of pyrrolo[2,3-d]pyrimidin-4-amine derivatives as JAK1 inhibitors based on 3D-QSAR, molecular docking, molecular dynamics (MD) and MM-PBSA calculations. 7-deazaadenine 30-61 Janus kinase 1 Homo sapiens 77-81 33597887-7 2020 In addition, curcumin significantly inhibited the activation of the JAK1/STAT5 signaling pathway, downregulation of JAK1, STAT5, and p-STAT5 proteins in colon tissue, and upregulation of PIAS1 proteins. Curcumin 13-21 Janus kinase 1 Homo sapiens 68-72 33597887-7 2020 In addition, curcumin significantly inhibited the activation of the JAK1/STAT5 signaling pathway, downregulation of JAK1, STAT5, and p-STAT5 proteins in colon tissue, and upregulation of PIAS1 proteins. Curcumin 13-21 Janus kinase 1 Homo sapiens 116-120 33597887-8 2020 These results suggested that curcumin effectively regulated the differentiation of naive, TCM, and TEM cells in the peripheral blood to alleviate DSS-induced experimental colitis, which might be related to the inhibition of JAK1/STAT5 signaling activity. Curcumin 29-37 Janus kinase 1 Homo sapiens 224-228 33597887-8 2020 These results suggested that curcumin effectively regulated the differentiation of naive, TCM, and TEM cells in the peripheral blood to alleviate DSS-induced experimental colitis, which might be related to the inhibition of JAK1/STAT5 signaling activity. Dextran Sulfate 146-149 Janus kinase 1 Homo sapiens 224-228 32926462-2 2021 Baricitinib, an oral, reversible, selective inhibitor of JAK1/JAK2, is in late-stage development for adult patients with moderate-to-severe AD. baricitinib 0-11 Janus kinase 1 Homo sapiens 57-61 33465556-6 2021 Notably, STAT3 knockdown or upstream inhibition through the JAK1/2 kinase inhibitor ruxolitinib prevented opioid-induced breast cancer cell metastasis and migration in vitro and in vivo. ruxolitinib 84-95 Janus kinase 1 Homo sapiens 60-66 31916502-0 2021 Molecular modeling studies of pyrrolo[2,3-d]pyrimidin-4-amine derivatives as JAK1 inhibitors based on 3D-QSAR, molecular docking, molecular dynamics (MD) and MM-PBSA calculations. poly(tetramethylene succinate-co-tetramethylene adipate) 161-165 Janus kinase 1 Homo sapiens 77-81 31916502-5 2021 In this study, we have performed three-dimensional quantitative structure-activity relationship (3 D-QSAR), molecular docking, molecular dynamics (MD) and free energy calculations on a series of pyrrolo[2,3-d]pyrimidin-4-amine JAK1 inhibitors. 7-deazaadenine 195-226 Janus kinase 1 Homo sapiens 227-231 31916502-9 2021 Analysis of the MD results of the most active compound (compound 49) with JAK1 showed the formation of H-bond interactions with residues Glu957, Leu959 and Gly887 and water-mediated H-bond interaction with Gly887 and His885. Water 167-172 Janus kinase 1 Homo sapiens 74-78 31916502-12 2021 MM-PBSA based free energy calculations indicated that the designed compounds were able to form stable binding with JAK1 primarily through electrostatic interactions and van der Waal interactions. poly(tetramethylene succinate-co-tetramethylene adipate) 3-7 Janus kinase 1 Homo sapiens 115-119 33428419-0 2021 Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors. n-methyl-pyrrolo[2,3-b]pyridine-5-carboxamide 39-84 Janus kinase 1 Homo sapiens 100-104 33509955-5 2021 METHODS: Assessment of cell senescence in lungs and cultured lung cells from patients with COPD and controls subjected to PLA2R1 knock-down, PLA2R1 gene transduction and treatment with the JAK1/2 inhibitor ruxolitinib. ruxolitinib 206-217 Janus kinase 1 Homo sapiens 189-195 33504485-1 2021 OBJECTIVE: To evaluate the efficacy and safety of the Janus kinase-1-preferential inhibitor filgotinib versus placebo or tumour necrosis factor-alpha inhibitor therapy in patients with active rheumatoid arthritis (RA) despite ongoing treatment with methotrexate (MTX). GLPG0634 92-102 Janus kinase 1 Homo sapiens 54-68 33434286-1 2021 Itacitinib is a potent, selective JAK-1 inhibitor currently in development for the treatment of chronic graft-versus-host-disease (GVHD) in combination with corticosteroids. INCB039110 0-10 Janus kinase 1 Homo sapiens 34-39 32986914-3 2021 Herein we show that such ring systems can be useful for medicinal chemistry at the example of the enantioselective synthesis of triquinazine, a novel chiral piperazine analog derived from angular triquinane, and it"s use to design a nanomolar and selective inhibitor of Janus Kinase 1 related to the marketed drug Tofacitinib useful to treat auto-immune diseases. triquinazine 128-140 Janus kinase 1 Homo sapiens 270-284 32986914-3 2021 Herein we show that such ring systems can be useful for medicinal chemistry at the example of the enantioselective synthesis of triquinazine, a novel chiral piperazine analog derived from angular triquinane, and it"s use to design a nanomolar and selective inhibitor of Janus Kinase 1 related to the marketed drug Tofacitinib useful to treat auto-immune diseases. Piperazine 157-167 Janus kinase 1 Homo sapiens 270-284 32986914-3 2021 Herein we show that such ring systems can be useful for medicinal chemistry at the example of the enantioselective synthesis of triquinazine, a novel chiral piperazine analog derived from angular triquinane, and it"s use to design a nanomolar and selective inhibitor of Janus Kinase 1 related to the marketed drug Tofacitinib useful to treat auto-immune diseases. triquinane 196-206 Janus kinase 1 Homo sapiens 270-284 32986914-3 2021 Herein we show that such ring systems can be useful for medicinal chemistry at the example of the enantioselective synthesis of triquinazine, a novel chiral piperazine analog derived from angular triquinane, and it"s use to design a nanomolar and selective inhibitor of Janus Kinase 1 related to the marketed drug Tofacitinib useful to treat auto-immune diseases. tofacitinib 314-325 Janus kinase 1 Homo sapiens 270-284 33278358-2 2021 Baricitinib, a clinically approved JAK1/JAK2 inhibitor, is currently being investigated in COVID-19 clinical trials. baricitinib 0-11 Janus kinase 1 Homo sapiens 35-39 33452004-1 2021 OBJECTIVES: To investigate efficacy and safety of the Janus kinase-1 inhibitor filgotinib in patients with active rheumatoid arthritis (RA) with limited or no prior methotrexate (MTX) exposure. GLPG0634 79-89 Janus kinase 1 Homo sapiens 54-68 33489899-8 2020 Accordingly, ruxolitinib is the only selective JAK1 and JAK2-inhibitor approved for the treatment of myelofibrosis and aGVHD. ruxolitinib 13-24 Janus kinase 1 Homo sapiens 47-51 33129109-4 2021 We previously performed a high-throughput screen that demonstrated additive/synergistic activity of Ruxolitinib, a JAK1/2 inhibitor, with AZD8055, an mTORC1/C2 inhibitor. ruxolitinib 100-111 Janus kinase 1 Homo sapiens 115-121 32783069-8 2021 RESULTS: Stimulation with IL-17A induced STAT3 phosphorylation, which was inhibited by the pretreatment with JAK2 inhibitor AZD1480 or JAK1/3 inhibitor tofacitinib. tofacitinib 152-163 Janus kinase 1 Homo sapiens 135-141 32829958-2 2021 Tofacitinib is one of these inhibitors targeting JAK1 and JAK3, and its efficacy has been demonstrated in the treatment of moderate to severe ulcerative colitis (UC). tofacitinib 0-11 Janus kinase 1 Homo sapiens 49-53 33397481-1 2021 Baricitinib is an oral selective inhibitor of Janus kinase (JAK)1 and JAK2 that has proved effective and well tolerated in the treatment of rheumatoid arthritis (RA) in an extensive programme of clinical studies of patients with moderate-to-severe disease. baricitinib 0-11 Janus kinase 1 Homo sapiens 46-65 33502484-1 2021 Importance: Ruxolitinib, a selective inhibitor of the Janus kinases 1/2 signaling pathway, has shown a significant response in steroid-refractory chronic graft-vs-host disease (SR-cGVHD), a major cause of morbidity and mortality in individuals who have undergone allogeneic hematopoietic stem cell transplantation (HSCT). ruxolitinib 12-23 Janus kinase 1 Homo sapiens 54-71 33502484-1 2021 Importance: Ruxolitinib, a selective inhibitor of the Janus kinases 1/2 signaling pathway, has shown a significant response in steroid-refractory chronic graft-vs-host disease (SR-cGVHD), a major cause of morbidity and mortality in individuals who have undergone allogeneic hematopoietic stem cell transplantation (HSCT). Steroids 127-134 Janus kinase 1 Homo sapiens 54-71 33129109-4 2021 We previously performed a high-throughput screen that demonstrated additive/synergistic activity of Ruxolitinib, a JAK1/2 inhibitor, with AZD8055, an mTORC1/C2 inhibitor. (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol 138-145 Janus kinase 1 Homo sapiens 115-121 33129109-6 2021 Here, we demonstrated that Upadacitinib, a JAK-1 inhibitor, inhibited the proliferation of cytokine-dependent ATL cell lines and the expression of p-STAT5. upadacitinib 27-39 Janus kinase 1 Homo sapiens 43-48 33374783-0 2020 Curcumin Analogue L48H37 Suppresses Human Osteosarcoma U2OS and MG-63 Cells" Migration and Invasion in Culture by Inhibition of uPA via the JAK/STAT Signaling Pathway. 1-ethyl-3,5-bis[(3,4,5-trimethoxyphenyl)methylidene]piperidin-4-one 18-24 Janus kinase 1 Homo sapiens 140-143 33374783-0 2020 Curcumin Analogue L48H37 Suppresses Human Osteosarcoma U2OS and MG-63 Cells" Migration and Invasion in Culture by Inhibition of uPA via the JAK/STAT Signaling Pathway. Curcumin 0-8 Janus kinase 1 Homo sapiens 140-143 33357183-0 2021 Design and Synthesis of New JAK1 Inhibitors based on SulfonamideTriazine Conjugates. sulfonamidetriazine 53-72 Janus kinase 1 Homo sapiens 28-32 33357183-1 2021 AIMS: Design of sulfonamide-triazine derivatives as JAK1 inhibitors. sulfonamide-triazine 16-36 Janus kinase 1 Homo sapiens 52-56 33357183-4 2021 OBJECTIVES: To design new JAK1 inhibitors based on sulfonamides-triazine conjugates capable of binding interactions comparable to observed interactions anchoring potent crystallographic JAK1 inhibitors. Sulfonamides 51-63 Janus kinase 1 Homo sapiens 26-30 33357183-4 2021 OBJECTIVES: To design new JAK1 inhibitors based on sulfonamides-triazine conjugates capable of binding interactions comparable to observed interactions anchoring potent crystallographic JAK1 inhibitors. Sulfonamides 51-63 Janus kinase 1 Homo sapiens 186-190 33357183-4 2021 OBJECTIVES: To design new JAK1 inhibitors based on sulfonamides-triazine conjugates capable of binding interactions comparable to observed interactions anchoring potent crystallographic JAK1 inhibitors. Triazines 64-72 Janus kinase 1 Homo sapiens 26-30 33357183-4 2021 OBJECTIVES: To design new JAK1 inhibitors based on sulfonamides-triazine conjugates capable of binding interactions comparable to observed interactions anchoring potent crystallographic JAK1 inhibitors. Triazines 64-72 Janus kinase 1 Homo sapiens 186-190 33357183-5 2021 METHODS: The crystallographic structures of 4 diverse nanomolar inhibitors complexed within JAK1 were used to guide the synthesis of new diaminotriazine-sulfonamide-based JAK1 inhibitors. diaminotriazine 137-152 Janus kinase 1 Homo sapiens 92-96 33357183-5 2021 METHODS: The crystallographic structures of 4 diverse nanomolar inhibitors complexed within JAK1 were used to guide the synthesis of new diaminotriazine-sulfonamide-based JAK1 inhibitors. diaminotriazine 137-152 Janus kinase 1 Homo sapiens 171-175 33357183-5 2021 METHODS: The crystallographic structures of 4 diverse nanomolar inhibitors complexed within JAK1 were used to guide the synthesis of new diaminotriazine-sulfonamide-based JAK1 inhibitors. Sulfonamides 153-164 Janus kinase 1 Homo sapiens 92-96 33357183-5 2021 METHODS: The crystallographic structures of 4 diverse nanomolar inhibitors complexed within JAK1 were used to guide the synthesis of new diaminotriazine-sulfonamide-based JAK1 inhibitors. Sulfonamides 153-164 Janus kinase 1 Homo sapiens 171-175 33357183-7 2021 CONCLUSIONS: Crystallographic complexes of diverse JAK1 inhibitors were successfully used to guide the synthesis of novel sulfonamide-triazine-based low micromolar JAK1 inhibitors. sulfonamide-triazine 122-142 Janus kinase 1 Homo sapiens 51-55 33357183-7 2021 CONCLUSIONS: Crystallographic complexes of diverse JAK1 inhibitors were successfully used to guide the synthesis of novel sulfonamide-triazine-based low micromolar JAK1 inhibitors. sulfonamide-triazine 122-142 Janus kinase 1 Homo sapiens 164-168 33374783-5 2020 L48H37 decreased the phosphorylation of STAT3, JAK1, JAK2, and JAK3 in U2OS cells, but did not affect the phosphorylation of ERK, JNK, p38, and Akt. 1-ethyl-3,5-bis[(3,4,5-trimethoxyphenyl)methylidene]piperidin-4-one 0-6 Janus kinase 1 Homo sapiens 47-51 33374783-7 2020 Collectively, L48H37 represses the invasion and migration capabilities of U2OS and MG-63 cells by the suppression of uPA expression and the inhibition of JAK/STAT signaling. 1-ethyl-3,5-bis[(3,4,5-trimethoxyphenyl)methylidene]piperidin-4-one 14-20 Janus kinase 1 Homo sapiens 154-157 33323549-6 2020 The signaling pathways associated with JAK1 expression were identified by performing a GSEA. gsea 87-91 Janus kinase 1 Homo sapiens 39-43 33338537-9 2021 Conversely, JAK2 inhibition by Ruxolitinib (JAK1/2 inhibitor) or BMS-911543 (JAK2 inhibitor) abrogated the differentiation from monocytes into IDEC. ruxolitinib 31-42 Janus kinase 1 Homo sapiens 44-50 32998963-0 2020 Itacitinib (INCB039110), a JAK1 inhibitor, Reduces Cytokines Associated with Cytokine Release Syndrome Induced by CAR T-Cell Therapy. INCB039110 0-10 Janus kinase 1 Homo sapiens 27-31 33338001-1 2021 OBJECTIVES: Baricitinib, an oral Janus kinase (JAK) 1-2 inhibitor, is currently used along biologic DMARDs (bDMARDs) after the failure of methotrexate (MTX) in rheumatoid arthritis (RA). baricitinib 12-23 Janus kinase 1 Homo sapiens 33-55 33044324-9 2020 NEAT1 accelerated proliferation and weakened apoptosis of neuroblastoma cells treated by cisplatin by targeting miR-326 through activating JAK1/STAT3 signaling pathway, suggesting that NEAT1 was a potential biomarker against neuroblastoma. Cisplatin 89-98 Janus kinase 1 Homo sapiens 139-143 32776305-0 2020 Selective JAK1 Inhibitors for the Treatment of Atopic Dermatitis: Focus on Upadacitinib and Abrocitinib. upadacitinib 75-87 Janus kinase 1 Homo sapiens 10-14 32776305-7 2020 Upadacitinib and abrocitinib are oral small molecules that inhibit the JAK/STAT pathway by selectively blocking JAK1. upadacitinib 0-12 Janus kinase 1 Homo sapiens 112-116 32818555-1 2020 Ruxolitinib is an oral JAK1/2 inhibitor that is approved for use in patients with intermediate and high-risk myelofibrosis (MF) based on its proven spleen and symptom burden reduction. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 23-29 32998963-0 2020 Itacitinib (INCB039110), a JAK1 inhibitor, Reduces Cytokines Associated with Cytokine Release Syndrome Induced by CAR T-Cell Therapy. INCB039110 12-22 Janus kinase 1 Homo sapiens 27-31 32998963-7 2020 RESULTS: We report that itacitinib, a potent, selective JAK1 inhibitor, was able to significantly and dose-dependently reduce levels of multiple cytokines implicated in CRS in several in vitro and in vivo models. INCB039110 24-34 Janus kinase 1 Homo sapiens 56-60 32876903-1 2020 INTRODUCTION: Baricitinib is an oral selective inhibitor of Janus kinase (JAK) 1 and JAK 2, which has demonstrated significant efficacy in patients with moderately to severely active rheumatoid arthritis (RA). baricitinib 14-25 Janus kinase 1 Homo sapiens 60-80 32801162-5 2020 As a result, increased P-Tyr was detected in previously reported TSLP-activated tyrosine kinases and substrates, including JAK1, JAK2, STAT5, and ERK1/2. Phosphotyrosine 23-28 Janus kinase 1 Homo sapiens 123-127 32789663-7 2020 Ruxolitinib, a tyrosine kinase inhibitor selective for JAK1, 2, blocks many pro- and anti-inflammatory cytokines including IL6. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 55-59 33354610-0 2021 Bridging to a selective Janus kinase 1 inhibitor in severe atopic dermatitis: An instructive case with upadacitinib. upadacitinib 103-115 Janus kinase 1 Homo sapiens 24-38 32738501-1 2020 Ruxolitinib, a selective Janus kinase (JAK)1/2 inhibitor, has recently been proposed for steroid refractory chronic graft-versus host disease (cGVHD) after allogeneic hematopoietic stem cell transplantation (HSCT), particularly in severe skin cGVHD. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 39-46 32738501-1 2020 Ruxolitinib, a selective Janus kinase (JAK)1/2 inhibitor, has recently been proposed for steroid refractory chronic graft-versus host disease (cGVHD) after allogeneic hematopoietic stem cell transplantation (HSCT), particularly in severe skin cGVHD. Steroids 89-96 Janus kinase 1 Homo sapiens 39-46 33162993-8 2020 Also, Janus Associated Kinases (JAK1 and JAK2) inhibitors, such as itacitinib (JAK1) and ruxolitinib (JAK1 and 2), are promising in the treatment of cGvHD. INCB039110 67-77 Janus kinase 1 Homo sapiens 32-36 32593209-4 2020 Here, we report a compelling case of a 55-yo patient with proven COVID-19 pneumonia, who was taking the JAK1/2 inhibitor ruxolitinib in-label for co-existing primary myelofibrosis for 15 months prior to coronavirus infection. ruxolitinib 121-132 Janus kinase 1 Homo sapiens 104-110 33102814-0 2020 Cucurbitacin E and I target the JAK/STAT pathway and induce apoptosis in Sezary cells. cucurbitacin E 0-14 Janus kinase 1 Homo sapiens 32-35 33102814-9 2020 Furthermore, while JAK2 inhibition leads to decreased viability in SeAx cells (IC50 of 9.98 and 29.15 muM for AZD1480 and ruxolitinib respectively), both JAK1 and JAK3 do not. ruxolitinib 122-133 Janus kinase 1 Homo sapiens 154-158 32861662-0 2020 Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseases. INCB039110 32-42 Janus kinase 1 Homo sapiens 88-92 32861662-0 2020 Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseases. INCB039110 44-54 Janus kinase 1 Homo sapiens 88-92 32861662-3 2020 We used recombinant enzymes and primary human lymphocytes to assess the JAK1 specificity of itacitinib (INCB039110) and study inhibition of signal transducers and activators of transcription (STAT) signaling. INCB039110 92-102 Janus kinase 1 Homo sapiens 72-76 32861662-5 2020 Itacitinib is a potent and selective JAK1 inhibitor when profiled against the other JAK family members. INCB039110 0-10 Janus kinase 1 Homo sapiens 37-41 33055240-6 2020 Through independent mechanisms, overexpression of NLRC5 (nucleotide-binding oligomerization domain-like receptor family caspase recruitment domain containing 5) and intratumoral delivery of BO-112, a potent nanoplexed version of polyinosinic:polycytidylic acid (poly I:C), each restored the efficacy of ACT against B16-Jak1 KO tumors. bo-112 190-196 Janus kinase 1 Homo sapiens 319-323 33332480-3 2020 Upadacitinib tartrate (Rinvoq), a selective and reversible JAK1 inhibitor, inhibited interleukin (IL)-6 and IL-7 and ameliorated adjuvant-induced arthritis in preclinical studies. Upadacitinib tartrate 0-21 Janus kinase 1 Homo sapiens 59-63 33332480-3 2020 Upadacitinib tartrate (Rinvoq), a selective and reversible JAK1 inhibitor, inhibited interleukin (IL)-6 and IL-7 and ameliorated adjuvant-induced arthritis in preclinical studies. upadacitinib 23-29 Janus kinase 1 Homo sapiens 59-63 32777582-2 2020 This case report on a critically ill patient with secondary hemophagocytic lymphohistiocytosis due to falciparum malaria treated successfully with ruxolitinib, demonstrates that JAK1/2 inhibition might be a promising treatment option for severe cases. ruxolitinib 147-158 Janus kinase 1 Homo sapiens 178-184 33114733-1 2020 Ruxolitinib (RUX), a JAK1/JAK2 inhibitor, is approved for second-line therapy in patients with polycythemia vera (PV) who are resistant or intolerant to hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-25 33114733-1 2020 Ruxolitinib (RUX), a JAK1/JAK2 inhibitor, is approved for second-line therapy in patients with polycythemia vera (PV) who are resistant or intolerant to hydroxyurea. ruxolitinib 13-16 Janus kinase 1 Homo sapiens 21-25 33194706-3 2020 MS is treated with ruxolitinib, a selective JAK1 and JAK2 inhibitor. ruxolitinib 19-30 Janus kinase 1 Homo sapiens 44-48 33193430-8 2020 Currently many trials with JAKinibs are ongoing for PsA and axSpA, with one phase III trial of upadacitinib (selective JAK1 inhibitor) showing good therapeutic response in active radiographic axSpA. upadacitinib 95-107 Janus kinase 1 Homo sapiens 119-123 33087723-5 2020 Accordingly, patient-derived lymphocytes exhibit increased STAT activation in vitro in response to interferon-gamma, IL-2 and IL-4 that is reverted by the JAK1/JAK2 inhibitor ruxolitinib. ruxolitinib 175-186 Janus kinase 1 Homo sapiens 155-159 32870648-4 2020 mVP40 also inhibits interferon (IFN) signaling by inhibiting the function of Janus kinase 1 (JAK1). mvp40 0-5 Janus kinase 1 Homo sapiens 77-91 32870648-4 2020 mVP40 also inhibits interferon (IFN) signaling by inhibiting the function of Janus kinase 1 (JAK1). mvp40 0-5 Janus kinase 1 Homo sapiens 93-97 33162993-8 2020 Also, Janus Associated Kinases (JAK1 and JAK2) inhibitors, such as itacitinib (JAK1) and ruxolitinib (JAK1 and 2), are promising in the treatment of cGvHD. INCB039110 67-77 Janus kinase 1 Homo sapiens 79-83 33162993-8 2020 Also, Janus Associated Kinases (JAK1 and JAK2) inhibitors, such as itacitinib (JAK1) and ruxolitinib (JAK1 and 2), are promising in the treatment of cGvHD. ruxolitinib 89-100 Janus kinase 1 Homo sapiens 32-36 33162993-8 2020 Also, Janus Associated Kinases (JAK1 and JAK2) inhibitors, such as itacitinib (JAK1) and ruxolitinib (JAK1 and 2), are promising in the treatment of cGvHD. ruxolitinib 89-100 Janus kinase 1 Homo sapiens 102-112 33028646-8 2020 To our knowledge, this report provides the most detailed look yet at defective JAK1 signaling in the context of dMMR and immunotherapy resistance. dmmr 112-116 Janus kinase 1 Homo sapiens 79-83 32697338-3 2020 Similarly, the role of the JAK1/JAK2 inhibitor ruxolitinib (RUX) is not well defined in patients who have increased blasts. ruxolitinib 47-58 Janus kinase 1 Homo sapiens 27-31 32788396-1 2020 OBJECTIVES: To evaluate the incidence of infection in patients with active rheumatoid arthritis (RA) treated with baricitinib, an oral selective Janus kinase (JAK)1 and JAK2 inhibitor. baricitinib 114-125 Janus kinase 1 Homo sapiens 145-164 32592721-0 2020 Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysis. Cardenolides 8-20 Janus kinase 1 Homo sapiens 72-76 32697338-3 2020 Similarly, the role of the JAK1/JAK2 inhibitor ruxolitinib (RUX) is not well defined in patients who have increased blasts. ruxolitinib 60-63 Janus kinase 1 Homo sapiens 27-31 32329368-7 2020 Quercetin treatment led to significantly higher levels of p-PI3K, p-AKT, p-JAK1, and p-STAT3. Quercetin 0-9 Janus kinase 1 Homo sapiens 75-79 32703039-5 2020 Baricitinib, a novel JAK1/JAK2 inhibitor is currently under investigation in AD clinical trials. baricitinib 0-11 Janus kinase 1 Homo sapiens 21-25 32329368-9 2020 CONCLUSION: Quercetin can mitigate LPS-induced injury in HOKs by downregulating miR-22, thereby activating PI3K/AKT and JAK1/STAT3 cascades. Quercetin 12-21 Janus kinase 1 Homo sapiens 120-124 33037080-8 2020 CONCLUSION: Baricitinib treatment induced significant reduction in the RNA expression of a network of genes associated with the JAK/STAT pathway, cytokine signalling and SLE pathogenesis. baricitinib 12-23 Janus kinase 1 Homo sapiens 128-131 32768575-10 2020 Inhibition of the IL-6/JAK/STAT3 pathway with the JAK1/2 specific inhibitor, AZD1480, reversed the associated increase of IL-6. AZD 1480 77-84 Janus kinase 1 Homo sapiens 50-56 33092696-13 2020 In addition, we pretreated the JAK1 or STAT3 inhibitor with testosterone to block the signaling transduction before CFT073 and J96 UPEC infection, and found the significant restoring in both the sizes of IBCs and bacterial numbers in RWPE-1 cells. Testosterone 60-72 Janus kinase 1 Homo sapiens 31-35 32943176-0 2020 Development and validation of an HPLC-MS/MS method for the determination of filgotinib, a selective Janus kinase 1 inhibitor: Application to a metabolic stability study. GLPG0634 76-86 Janus kinase 1 Homo sapiens 100-114 32915978-0 2020 ACVR1/JAK1/JAK2 inhibitor momelotinib reverses transfusion dependency and suppresses hepcidin in myelofibrosis phase 2 trial. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 26-37 Janus kinase 1 Homo sapiens 6-10 33028675-0 2020 Changes in selected haematological parameters associated with JAK1/JAK2 inhibition observed in patients with rheumatoid arthritis treated with baricitinib. baricitinib 143-154 Janus kinase 1 Homo sapiens 62-66 32822738-8 2020 Activation of the Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway by IFN-gamma was significantly suppressed by salinomycin, via inhibiting the Jak1, Jak2, and STAT1/3 phosphorylation. salinomycin 144-155 Janus kinase 1 Homo sapiens 176-180 32822738-11 2020 These findings suggest that salinomycin suppresses kynurenine synthesis by inhibiting the catalytic activity of IDO1 and its expression by inhibiting the JAK/STAT and NF-kappaB pathways. salinomycin 28-39 Janus kinase 1 Homo sapiens 154-157 32915978-1 2020 Momelotinib (MMB) is a JAK1/2 and ACVR1 inhibitor with demonstrated clinical activity in all 3 hallmarks of myelofibrosis (MF): anemia, constitutional symptoms, and splenomegaly. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 23-29 32915978-1 2020 Momelotinib (MMB) is a JAK1/2 and ACVR1 inhibitor with demonstrated clinical activity in all 3 hallmarks of myelofibrosis (MF): anemia, constitutional symptoms, and splenomegaly. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 13-16 Janus kinase 1 Homo sapiens 23-29 32995780-3 2020 Baricitinib, a clinically approved JAK1/2 inhibitor with potent anti-inflammatory properties is currently being investigated in COVID-19 human clinical trials. baricitinib 0-11 Janus kinase 1 Homo sapiens 35-41 33230423-3 2020 Specifically, cancer therapeutics have been hypothesized to treat cytokine release syndrome in patients with COVID-19, and the JAK1/2 inhibitor, ruxolitinib, is currently being used in a Phase III trial to assess its efficacy. ruxolitinib 145-156 Janus kinase 1 Homo sapiens 127-133 32873116-7 2021 Tofacitinib is an oral pan-JAK inhibitor, primarily of JAK1 and JAK3, that was recently approved by the Food and Drug Administration (FDA) for the chronic treatment of UC in 2018. tofacitinib 0-11 Janus kinase 1 Homo sapiens 55-59 32750333-7 2020 Given these results, the patient was treated with tofacitinib, a JAK inhibitor, leading to the rapid resolution of clinical disease. tofacitinib 50-61 Janus kinase 1 Homo sapiens 65-68 32927842-2 2020 Baricitinib and Tofacitinib both act intracellularly, blocking the ATP-binding side of JAK proteins and thereby the downstream signalling pathway via STAT-3. baricitinib 0-11 Janus kinase 1 Homo sapiens 87-90 32927842-2 2020 Baricitinib and Tofacitinib both act intracellularly, blocking the ATP-binding side of JAK proteins and thereby the downstream signalling pathway via STAT-3. tofacitinib 16-27 Janus kinase 1 Homo sapiens 87-90 32927842-2 2020 Baricitinib and Tofacitinib both act intracellularly, blocking the ATP-binding side of JAK proteins and thereby the downstream signalling pathway via STAT-3. Adenosine Triphosphate 67-70 Janus kinase 1 Homo sapiens 87-90 32895373-4 2020 AH057, the best JAK inhibitor identified, effectively blocked the JAK/STAT pathways by directly inhibiting JAK1/2 kinase activities, and led to compromised cell proliferation and invasion, increased apoptosis, arrested cell cycles, and impaired tumor progression in vitro and in vivo. ah057 0-5 Janus kinase 1 Homo sapiens 107-113 33042272-9 2020 By contrast, pharmacological inhibition of JAK1/2 by ruxolitinib reversed paclitaxel resistance both in vitro and in vivo. ruxolitinib 53-64 Janus kinase 1 Homo sapiens 43-49 32812339-2 2020 Herein, a noninteracting multiphase molecular assembly approach is developed to crystallize tofacitinib, a potent JAK1/3 inhibitor, within a shear-thinning self-assembled fibrillar peptide hydrogel network. tofacitinib 92-103 Janus kinase 1 Homo sapiens 114-120 33042272-9 2020 By contrast, pharmacological inhibition of JAK1/2 by ruxolitinib reversed paclitaxel resistance both in vitro and in vivo. Paclitaxel 74-84 Janus kinase 1 Homo sapiens 43-49 32515665-2 2020 New compounds under investigation, like upadacitinib, with greater selectivity for JAK1 inhibition have recently been approved for the treatment of adults with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to conventional synthetic disease-modifying antirheumatic drugs. upadacitinib 40-52 Janus kinase 1 Homo sapiens 83-87 32515665-4 2020 EXPERT OPINION: Upadacitinib was able to accomplish all the primary and secondary end points in most of the trials, with a safety profile that is similar to the other JAK inhibitors. upadacitinib 16-28 Janus kinase 1 Homo sapiens 167-170 31907296-5 2020 RESULTS: We identified 296 IHCA (45%), 81% of them were mutated in either IL6ST (61%), FRK (8%), STAT3 (5%), GNAS (3%) or JAK1 (2%). 2-(4-imidazoyl)hydrocinnamic acid 27-31 Janus kinase 1 Homo sapiens 122-126 32645632-6 2020 Baricitinib intracellularly inhibits the proinflammatory signal of several cytokines by suppressing Janus kinase (JAK) JAK1/JAK2. baricitinib 0-11 Janus kinase 1 Homo sapiens 119-123 32585295-4 2020 As many of the elevated cytokines signal through Janus kinase (JAK)1/JAK2, inhibition of these pathways with ruxolitinib has the potential to mitigate the COVID-19-associated cytokine storm and reduce mortality. ruxolitinib 109-120 Janus kinase 1 Homo sapiens 49-68 32530345-3 2020 Upadacitinib is a JAK inhibitor engineered to be selective for JAK1, and has recently been approved for use in patients with moderate-to-severe RA. upadacitinib 0-12 Janus kinase 1 Homo sapiens 63-67 32629176-10 2020 Inhibition of JAK1 activity by ruxolitinib or knockdown of JAK1 expression by siRNA significantly inhibits TROY-induced STAT3 activation, GBM cell migration, and decreases resistance to temozolomide. ruxolitinib 31-42 Janus kinase 1 Homo sapiens 14-18 32629176-10 2020 Inhibition of JAK1 activity by ruxolitinib or knockdown of JAK1 expression by siRNA significantly inhibits TROY-induced STAT3 activation, GBM cell migration, and decreases resistance to temozolomide. Temozolomide 186-198 Janus kinase 1 Homo sapiens 14-18 32629176-10 2020 Inhibition of JAK1 activity by ruxolitinib or knockdown of JAK1 expression by siRNA significantly inhibits TROY-induced STAT3 activation, GBM cell migration, and decreases resistance to temozolomide. Temozolomide 186-198 Janus kinase 1 Homo sapiens 59-63 32843425-5 2020 We describe a case of relapsed T-ALL in an adult patient, with two JAK3 activating mutations identified by whole-exome sequencing (WES), leading to hypothesis-based treatment with the JAK1 and JAK3 inhibitor, tofacitinib, following failure of salvage chemotherapy reinduction. tofacitinib 209-220 Janus kinase 1 Homo sapiens 184-188 32904684-12 2020 Further investigations revealed that the constitutive activation of STAT3 may be induced by JAK1 and JAK2, and thus effect the 5-FU resistance by regulating NHE1. Fluorouracil 127-131 Janus kinase 1 Homo sapiens 92-96 32536506-8 2020 Fresh EA NK cells generated high levels of gamma interferon (IFN-gamma), which was abrogated by JAK1/JAK2 inhibition with ruxolitinib, but C/T EA NK cells showed lower IFN-gamma unaffected by JAK1/JAK2 inhibition. ruxolitinib 122-133 Janus kinase 1 Homo sapiens 96-100 32850921-6 2020 Methods: Ruxolitinib, a JAK1 and JAK2 inhibitor, has been successfully used to treat severe immune-mediated diseases, such as graft vs. host disease and Hemophagocytic lymphohistiocytosis. ruxolitinib 9-20 Janus kinase 1 Homo sapiens 24-28 31821750-0 2020 Evaluation of Clinical Cardiac Safety of Itacitinib, a JAK1 Inhibitor, in Healthy Participants. INCB039110 41-51 Janus kinase 1 Homo sapiens 55-59 31821750-1 2020 Itacitinib is a JAK1-selective inhibitor in phase 3 development in graft-versus-host disease. INCB039110 0-10 Janus kinase 1 Homo sapiens 16-20 32808031-0 2020 The JAK1/3 inhibitor tofacitinib suppresses T cell homing and activation in chronic intestinal inflammation. tofacitinib 21-32 Janus kinase 1 Homo sapiens 4-10 32473600-1 2020 Baricitinib is an oral Janus kinase (JAK)1/JAK2 inhibitor approved for the treatment of rheumatoid arthritis (RA) that was independently predicted, using artificial intelligence (AI) algorithms, to be useful for COVID-19 infection via proposed anti-cytokine effects and as an inhibitor of host cell viral propagation. baricitinib 0-11 Janus kinase 1 Homo sapiens 23-42 32636055-1 2020 Ruxolitinib is the first approved JAK1 and JAK2 inhibitor, and is known to interfere with the JAK / STAT signaling pathway, one of the critical cellular signaling pathways involved in the inflammatory response. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 34-38 32598086-6 2020 Prior studies suggest that A77 1726, the active metabolite of leflunomide, inhibits the activity of JAK1 and JAK3. Leflunomide 62-73 Janus kinase 1 Homo sapiens 100-104 33025946-1 2020 Peficitinib hydrobromide is a small Janus kinase inhibitor (JAK1, JAK2, JAK3 and TYK2) molecule for the treatment of rheumatoid arthritis (RA). Peficitinib hydrobromide 0-24 Janus kinase 1 Homo sapiens 60-64 33025946-3 2020 This JAK inhibitor oral drug demonstrated clinical response as once-daily monotherapy in patients with moderate to severe RA, also in combination with methotrexate (MTX), who had an inadequate response to MTX. Methotrexate 151-163 Janus kinase 1 Homo sapiens 5-8 33025946-3 2020 This JAK inhibitor oral drug demonstrated clinical response as once-daily monotherapy in patients with moderate to severe RA, also in combination with methotrexate (MTX), who had an inadequate response to MTX. Methotrexate 165-168 Janus kinase 1 Homo sapiens 5-8 33025946-3 2020 This JAK inhibitor oral drug demonstrated clinical response as once-daily monotherapy in patients with moderate to severe RA, also in combination with methotrexate (MTX), who had an inadequate response to MTX. Methotrexate 205-208 Janus kinase 1 Homo sapiens 5-8 31612426-0 2020 Discovery and evaluation of Atopaxar hydrobromide, a novel JAK1 and JAK2 inhibitor, selectively induces apoptosis of cancer cells with constitutively activated STAT3. E 5555 28-49 Janus kinase 1 Homo sapiens 59-63 32180118-10 2020 We report the potential of JAK1/2 inhibition with ruxolitinib for both CMC and steroid-dependent autoimmunity. ruxolitinib 50-61 Janus kinase 1 Homo sapiens 27-31 32180118-10 2020 We report the potential of JAK1/2 inhibition with ruxolitinib for both CMC and steroid-dependent autoimmunity. Steroids 79-86 Janus kinase 1 Homo sapiens 27-31 31612426-7 2020 Our results suggest that AHB not only blocks constitutively activated and cytokine-induced STAT3 phosphorylation but also inhibits JAK1 and JAK2 phosphorylation. E 5555 25-28 Janus kinase 1 Homo sapiens 131-135 32149388-1 2020 Itacitinib is a novel, selective, Janus kinase 1 inhibitor in development for treatment of graft-versus-host disease. INCB039110 0-10 Janus kinase 1 Homo sapiens 34-48 32359221-0 2020 JAK1/STAT3 regulatory effect of beta-caryophyllene on MG-63 osteosarcoma cells via ROS-induced apoptotic mitochondrial pathway by DNA fragmentation. caryophyllene 32-50 Janus kinase 1 Homo sapiens 0-4 32359221-0 2020 JAK1/STAT3 regulatory effect of beta-caryophyllene on MG-63 osteosarcoma cells via ROS-induced apoptotic mitochondrial pathway by DNA fragmentation. Reactive Oxygen Species 83-86 Janus kinase 1 Homo sapiens 0-4 32359221-7 2020 Our results also showed stimulation of Janus kinase 1/signal transducer and activator of transcription 3 (JAK1/STAT3) signaling pathway in bone cancer MG-63 cells upon BCP treatment along with the induction of proinflammatory genes at the messenger RNA level. caryophyllene 168-171 Janus kinase 1 Homo sapiens 39-53 32359221-7 2020 Our results also showed stimulation of Janus kinase 1/signal transducer and activator of transcription 3 (JAK1/STAT3) signaling pathway in bone cancer MG-63 cells upon BCP treatment along with the induction of proinflammatory genes at the messenger RNA level. caryophyllene 168-171 Janus kinase 1 Homo sapiens 106-110 32359221-8 2020 Overall results suggest that the treatment of MG-63 cells with BCP promotes apoptosis and inflammation via ROS and JAK1/STAT3 signaling pathway. caryophyllene 63-66 Janus kinase 1 Homo sapiens 115-119 31781755-5 2020 In contrast, efficacy of filgotinib, a selective JAK1 inhibitor, in CD patients was demonstrated in the randomized, double-blinded, placebo-controlled phase II FITZROY study. GLPG0634 25-35 Janus kinase 1 Homo sapiens 49-53 31972249-0 2020 Molecular and Cellular Responses to the TYK2/JAK1 Inhibitor, PF 06700841, Reveal Reduction of Skin Inflammation in Plaque Psoriasis: TYK2/JAK1 inhibitor in plaque psoriasis. Platelet Factor 3 61-72 Janus kinase 1 Homo sapiens 45-49 32052886-1 2020 Although recent drugs including biological agents and small molecules targeting key inflammatory mediators have revolutionized the management of different chronic inflammatory diseases, these treatments lead to the development of psoriasis-like skin lesions in 2-5% of treated patients called paradoxical psoriasis.1 Here we report the first case of paradoxical psoriasis induced by baricitinib, a novel janus kinase (JAK) 1/2 inhibitor. baricitinib 383-394 Janus kinase 1 Homo sapiens 404-426 31972249-0 2020 Molecular and Cellular Responses to the TYK2/JAK1 Inhibitor, PF 06700841, Reveal Reduction of Skin Inflammation in Plaque Psoriasis: TYK2/JAK1 inhibitor in plaque psoriasis. Platelet Factor 3 61-72 Janus kinase 1 Homo sapiens 138-142 31972249-2 2020 The tyrosine kinase 2 (TYK2)/Janus kinase 1 (JAK1) inhibitor, PF-06700841, will directly suppress TYK2-dependent IL-12 and IL-23 signaling and JAK1-dependent signaling in cells expressing these signaling molecules, including T cells and keratinocytes. Platelet Factor 3 62-73 Janus kinase 1 Homo sapiens 29-43 31972249-2 2020 The tyrosine kinase 2 (TYK2)/Janus kinase 1 (JAK1) inhibitor, PF-06700841, will directly suppress TYK2-dependent IL-12 and IL-23 signaling and JAK1-dependent signaling in cells expressing these signaling molecules, including T cells and keratinocytes. Platelet Factor 3 62-73 Janus kinase 1 Homo sapiens 45-49 31972249-2 2020 The tyrosine kinase 2 (TYK2)/Janus kinase 1 (JAK1) inhibitor, PF-06700841, will directly suppress TYK2-dependent IL-12 and IL-23 signaling and JAK1-dependent signaling in cells expressing these signaling molecules, including T cells and keratinocytes. Platelet Factor 3 62-73 Janus kinase 1 Homo sapiens 143-147 31972249-9 2020 PF-06700841 improves clinical symptoms of chronic plaque psoriasis by inhibition of pro-inflammatory cytokines that require TYK2 and JAK1 for signal transduction. Platelet Factor 3 0-11 Janus kinase 1 Homo sapiens 133-137 32428222-2 2020 In this study, we found that occupationally relevant level of Pb exposure impaired ILC development at the progenitor level by activating Janus Kinase1 (JAK1). Lead 62-64 Janus kinase 1 Homo sapiens 137-150 32758351-6 2020 Chemical inhibition of JAK1 in COV434 cells with 100nM ruxolitinib for 72h resulted in significant increases in STAT3 mRNA (P=0.034) and p-Y701-STAT1 protein (P=0.0117), demonstrating a role for JAK1 in modulating STAT in granulosa cells. ruxolitinib 55-66 Janus kinase 1 Homo sapiens 23-27 32758351-6 2020 Chemical inhibition of JAK1 in COV434 cells with 100nM ruxolitinib for 72h resulted in significant increases in STAT3 mRNA (P=0.034) and p-Y701-STAT1 protein (P=0.0117), demonstrating a role for JAK1 in modulating STAT in granulosa cells. ruxolitinib 55-66 Janus kinase 1 Homo sapiens 195-199 32428222-8 2020 In vitro assays suggested that the obstruction of ILCP differentiation by Pb exposure was due to increased activation of JAK1. Lead 74-76 Janus kinase 1 Homo sapiens 121-125 32297800-1 2020 Over the last decade, the Janus kinase1/2 (JAK1/2) inhibitor ruxolitinib has emerged as a cornerstone of myelofibrosis (MF) management. ruxolitinib 61-72 Janus kinase 1 Homo sapiens 43-49 32724162-8 2020 Afterward, IL-6-JAK1-STAT3 signaling was demonstrated to promote SOX9 expression and invasion following ATP treatment. Adenosine Triphosphate 104-107 Janus kinase 1 Homo sapiens 16-20 32428222-2 2020 In this study, we found that occupationally relevant level of Pb exposure impaired ILC development at the progenitor level by activating Janus Kinase1 (JAK1). Lead 62-64 Janus kinase 1 Homo sapiens 152-156 32732872-9 2020 Administration of the JAK1 inhibitor, baricitinib, caused the activation of signal transducer and activator of transcription 3 (STAT3) and revealed an effect similar to that of circ9119 silencing on cell proliferation and apoptosis. baricitinib 38-49 Janus kinase 1 Homo sapiens 22-26 32732872-10 2020 These results showed that circ9119 could modulate apoptosis, and broadly, cell proliferation by competitively binding miR-26a, which targeted JAK1-STAT3, in HCC cell lines. circ9119 26-34 Janus kinase 1 Homo sapiens 142-146 32278762-8 2020 RESULTS: Curcumol reduced the expression of phosphorylated signal transducer and activator of transcription 3 (p-STAT3) via JAK1, JAK2, and Src pathways and inhibited hypoxia-inducible factor-1alpha (HIF-1alpha) protein synthesis via mTOR/p70S6K/eIF4E and MAPK pathways. curcumol 9-17 Janus kinase 1 Homo sapiens 124-128 32732367-4 2021 This prospective study aimed to investigate the efficacy and safety of ruxolitinib, a Janus kinase (JAK) 1/2 inhibitor, as a front-line therapy in children with secondary HLH. ruxolitinib 71-82 Janus kinase 1 Homo sapiens 86-108 32698510-13 2020 Ruxolitinib suppressed the phosphorylation of JAK1, JAK2 and JAK3, and STAT1 and 3 compared to IFN-gamma pretreated hDPCs. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 46-50 32614965-7 2020 Inhibition of JAK/STAT signaling using the selective JAK1/2 inhibitor ruxolitinib resulted in significant antileukemic activity in AML in vitro which is mediated through both cell-autonomous and microenvironment-mediated mechanisms. ruxolitinib 70-81 Janus kinase 1 Homo sapiens 53-59 32462873-0 2020 Fragment-based discovery of pyrazolopyridones as JAK1 inhibitors with excellent subtype selectivity. pyrazolopyridones 28-45 Janus kinase 1 Homo sapiens 49-53 32647892-12 2021 Notably, we demonstrate that CD28null T cell expansion was significantly inhibited by Tofacitinib, a selective JAK1/JAK3 inhibitor that blocks IL-7/IL-15 signalling. tofacitinib 86-97 Janus kinase 1 Homo sapiens 111-115 32446385-10 2020 In addition, we confirmed the suppression of phosphorylated EGFR, JAK1, and Stat3 expression in erlotinib and CJ14939-treated human NSCLC cell lines. cj14939 110-117 Janus kinase 1 Homo sapiens 66-70 32452344-1 2020 OBJECTIVES: This study evaluated the efficacy and safety of baricitinib, an oral Janus kinase (JAK)1/JAK2 inhibitor, in patients with moderately to severely active rheumatoid arthritis (RA) and inadequate response to methotrexate (MTX) therapy. baricitinib 60-71 Janus kinase 1 Homo sapiens 81-100 32446385-6 2020 To overcome resistance to EGFR TKI, we discovered a JAK1 inhibitor, CJ14939. cj14939 68-75 Janus kinase 1 Homo sapiens 52-56 32417942-3 2020 JAK 1/2 inhibitors, such as ruxolitinib and fedratinib, are the mainstay of therapy and produce significant and durable reductions in spleen volume. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 0-7 32417942-3 2020 JAK 1/2 inhibitors, such as ruxolitinib and fedratinib, are the mainstay of therapy and produce significant and durable reductions in spleen volume. Fedratinib 44-54 Janus kinase 1 Homo sapiens 0-7 32923146-3 2020 Therapy with Ruxolitinib (RUX), a JAK1/2 inhibitor, may further increase the infectious risk. ruxolitinib 13-24 Janus kinase 1 Homo sapiens 34-40 32923146-3 2020 Therapy with Ruxolitinib (RUX), a JAK1/2 inhibitor, may further increase the infectious risk. ruxolitinib 26-29 Janus kinase 1 Homo sapiens 34-40 32446385-10 2020 In addition, we confirmed the suppression of phosphorylated EGFR, JAK1, and Stat3 expression in erlotinib and CJ14939-treated human NSCLC cell lines. Erlotinib Hydrochloride 96-105 Janus kinase 1 Homo sapiens 66-70 32334196-3 2020 A cellular selectivity study further confirmed that 11i preferentially inhibits JAK3 over JAK1, in JAK/STAT signaling pathway. 11i 52-55 Janus kinase 1 Homo sapiens 90-94 32560455-8 2020 Next, we tested IL89"s sensitivity to the JAK inhibitor ruxolitinib and observed a potent anti-tumor effect, both in vitro and in vivo. ruxolitinib 56-67 Janus kinase 1 Homo sapiens 42-45 32606953-12 2020 Tofacitinib (JAK1 inhibitor) reversed the tumor-promoting effect of LINC00346 overexpression on CRC cells. tofacitinib 0-11 Janus kinase 1 Homo sapiens 13-17 32017044-1 2020 Ruxolitinib is a potent Janus kinase (JAK) 1/JAK2 inhibitor approved for the treatment of myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 24-44 32295912-6 2020 It blocked STAT1 tyrosine phosphorylation induced either by type I IFN or over-expressed Jak1, paralleling MARV VP40. Tyrosine 17-25 Janus kinase 1 Homo sapiens 89-93 33613945-1 2021 Tofacitinib is an oral, Janus kinase (JAK) molecule, which selectively inhibits Janus-associated tyrosine kinases JAK1 and JAK3. tofacitinib 0-11 Janus kinase 1 Homo sapiens 114-118 32208940-3 2020 Baricitinib is an orally available selective JAK1/JAK2 inhibitor that is approved for use in the treatment of moderate-to-severe rheumatoid arthritis (RA). baricitinib 0-11 Janus kinase 1 Homo sapiens 45-49 32092309-1 2020 BACKGROUND & AIMS: We evaluated the efficacy and safety of upadacitinib, an oral selective inhibitor of Janus kinase 1, as induction therapy for ulcerative colitis (UC). upadacitinib 59-71 Janus kinase 1 Homo sapiens 104-118 32301699-1 2020 OBJECTIVES: We assessed the relative efficacy and safety of once-daily administration of 100 and 200 mg filgotinib (a JAK1-selective inhibitor) in patients with active rheumatoid arthritis (RA). GLPG0634 104-114 Janus kinase 1 Homo sapiens 118-122 31867699-1 2020 Upadacitinib is a Janus kinase 1 inhibitor developed for treatment of moderate to severe rheumatoid arthritis (RA) and was recently approved by the US Food and Drug Administration for this indication in adults who have had an inadequate response or intolerance to methotrexate. upadacitinib 0-12 Janus kinase 1 Homo sapiens 18-32 31286322-2 2020 We hypothesized that selective inhibition of JAK1/2 by ruxolitinib could induce autophagy and limit drug efficacy in myeloproliferative neoplasms (MPN). ruxolitinib 55-66 Janus kinase 1 Homo sapiens 45-49 32125282-5 2020 By MSRE-qPCR, multiple genes of the IL-12-IFN-gamma signaling pathway (IL12B, IL12RB2, TYK2, IFNGR1, JAK1 and JAK2) were hyper-methylated in TB patients. Terbium 141-143 Janus kinase 1 Homo sapiens 101-105 32320566-2 2020 In a phase 2 trial, ruxolitinib, a selective Janus kinase (JAK1 and JAK2) inhibitor, showed potential efficacy in patients with glucocorticoid-refractory acute GVHD. ruxolitinib 20-31 Janus kinase 1 Homo sapiens 59-63 32022397-0 2020 Comparative QSAR model generation using Pyrazole derivatives for screening Janus Kinase-1 inhibitors. Pyrazoles 40-48 Janus kinase 1 Homo sapiens 75-89 32022397-5 2020 In the present study,three dimensional QSAR analyses on a set of pyrazole derivatives against JAK1 and JAK2 enzymes inhibition had been executed. Pyrazoles 65-73 Janus kinase 1 Homo sapiens 94-98 32022397-6 2020 Molecular docking studies were conducted with the target JAK1 using the pyrazole derivative compounds and found out potential intermolecular interactions operating among them. Pyrazoles 72-80 Janus kinase 1 Homo sapiens 57-61 31575356-2 2020 Three publications reported success with ruxolitinib, a Janus-associated kinase (JAK1/2) inhibitor. ruxolitinib 41-52 Janus kinase 1 Homo sapiens 81-87 31978425-8 2020 Finally, we show that the effects of nobiletin are mediated through the JAK1/STAT3 pathway, as nobiletin significantly reduced the phosphorylation of both JAK1 and STAT3. nobiletin 37-46 Janus kinase 1 Homo sapiens 72-76 31978425-8 2020 Finally, we show that the effects of nobiletin are mediated through the JAK1/STAT3 pathway, as nobiletin significantly reduced the phosphorylation of both JAK1 and STAT3. nobiletin 37-46 Janus kinase 1 Homo sapiens 155-159 31978425-8 2020 Finally, we show that the effects of nobiletin are mediated through the JAK1/STAT3 pathway, as nobiletin significantly reduced the phosphorylation of both JAK1 and STAT3. nobiletin 95-104 Janus kinase 1 Homo sapiens 72-76 31978425-8 2020 Finally, we show that the effects of nobiletin are mediated through the JAK1/STAT3 pathway, as nobiletin significantly reduced the phosphorylation of both JAK1 and STAT3. nobiletin 95-104 Janus kinase 1 Homo sapiens 155-159 32297743-6 2020 Herein, an account of the medicinal chemistry optimization from the promiscuous kinase screening hit 3 to the candidate drug 21 (AZD4205), a highly selective JAK1 kinase inhibitor, is reported. golidocitinib 129-136 Janus kinase 1 Homo sapiens 158-162 32064884-0 2020 MiR-769-5p inhibits cancer progression in oral squamous cell carcinoma by directly targeting JAK1/STAT3 pathway. ABT-769 0-10 Janus kinase 1 Homo sapiens 93-97 32293938-5 2020 Ruxolitinib phosphate is a Janus Kinase 1 and 2 (JAK1, JAK2) inhibitor which inhibits pro-inflammatory signaling, and modulates T-cell subsets to an anti-inflammatory phenotype. Ruxolitinib phosphate 0-21 Janus kinase 1 Homo sapiens 49-53 32276266-0 2020 Inhibition of esophageal-carcinoma cell proliferation by genistein via suppression of JAK1/2-STAT3 and AKT/MDM2/p53 signaling pathways. Genistein 57-66 Janus kinase 1 Homo sapiens 86-92 32113874-6 2020 Simultaneously, panaxadiol inhibited STAT3 activation through the JAK1, JAK2, and Src pathways. panaxadiol 16-26 Janus kinase 1 Homo sapiens 66-70 32324888-0 2020 A phase 1 trial of itacitinib, a selective JAK1 inhibitor, in patients with acute graft-versus-host disease. INCB039110 19-29 Janus kinase 1 Homo sapiens 43-47 32324888-2 2020 Itacitinib is a Janus kinase (JAK)1-selective inhibitor that has demonstrated efficacy in preclinical models of aGVHD. INCB039110 0-10 Janus kinase 1 Homo sapiens 30-35 32346301-1 2020 Background: Baricitinib is a janus kinase (JAK1/JAK2) inhibitor developed for the treatment of patients suffering from rheumatoid arthritis (RA). baricitinib 12-23 Janus kinase 1 Homo sapiens 43-47 32122740-4 2020 The results of enzymatic activity assays supported compound 16m-(R) as a potential and selective JAK2 inhibitor, which exhibited high inhibitory activity with an IC50 of 3 nM against JAK2, and 85- and 76-fold selectivity over JAK1 and JAK3, respectively. r) 65-67 Janus kinase 1 Homo sapiens 226-230 32276266-10 2020 Taken together, genistein suppressed the JAK1/2-STAT3 and AKT/MDM2/p53 signaling pathways by decreasing EGFR expression, leading to cell apoptosis, cell cycle arrest, and proliferation inhibition in EsC cells. Genistein 16-25 Janus kinase 1 Homo sapiens 41-47 32276266-7 2020 Additionally, genistein dramatically decreased epidermal growth factor receptor (EGFR) expression and attenuated its down-stream signaling molecules STAT3, MDM2, Akt and JAK1/2 phosphorylation, resulting in inhibited nuclear translocation of STAT3 and MDM2, thereby inhibiting the JAK1/2-STAT3 and AKT/MDM2/p53 signaling pathways. Genistein 14-23 Janus kinase 1 Homo sapiens 170-176 32276266-7 2020 Additionally, genistein dramatically decreased epidermal growth factor receptor (EGFR) expression and attenuated its down-stream signaling molecules STAT3, MDM2, Akt and JAK1/2 phosphorylation, resulting in inhibited nuclear translocation of STAT3 and MDM2, thereby inhibiting the JAK1/2-STAT3 and AKT/MDM2/p53 signaling pathways. Genistein 14-23 Janus kinase 1 Homo sapiens 281-287 31880950-2 2020 We sought to evaluate safety and efficacy of the JAK1/2 inhibitor ruxolitinib in patients with CNL and aCML, irrespective of CSF3R mutation status. ruxolitinib 66-77 Janus kinase 1 Homo sapiens 49-55 31605536-2 2020 Interferon-gamma signaling mediated by Janus kinase (JAK) has been implicated in the pathogenesis of vitiligo.1 Systemic administration of tofacitinib, a potent JAK1/3 inhibitor, has been effective in treating vitiligo in case reports,2 however, it is associated with infections, malignancies, cytopenias, gastrointestinal perforations, and hyperlipidemia in some patients with rheumatoid arthritis. tofacitinib 139-150 Janus kinase 1 Homo sapiens 161-167 31992541-9 2020 Patient-derived organoids (PDOs) obtained from tumors with high AXL and JAK1 were sensitive to TP-0903 and ruxolitinib (JAK inhibitor) treatments supporting the CyTOF findings. ceftaroline fosamil 95-102 Janus kinase 1 Homo sapiens 72-76 31992541-9 2020 Patient-derived organoids (PDOs) obtained from tumors with high AXL and JAK1 were sensitive to TP-0903 and ruxolitinib (JAK inhibitor) treatments supporting the CyTOF findings. ruxolitinib 107-118 Janus kinase 1 Homo sapiens 72-76 32196928-0 2020 The JAK1/2 inhibitor ruxolitinib delays premature aging phenotypes. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 32196928-5 2020 Here, we show that JAK1/2 inhibition with ruxolitinib rescues progerin-induced cell cycle arrest, cellular senescence, and misshapen nuclei in human normal fibroblasts expressing progerin. ruxolitinib 42-53 Janus kinase 1 Homo sapiens 19-23 32034662-3 2020 Other currently available therapies include pegylated interferon alfa-2a and the JAK1/2 inhibitor ruxolitinib. ruxolitinib 98-109 Janus kinase 1 Homo sapiens 81-87 32166597-3 2020 Delgocitinib inhibits all members of the JAK family [JAK1, JAK2, JAK3 and tyrosine kinase 2]. delgocitinib 0-12 Janus kinase 1 Homo sapiens 53-57 32153201-1 2020 Introduction: Ruxolitinib is an oral selective JAK1/JAK2 inhibitor, initially approved by the FDA for the treatment of intermediate-2 or high-risk myelofibrosis and patients with polycythemia vera who have had an inadequate response or are intolerant to hydroxyurea.Areas Covered: Accumulating evidence supports the role of JAK1/JAK2 pathways in the pathogenesis of graft-versus-host disease (GVHD), and preclinical studies have demonstrated promising efficacy of ruxolitinib in treatment/prevention of GVHD. ruxolitinib 14-25 Janus kinase 1 Homo sapiens 47-51 32153201-1 2020 Introduction: Ruxolitinib is an oral selective JAK1/JAK2 inhibitor, initially approved by the FDA for the treatment of intermediate-2 or high-risk myelofibrosis and patients with polycythemia vera who have had an inadequate response or are intolerant to hydroxyurea.Areas Covered: Accumulating evidence supports the role of JAK1/JAK2 pathways in the pathogenesis of graft-versus-host disease (GVHD), and preclinical studies have demonstrated promising efficacy of ruxolitinib in treatment/prevention of GVHD. ruxolitinib 14-25 Janus kinase 1 Homo sapiens 324-328 32153201-3 2020 Based on the data from the REACH1 trial, ruxolitinib was approved by the FDA in May 2019 for SR acute GVHD in adult and pediatric patients 12 years and older.Expert Opinion: Ruxolitinib and other JAK1/JAK2 inhibitors hold promise in other treatment settings such as GVHD prevention and/or first line therapy. ruxolitinib 41-52 Janus kinase 1 Homo sapiens 196-200 31701537-1 2020 Upadacitinib (ABT-494) is a selective Janus kinase (JAK)1 inhibitor being developed for treatment of several inflammatory disorders. upadacitinib 0-12 Janus kinase 1 Homo sapiens 52-57 31701537-1 2020 Upadacitinib (ABT-494) is a selective Janus kinase (JAK)1 inhibitor being developed for treatment of several inflammatory disorders. AG 494 14-21 Janus kinase 1 Homo sapiens 52-57 32201152-4 2021 The only and curative option for PMF is allogeneic hematopoietic stem cell transplant (allo-HSCT); however, the Janus kinase (JAK) 1/2 inhibitor ruxolitinib is highly effective in reducing constitutional symptoms and spleen volume, and has been found to improve survival. ruxolitinib 145-156 Janus kinase 1 Homo sapiens 112-132 32609446-2 2020 Tofacitinib, an oral JAK 1/3 inhibitor approved for the treatment of rheumatoid arthritis, has previously been shown to induce significant re-pigmentation in vitiligo. tofacitinib 0-11 Janus kinase 1 Homo sapiens 21-28 32019673-9 2020 Taken together, these findings identified a novel signaling axis, CYP1A1-15(S)-HETE-JAK1-STAT6, that may be a promising target for the proper maintenance of macrophage polarization and may also be a means by which to treat immune-related disease due to macrophage dysfunction. 15-hydroxy-5,8,11,13-eicosatetraenoic acid 73-83 Janus kinase 1 Homo sapiens 84-88 32011040-10 2020 Besides, ICA notably frustrated JAK1/STAT3 and PI3K/AKT activations in DAOY cells. icariin 9-12 Janus kinase 1 Homo sapiens 32-36 31711337-1 2020 Ruxolitinib is a JAK1/2 inhibitor approved for the treatment of myelofibrosis (MF) and polycythemia vera (PV). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-23 31970549-3 2020 As a selective inhibitor of JAK1 and JAK3, tofacitinib has the potential to play a role in the management of rheumatic diseases such as RA and PsA. tofacitinib 43-54 Janus kinase 1 Homo sapiens 28-32 31970549-6 2020 In this review, the authors summarize current knowledge on the relationship between the immune system and the skeleton before examining the involvement of JAK-STAT signaling in bone homeostasis as well as the available preclinical and clinical evidence on the benefits of tofacitinib on prevention of bone involvement in RA and PsA.Key Points Chronic inflammation in rheumatoid arthritis (RA) and psoriatic arthritis (PsA) leads to disturbances in bone remodeling Bone remodeling is mediated by several signaling pathways, including the JAK-STAT pathway Tofacitinib, a selective inhibitor of JAK1 and JAK3, is active in RA and PsA and may help limit systemic bone loss through inhibiting disturbed osteoclastogenesis Clinical trials show that tofacitinib reduces articular bone erosion. tofacitinib 272-283 Janus kinase 1 Homo sapiens 595-599 32020553-8 2020 Brepocitinib, a potent TYK2/JAK1 inhibitor, is also being evaluated, as both oral and topical treatment. Brepocitinib 0-12 Janus kinase 1 Homo sapiens 28-32 31786154-2 2020 OBJECTIVE: This study evaluated the safety and efficacy of multiple doses of the selective Janus kinase 1 inhibitor upadacitinib in patients with moderate-to-severe atopic dermatitis. upadacitinib 116-128 Janus kinase 1 Homo sapiens 91-105 32022429-6 2020 Pre-treatment with ruxolitinib, a selective Janus kinase (JAK) 1/2 inhibitor, prevented the LPS-induced Stat3 phosphorylation and restored the sensitivity of hepatocytes to Fas-mediated apoptosis. ruxolitinib 19-30 Janus kinase 1 Homo sapiens 44-66 31982039-2 2020 Ruxolitinib, a JAK 1 and JAK 2 inhibitor, showed superiority over best available therapy in a phase 2 study in patients with polycythaemia vera who were resistant to or intolerant of hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-20 32011040-12 2020 The results concluded that ICA exhibited the antitumor activity in DAOY cells via decreasing SPARC and inactivating JAK1/STAT3 and PI3K/AKT pathways. icariin 27-30 Janus kinase 1 Homo sapiens 116-120 32258058-7 2020 We report a positive clinical response in LPP to tofacitinib, a JAK1/3 inhibitor, and dapsone, an anti-neutrophilic agent. tofacitinib 49-60 Janus kinase 1 Homo sapiens 64-70 31912462-0 2020 Filgotinib, a JAK1 Inhibitor, Modulates Disease-Related Biomarkers in Rheumatoid Arthritis: Results from Two Randomized, Controlled Phase 2b Trials. GLPG0634 0-10 Janus kinase 1 Homo sapiens 14-18 31912462-2 2020 We sought to gain insight into the mode of action and immunological effects of filgotinib, a JAK1 selective inhibitor, in active RA by analyzing secreted and cell-based biomarkers key to RA pathophysiology in two phase 2b trials of filgotinib in active RA. GLPG0634 79-89 Janus kinase 1 Homo sapiens 93-97 31697835-3 2020 Both receptors could be expressed in human T lymphocytes; Epo ligation induced STAT5 phosphorylation, which was abrogated by nontoxic concentrations of the JAK1/2 inhibitor ruxolitinib. ruxolitinib 173-184 Janus kinase 1 Homo sapiens 156-162 31448433-8 2020 This study confirms that in humans, upadacitinib has greater selectivity for JAK1 vs JAK3 relative to the rheumatoid arthritis approved dose of tofacitinib, and results from these analyses informed the selection of upadacitinib IR doses evaluated in phase 2. upadacitinib 36-48 Janus kinase 1 Homo sapiens 77-81 32054011-0 2020 Discovery of 9O-Substituted Palmatine Derivatives as a New Class of anti-COL1A1 Agents via Repressing TGF-beta1/Smads and JAK1/STAT3 Pathways. palmatine 13-37 Janus kinase 1 Homo sapiens 122-126 31629805-0 2020 Treatment of Atopic Dermatitis With Ruxolitinib Cream (JAK1/JAK2 Inhibitor) or Triamcinolone Cream. ruxolitinib 36-47 Janus kinase 1 Homo sapiens 55-59 31629805-2 2020 Ruxolitinib, a selective inhibitor of Janus kinase (JAK)-1 and JAK2, potently suppresses cytokine signaling involved in AD pathogenesis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-58 31833760-1 2020 Tofacitinib is an orally administered medication with a mechanism of action that involves JAK1, JAK2, JAK3 and TYK2 pathway inhibition. tofacitinib 0-11 Janus kinase 1 Homo sapiens 90-94 31782014-2 2020 Baricitinib is a synthetic small molecule which targets the JAK/STAT pathway which is implicated in the inflammatory response in RA. baricitinib 0-11 Janus kinase 1 Homo sapiens 60-63 31782014-3 2020 Baricitinib selectively targets JAK1 and JAK2 and has been shown to have efficacy in treating patients with RA. baricitinib 0-11 Janus kinase 1 Homo sapiens 32-36 32096183-0 2020 MiR-30c-5p inhibits high glucose-induced EMT and renal fibrogenesis by down-regulation of JAK1 in diabetic nephropathy. mir-30c-5p 0-10 Janus kinase 1 Homo sapiens 90-94 32096183-0 2020 MiR-30c-5p inhibits high glucose-induced EMT and renal fibrogenesis by down-regulation of JAK1 in diabetic nephropathy. Glucose 25-32 Janus kinase 1 Homo sapiens 90-94 32096183-12 2020 Furthermore, overexpression of JAK1 attenuated the inhibitory effect of miR-30c-5p on HG-induced EMT and renal fibrogenesis in HK2 cells. mir-30c-5p 72-82 Janus kinase 1 Homo sapiens 31-35 31448433-1 2020 Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being developed for treatment of rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-48 31448433-2 2020 This study characterizes the relationships between upadacitinib exposure and interleukin (IL)-6-induced signal transducer and activator of transcription proteins 3 (STAT3) phosphorylation (pSTAT3) and IL-7-induced STAT5 phosphorylation (pSTAT5) in the ex vivo setting as measures for JAK1 and JAK1/JAK3 inhibition, respectively, with comparison to tofacitinib. upadacitinib 51-63 Janus kinase 1 Homo sapiens 284-288 31448433-2 2020 This study characterizes the relationships between upadacitinib exposure and interleukin (IL)-6-induced signal transducer and activator of transcription proteins 3 (STAT3) phosphorylation (pSTAT3) and IL-7-induced STAT5 phosphorylation (pSTAT5) in the ex vivo setting as measures for JAK1 and JAK1/JAK3 inhibition, respectively, with comparison to tofacitinib. upadacitinib 51-63 Janus kinase 1 Homo sapiens 293-297 30725185-1 2020 OBJECTIVES: We assessed the relative efficacy and safety of once-daily administration of 15 and 30 mg upadacitinib (a JAK1-selective inhibitor) in patients with active rheumatoid arthritis (RA). upadacitinib 102-114 Janus kinase 1 Homo sapiens 118-122 32099414-3 2020 Baricitinib is an oral JAK inhibitor highly selective for JAK1 and JAK2. baricitinib 0-11 Janus kinase 1 Homo sapiens 58-62 31423579-0 2020 JAK1/2 pathway inhibition suppresses M2 polarization and overcomes resistance of myeloma to lenalidomide by reducing TRIB1, MUC1, CD44, CXCL12, and CXCR4 expression. Lenalidomide 92-104 Janus kinase 1 Homo sapiens 0-6 31831383-0 2020 Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34. pyrazolo(1,5-a)pyrimidine 45-71 Janus kinase 1 Homo sapiens 111-115 31956784-3 2020 In the present study, the susceptibility of the oral JAK inhibitor tofacitinib against these three JAKs was elucidated using the 500-ns molecular dynamics (MD) simulations and free energy calculations based on MM-PB(GB)SA, QM/MM-GBSA (PM3 and SCC-DFTB), and SIE methods. tofacitinib 67-78 Janus kinase 1 Homo sapiens 99-103 31956784-4 2020 The obtained results revealed that tofacitinib could interact with all JAKs at the ATP-binding site via electrostatic attraction, hydrogen bond formation, and in particular van der Waals interaction. tofacitinib 35-46 Janus kinase 1 Homo sapiens 71-75 31956784-4 2020 The obtained results revealed that tofacitinib could interact with all JAKs at the ATP-binding site via electrostatic attraction, hydrogen bond formation, and in particular van der Waals interaction. Adenosine Triphosphate 83-86 Janus kinase 1 Homo sapiens 71-75 31956784-5 2020 The conserved glutamate and leucine residues (E957 and L959 of JAK1, E930 and L932 of JAK2, and E903 and L905 of JAK3) located in the hinge region stabilized tofacitinib binding through strongly formed hydrogen bonds. Glutamic Acid 14-23 Janus kinase 1 Homo sapiens 63-67 31956784-5 2020 The conserved glutamate and leucine residues (E957 and L959 of JAK1, E930 and L932 of JAK2, and E903 and L905 of JAK3) located in the hinge region stabilized tofacitinib binding through strongly formed hydrogen bonds. Leucine 28-35 Janus kinase 1 Homo sapiens 63-67 31956784-5 2020 The conserved glutamate and leucine residues (E957 and L959 of JAK1, E930 and L932 of JAK2, and E903 and L905 of JAK3) located in the hinge region stabilized tofacitinib binding through strongly formed hydrogen bonds. tofacitinib 158-169 Janus kinase 1 Homo sapiens 63-67 31956784-5 2020 The conserved glutamate and leucine residues (E957 and L959 of JAK1, E930 and L932 of JAK2, and E903 and L905 of JAK3) located in the hinge region stabilized tofacitinib binding through strongly formed hydrogen bonds. Hydrogen 202-210 Janus kinase 1 Homo sapiens 63-67 31956784-7 2020 The binding affinities of tofacitinib/JAKs were ranked in the order of JAK3 > JAK2 ~ JAK1, which are in line with the reported experimental data. tofacitinib 26-37 Janus kinase 1 Homo sapiens 38-42 31956784-7 2020 The binding affinities of tofacitinib/JAKs were ranked in the order of JAK3 > JAK2 ~ JAK1, which are in line with the reported experimental data. tofacitinib 26-37 Janus kinase 1 Homo sapiens 85-89 31819176-0 2020 Serotonin activates glycolysis and mitochondria biogenesis in human breast cancer cells through activation of the Jak1/STAT3/ERK1/2 and adenylate cyclase/PKA, respectively. Serotonin 0-9 Janus kinase 1 Homo sapiens 114-118 31534088-3 2020 We describe the case of a patient with MF-associated PH who developed left ventricular dysfunction after five years of treatment with the JAK 1/2 inhibitor, ruxolitinib. ruxolitinib 157-168 Janus kinase 1 Homo sapiens 138-145 32067619-1 2020 BACKGROUND: Ruxolitinib is a selective JAK1/2 inhibitor approved by FDA for myelofibrosis in 2014 and nowadays, comprehensive investigations on the potential of the agent as a targeted therapy for haematological malignancies are on the rise. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 39-45 30962501-1 2020 Ruxolitinib (Rux), a Jak1/2 inhibitor, results in reduced spleen size and improvement in constitutional symptoms in the majority of patients with myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-27 30962501-1 2020 Ruxolitinib (Rux), a Jak1/2 inhibitor, results in reduced spleen size and improvement in constitutional symptoms in the majority of patients with myelofibrosis (MF). ruxolitinib 0-3 Janus kinase 1 Homo sapiens 21-27 31819176-5 2020 We also showed that increased glucose metabolism is provoked by the upregulation of pyruvate kinase M2 (PKM2) isoform through 5-HTR2A/C-triggered activation of Jak1/STAT3 and ERK1/2 subcellular pathways. Glucose 30-37 Janus kinase 1 Homo sapiens 160-164 31423579-5 2020 Ruxolitinib (RUX) is an inhibitor of the Janus kinase family of protein tyrosine kinases (JAKs) and is effective for treating patients with myeloproliferative disorders. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 90-94 31819176-8 2020 CONCLUSIONS: We showed that serotonin, through 5-HTR2A/C, interferes with breast cancer cells proliferation and metabolism by triggering two distinct signalling pathways: Jak1/STAT3 that boosts glycolysis through upregulation of PKM2, and adenylyl cyclase/PKA that enhances mitochondrial biogenesis. Serotonin 28-37 Janus kinase 1 Homo sapiens 171-175 31423579-5 2020 Ruxolitinib (RUX) is an inhibitor of the Janus kinase family of protein tyrosine kinases (JAKs) and is effective for treating patients with myeloproliferative disorders. ruxolitinib 13-16 Janus kinase 1 Homo sapiens 90-94 31797578-1 2020 Filgotinib, a selective inhibitor of Janus kinase 1, is being developed for the treatment of chronic inflammatory diseases. GLPG0634 0-10 Janus kinase 1 Homo sapiens 37-51 31378969-1 2020 The aim of this study was to characterize the effects of upadacitinib, a Janus kinase 1 inhibitor, on in vivo activity of different cytochrome P450 (CYP) enzymes using a cocktail approach. upadacitinib 57-69 Janus kinase 1 Homo sapiens 73-87 31666386-4 2020 Based on these results she was treated with the JAK1/2 inhibitor ruxolitinib, which resulted in reduction in IFN signalling and appeared to be associated with partial though incomplete decrease in the severity of her pulmonary disease. ruxolitinib 65-76 Janus kinase 1 Homo sapiens 48-54 31778911-1 2020 Ruxolitinib, a selective JAK1/JAK2 inhibitor, is the current first line therapy for myelofibrosis (MF), which reduces symptomatology and splenomegaly, but does not clearly modify disease course. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 25-29 30784354-1 2020 OBJECTIVES: Baricitinib is a selective oral inhibitor of JAK1/JAK2 for patients with moderately-to-severely active rheumatoid arthritis (RA). baricitinib 12-23 Janus kinase 1 Homo sapiens 57-61 31654094-0 2020 Potent repression of C-reactive protein (CRP) expression by the JAK1/2 inhibitor ruxolitinib in inflammatory human hepatocytes. ruxolitinib 81-92 Janus kinase 1 Homo sapiens 64-70 31821455-0 2019 Resolution of secondary hemophagocytic lymphohistiocytosis after treatment with the JAK1/2 inhibitor ruxolitinib. ruxolitinib 101-112 Janus kinase 1 Homo sapiens 84-90 31892268-8 2019 In interleukin-2 (IL-2)-induced STAT5 activation JAK1 was dominant over JAK3 but in interferon-gamma (IFNgamma) and interferon-alpha (IFNalpha) signaling both JAK1 and heteromeric partner JAK2 or TYK2 were both indispensable for STAT1 activation. Interferon-alpha 116-132 Janus kinase 1 Homo sapiens 159-163 31892268-10 2019 To investigate the regulatory function, we focused on two allosteric regions in JAK1 JH2, the ATP-binding pocket and the alphaC-helix. Adenosine Triphosphate 94-97 Janus kinase 1 Homo sapiens 80-84 31920387-2 2019 In late 2019, the FDA approved the highly selective JAK2 inhibitor, fedratinib, for intermediate-2 or high-risk primary or secondary MF, making it the second drug approved for MF after ruxolitinib, a JAK1/2 inhibitor, which was approved for MF in 2011. Fedratinib 68-78 Janus kinase 1 Homo sapiens 200-206 32015973-6 2020 LEARNING POINTS: Baricitinib is a small, orally active molecule that inhibits JAK-1 and JAK-2, which is used in the treatment of rheumatoid arthritis.Baricitinib has been also used in the treatment of psoriasis, alopecia areata and atopic dermatitis.Palmoplantar pustulosis is a rare cutaneous side effect of baricitinib. baricitinib 17-28 Janus kinase 1 Homo sapiens 78-83 32015973-6 2020 LEARNING POINTS: Baricitinib is a small, orally active molecule that inhibits JAK-1 and JAK-2, which is used in the treatment of rheumatoid arthritis.Baricitinib has been also used in the treatment of psoriasis, alopecia areata and atopic dermatitis.Palmoplantar pustulosis is a rare cutaneous side effect of baricitinib. baricitinib 150-161 Janus kinase 1 Homo sapiens 78-83 32015973-6 2020 LEARNING POINTS: Baricitinib is a small, orally active molecule that inhibits JAK-1 and JAK-2, which is used in the treatment of rheumatoid arthritis.Baricitinib has been also used in the treatment of psoriasis, alopecia areata and atopic dermatitis.Palmoplantar pustulosis is a rare cutaneous side effect of baricitinib. baricitinib 309-320 Janus kinase 1 Homo sapiens 78-83 31878046-5 2019 Additionally, DDZ mitigated the phosphorylation of STAT3 upstream Janus-activated kinases (JAK1/2) and c-Src kinases. daidzin 14-17 Janus kinase 1 Homo sapiens 91-97 31847229-6 2019 In addition, ACHP imparted inhibitory activity on the constitutive activation of upstream protein tyrosine kinases, including JAK1, JAK2, and Src. 2-amino-6-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-4-piperidin-4-yl nicotinonitrile 13-17 Janus kinase 1 Homo sapiens 126-130 31866997-8 2019 Treatment with Janus kinase 1 and 2 (JAK1/2) inhibitor baricitinib was beneficiary for a vasculitic ulcer, induced hair regrowth and improved overall well-being in one patient. baricitinib 55-66 Janus kinase 1 Homo sapiens 37-43 31732180-2 2019 This study assessed the efficacy and safety of upadacitinib, a selective JAK1 inhibitor, in patients with ankylosing spondylitis. upadacitinib 47-59 Janus kinase 1 Homo sapiens 73-77 30831034-0 2019 Notoginsenoside R1 promotes MC3T3-E1 differentiation by up-regulating miR-23a via MAPK and JAK1/STAT3 pathways. notoginsenoside 0-15 Janus kinase 1 Homo sapiens 91-95 31791386-2 2019 We compared upadacitinib, an oral, selective JAK-1 inhibitor, with placebo to assess clinically meaningful improvements in PROs in patients with RA who have had inadequate responses to biologic disease-modifying antirheumatic drugs (bDMARD-IR). upadacitinib 12-24 Janus kinase 1 Homo sapiens 45-50 31719581-1 2019 Ruxolitinib is an FDA approved janus kinase (JAK)1/2 inhibitor used to treat myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 31-50 31282592-1 2019 Itacitinib is a potent, selective JAK-1 inhibitor currently in phase 3 development for the treatment of acute and chronic graft-versus-host disease (GVHD) in combination with corticosteroids. INCB039110 0-10 Janus kinase 1 Homo sapiens 34-39 31577341-3 2019 Abrocitinib (PF-04965842) is an oral Janus kinase 1 selective inhibitor under investigation for the treatment of atopic dermatitis. Abrocitinib 0-11 Janus kinase 1 Homo sapiens 37-51 31577341-3 2019 Abrocitinib (PF-04965842) is an oral Janus kinase 1 selective inhibitor under investigation for the treatment of atopic dermatitis. Abrocitinib 13-24 Janus kinase 1 Homo sapiens 37-51 31725895-7 2019 Here we report that the recently developed pan-PIM inhibitor INCB053914 augments the efficacy of the US Food and Drug Administration-approved JAK1/2 inhibitor ruxolitinib in both in vitro and in vivo MPN models. INCB3619 61-71 Janus kinase 1 Homo sapiens 142-148 31725895-7 2019 Here we report that the recently developed pan-PIM inhibitor INCB053914 augments the efficacy of the US Food and Drug Administration-approved JAK1/2 inhibitor ruxolitinib in both in vitro and in vivo MPN models. ruxolitinib 159-170 Janus kinase 1 Homo sapiens 142-148 31537486-4 2019 We therefore aimed to determine the activity and safety of ruxolitinib, a JAK inhibitor, in adults with secondary haemophagocytic lymphohistiocytosis. ruxolitinib 59-70 Janus kinase 1 Homo sapiens 74-77 31287230-1 2019 OBJECTIVE: To evaluate the efficacy, including capacity for inhibition of radiographic progression, and safety of upadacitinib, a JAK1-selective inhibitor, as compared to placebo or adalimumab in patients with rheumatoid arthritis (RA) who have experienced an inadequate response to methotrexate (MTX). upadacitinib 114-126 Janus kinase 1 Homo sapiens 130-134 31788449-4 2019 Ruxolitinib is a potent and selective oral inhibitor of both JAK2 and JAK1 protein kinases. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 70-74 31507089-5 2019 We showed that forced miR-206 expression restored gefitinib sensitivity in IL6-induced gefitinib-resistant EGFR-mutant lung cancer cells by inhibiting IL6/JAK1/STAT3 pathway. Gefitinib 50-59 Janus kinase 1 Homo sapiens 155-159 31642025-1 2019 Upadacitinib (Rinvoq ), an orally-administered Janus kinase 1 (JAK-1) inhibitor, is being developed by AbbVie for the treatment of rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 47-61 31642025-1 2019 Upadacitinib (Rinvoq ), an orally-administered Janus kinase 1 (JAK-1) inhibitor, is being developed by AbbVie for the treatment of rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 63-68 31507089-5 2019 We showed that forced miR-206 expression restored gefitinib sensitivity in IL6-induced gefitinib-resistant EGFR-mutant lung cancer cells by inhibiting IL6/JAK1/STAT3 pathway. Gefitinib 87-96 Janus kinase 1 Homo sapiens 155-159 31654328-1 2019 Upadacitinib is a selective Janus Kinase 1 inhibitor which is being developed for the treatment of several inflammatory diseases including rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 31313387-4 2019 MTX has also been shown to exert JAK inhibition of JAK2 and JAK1 when tested in Drosophila melanogaster as a model of kinase activity and in human cell lines (nodular sclerosis Hodgkin"s lymphoma and acute myeloid leukemia cell lines). Methotrexate 0-3 Janus kinase 1 Homo sapiens 60-64 31313387-5 2019 These effects may explain why MTX leads to clinical effects similar to anti-TNFalpha biologics in monotherapy, but is less effective when compared to anti-IL6R in monotherapy, which acting upstream exerts major effects downstream on the JAK1-STAT3 pathway. Methotrexate 30-33 Janus kinase 1 Homo sapiens 237-241 31313387-6 2019 The MTX effects on JAK1/JAK2 inhibition also allows to understand why the combination of MTX with Leflunomide, or JAK1/JAK3 inhibitor leads to better clinical outcomes than monotherapy, while the combination with JAK1/JAK2 or JAK1 specific inhibitors does not seem to exert additive clinical benefit. Methotrexate 4-7 Janus kinase 1 Homo sapiens 19-23 31313387-6 2019 The MTX effects on JAK1/JAK2 inhibition also allows to understand why the combination of MTX with Leflunomide, or JAK1/JAK3 inhibitor leads to better clinical outcomes than monotherapy, while the combination with JAK1/JAK2 or JAK1 specific inhibitors does not seem to exert additive clinical benefit. Methotrexate 4-7 Janus kinase 1 Homo sapiens 114-118 31313387-6 2019 The MTX effects on JAK1/JAK2 inhibition also allows to understand why the combination of MTX with Leflunomide, or JAK1/JAK3 inhibitor leads to better clinical outcomes than monotherapy, while the combination with JAK1/JAK2 or JAK1 specific inhibitors does not seem to exert additive clinical benefit. Methotrexate 4-7 Janus kinase 1 Homo sapiens 114-118 31313387-6 2019 The MTX effects on JAK1/JAK2 inhibition also allows to understand why the combination of MTX with Leflunomide, or JAK1/JAK3 inhibitor leads to better clinical outcomes than monotherapy, while the combination with JAK1/JAK2 or JAK1 specific inhibitors does not seem to exert additive clinical benefit. Methotrexate 4-7 Janus kinase 1 Homo sapiens 114-118 31313387-6 2019 The MTX effects on JAK1/JAK2 inhibition also allows to understand why the combination of MTX with Leflunomide, or JAK1/JAK3 inhibitor leads to better clinical outcomes than monotherapy, while the combination with JAK1/JAK2 or JAK1 specific inhibitors does not seem to exert additive clinical benefit. Methotrexate 89-92 Janus kinase 1 Homo sapiens 19-23 31313387-6 2019 The MTX effects on JAK1/JAK2 inhibition also allows to understand why the combination of MTX with Leflunomide, or JAK1/JAK3 inhibitor leads to better clinical outcomes than monotherapy, while the combination with JAK1/JAK2 or JAK1 specific inhibitors does not seem to exert additive clinical benefit. Leflunomide 98-109 Janus kinase 1 Homo sapiens 19-23 31696160-1 2019 Background: Baricitinib, with a 2-(1-(ethylsulfonyl)azetidin-3-yl)acetonitrile moiety at N-2 position of the pyrazol skeleton, is an oral and selective reversible inhibitor of the JAK1 and JAK2 and displays potent anti-inflammatory activity. baricitinib 12-23 Janus kinase 1 Homo sapiens 180-184 31635416-0 2019 Inhibition of JAK-STAT Signaling with Baricitinib Reduces Inflammation and Improves Cellular Homeostasis in Progeria Cells. baricitinib 38-49 Janus kinase 1 Homo sapiens 14-17 31692920-6 2019 Both these new compounds are active on the majority of four JAK family members (JAK1, JAK2, JAK3, and TYK2), whereas the most recent emerging approach is directed toward the development of JAK1 selective inhibitors (upadacitinib and filgotinib) with the aim to improve the safety profile by minimizing the effects on JAK3 and, especially, JAK2. upadacitinib and filgotinib 216-243 Janus kinase 1 Homo sapiens 189-193 31635416-7 2019 We report that the inhibition of the JAK-STAT pathway with baricitinib, a Food and Drug Administration-approved JAK1/2 inhibitor, restored cellular homeostasis, delayed senescence and decreased proinflammatory markers in HGPS cells. baricitinib 59-70 Janus kinase 1 Homo sapiens 37-40 31635416-7 2019 We report that the inhibition of the JAK-STAT pathway with baricitinib, a Food and Drug Administration-approved JAK1/2 inhibitor, restored cellular homeostasis, delayed senescence and decreased proinflammatory markers in HGPS cells. baricitinib 59-70 Janus kinase 1 Homo sapiens 112-118 31276975-5 2019 The results suggest that celastrol acts against rheumatoid arthritis by regulating the function of several signaling proteins, including MMP-9, COX-2, c-Myc, TGF-beta, c-JUN, JAK-1, JAK-3, IKK-beta, SYK, MMP-3, JNK and MEK1, which regulate the functions of Th1 and Th2 cells, macrophages, fibroblasts and endothelial cells in rheumatoid arthritis. celastrol 25-34 Janus kinase 1 Homo sapiens 175-180 31575007-5 2019 The data from the cell-based experiments suggested that BT-induced cytotoxicity and abrogated the activation of STAT3 and that of upstream kinases such as JAK1, JAK2, and Src. brusatol 56-58 Janus kinase 1 Homo sapiens 155-159 31348981-4 2019 The highest percentage of apoptosis was observed in the treatment of Jak1 siRNA/cisplatin group in cancerous HN5 cells (96.5%) where this treatment showed 12.84% apoptosis in normal HUVEC cell line. Cisplatin 80-89 Janus kinase 1 Homo sapiens 69-73 31554739-6 2019 Last, using drug prediction algorithms, we identify JAK inhibitors as promising therapeutic agents in LP and demonstrate that the JAK1/2 inhibitor baricitinib fully protects keratinocytes against cell-mediated cytotoxic responses in vitro. baricitinib 147-158 Janus kinase 1 Homo sapiens 130-136 31549971-6 2019 Recently, the Janus kinase (JAK) family of tyrosine kinases, including JAK1 and JAK2, has been shown to play a role in the pathogenesis of MM. Tyrosine 43-51 Janus kinase 1 Homo sapiens 71-75 31549971-7 2019 Preclinical studies have demonstrated that the JAK1/2 inhibitor ruxolitinib, in combination with lenalidomide and dexamethasone, reduces proliferation of the MM cell lines and primary tumor cells derived from MM patients, and this inhibition is greater when these drugs are combined than with single agents. ruxolitinib 64-75 Janus kinase 1 Homo sapiens 47-51 31549971-7 2019 Preclinical studies have demonstrated that the JAK1/2 inhibitor ruxolitinib, in combination with lenalidomide and dexamethasone, reduces proliferation of the MM cell lines and primary tumor cells derived from MM patients, and this inhibition is greater when these drugs are combined than with single agents. lenalidomide 97-109 Janus kinase 1 Homo sapiens 47-51 31549971-7 2019 Preclinical studies have demonstrated that the JAK1/2 inhibitor ruxolitinib, in combination with lenalidomide and dexamethasone, reduces proliferation of the MM cell lines and primary tumor cells derived from MM patients, and this inhibition is greater when these drugs are combined than with single agents. Dexamethasone 114-127 Janus kinase 1 Homo sapiens 47-51 30907116-4 2019 Data Synthesis: Baricitinib exerts its effects by inhibiting JAK1 and JAK2 enzymes, targeting cytokine and growth factor receptor stimulation, thus reducing downstream immune cell function. baricitinib 16-27 Janus kinase 1 Homo sapiens 61-65 30671927-5 2019 TAM-derived IL-10 promoted CSC-like properties of NSCLC cells through JAK1/STAT1/NF-kappaB/Notch1 signaling. tam 0-3 Janus kinase 1 Homo sapiens 70-74 30973649-1 2019 Upadacitinib is a selective Janus kinase 1 inhibitor being developed for the treatment of several inflammatory autoimmune diseases, including rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 31401212-6 2019 Emerging data with selective JAK1 inhibitors upadacitinib and filgotinib looks very promising. upadacitinib 45-57 Janus kinase 1 Homo sapiens 29-33 31401212-6 2019 Emerging data with selective JAK1 inhibitors upadacitinib and filgotinib looks very promising. GLPG0634 62-72 Janus kinase 1 Homo sapiens 29-33 31449490-13 2019 In contrast to IL-1 (interleukin-1), IL-6, and TNF (tumor necrosis factor) inhibitors, baricitinib was very successful, probably because baricitinib acts as a JAK-1/2 (janus kinase-1/2) inhibitor in the IFNalpha/beta (inteferone alpha/beta) pathway. baricitinib 87-98 Janus kinase 1 Homo sapiens 159-166 31449490-13 2019 In contrast to IL-1 (interleukin-1), IL-6, and TNF (tumor necrosis factor) inhibitors, baricitinib was very successful, probably because baricitinib acts as a JAK-1/2 (janus kinase-1/2) inhibitor in the IFNalpha/beta (inteferone alpha/beta) pathway. baricitinib 137-148 Janus kinase 1 Homo sapiens 159-166 30671927-6 2019 Blockade of IL-10/JAK1 signaling inhibited TAM-mediated NSCLC tumor growth in vivo, and the TAM-mediated expression of CSC-related and mesenchymal-related genes in NSCLC. tam 43-46 Janus kinase 1 Homo sapiens 18-22 30650179-6 2019 JAK1/2 inhibition via ruxolitinib decreased, while stimulation with LIF increased, phosphorylation of STAT3 and the number of cells with CSC properties indicating that JAK-STAT signalling controlled the number of cells with CSC features. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 0-6 31375130-6 2019 For example, tofacitinib and upadacitinib were the most potent inhibitors of the JAK1/3-dependent cytokines tested (interleukin [IL]-2, IL-4, IL-15, and IL-21) with lower IC50 values and increased time above IC50 translating to a greater overall inhibition of STAT signaling during the dosing interval. tofacitinib 13-24 Janus kinase 1 Homo sapiens 81-85 31375130-6 2019 For example, tofacitinib and upadacitinib were the most potent inhibitors of the JAK1/3-dependent cytokines tested (interleukin [IL]-2, IL-4, IL-15, and IL-21) with lower IC50 values and increased time above IC50 translating to a greater overall inhibition of STAT signaling during the dosing interval. upadacitinib 29-41 Janus kinase 1 Homo sapiens 81-85 31375130-9 2019 Notably, baricitinib inhibited JAK1/3 signaling to a lesser extent than upadacitinib and tofacitinib, while upadacitinib, baricitinib, and tofacitinib inhibited the signaling of JAK2/2-dependent cytokines, including GM-CSF and IL-3, as well as the signaling of the JAK2/TYK2-dependent cytokine G-CSF. baricitinib 9-20 Janus kinase 1 Homo sapiens 31-35 30945116-1 2019 BACKGROUND AND OBJECTIVES: Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being developed as an orally administered treatment for patients with moderate to severe rheumatoid arthritis (RA) and other autoimmune disorders. upadacitinib 27-39 Janus kinase 1 Homo sapiens 55-75 31201513-1 2019 Ruxolitinib is the only commercially available JAK1/2 inhibitor approved for the treatment of myelofibrosis-related splenomegaly and symptoms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 47-53 31317509-10 2019 Several more selective JAK-1 inhibitors, including filgotinib and upadacitinib, have also shown positive results in phase II studies and are currently enrolling in phase III development programs. GLPG0634 51-61 Janus kinase 1 Homo sapiens 23-28 31317509-10 2019 Several more selective JAK-1 inhibitors, including filgotinib and upadacitinib, have also shown positive results in phase II studies and are currently enrolling in phase III development programs. upadacitinib 66-78 Janus kinase 1 Homo sapiens 23-28 31334773-0 2019 Filgotinib, a JAK1 Inhibitor, for Treatment-Resistant Rheumatoid Arthritis. GLPG0634 0-10 Janus kinase 1 Homo sapiens 14-18 30768860-1 2019 Filgotinib is a potent, selective Janus kinase-1 inhibitor being developed to treat chronic inflammatory diseases. GLPG0634 0-10 Janus kinase 1 Homo sapiens 34-48 31360575-1 2019 Baricitinib is a Janus kinase 1/2 (JAK1/2) inhibitor used in the treatment of rheumatoid arthritis. baricitinib 0-11 Janus kinase 1 Homo sapiens 35-41 31289316-1 2019 JAK2/STAT signaling participates in the Ph-negative myeloproliferative neoplasms (MPN) pathophysiology and has been targeted by ruxolitinib, a JAK1/2 inhibitor. ruxolitinib 128-139 Janus kinase 1 Homo sapiens 143-149 30663869-1 2019 OBJECTIVE: To assess the frequency of cardiovascular and venous thromboembolic events in clinical studies of baricitinib, an oral, selective JAK1 and JAK2 inhibitor approved in more than 50 countries for the treatment of moderately-to-severely active rheumatoid arthritis (RA). baricitinib 109-120 Janus kinase 1 Homo sapiens 141-145 30940655-8 2019 By targeting the RET-Src axis, regorafenib potently inhibited JAK1/2-STAT1 and MAPK signaling and subsequently attenuated the IFNgamma-induced PD-L1 and IDO1 expression without affecting MHC-I expression much. regorafenib 31-42 Janus kinase 1 Homo sapiens 62-66 31040122-1 2019 OBJECTIVE: To evaluate clinical outcomes in patients who changed treatment from adalimumab to baricitinib, an oral Janus kinase (JAK)1/JAK2 inhibitor, during a phase III programme. baricitinib 94-105 Janus kinase 1 Homo sapiens 115-134 30767864-4 2019 Baricitinib, an oral selective inhibitor of JAK1 and JAK2, offers an effective treatment for RA in a wide range of patients. baricitinib 0-11 Janus kinase 1 Homo sapiens 44-48 30767864-7 2019 This narrative review focuses on the clinical efficacy and safety of baricitinib, but also provides an overview of its mechanism of action in relation to JAK1/JAK2 signalling and discusses the possible clinical implications in patients with RA. baricitinib 69-80 Janus kinase 1 Homo sapiens 154-158 31144250-5 2019 The JAK1/2 inhibitor ruxolitinib was administered on an off-label basis. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 30997845-0 2019 Combined use of tofacitinib (pan-JAK inhibitor) and ruxolitinib (a JAK1/2 inhibitor) for refractory T-cell prolymphocytic leukemia (T-PLL) with a JAK3 mutation. ruxolitinib 52-63 Janus kinase 1 Homo sapiens 67-73 30997748-1 2019 Ruxolitinib, an orally bioavailable and selective inhibitor of Janus kinase 1 (JAK1) and JAK2, significantly reduces splenomegaly and disease-related symptoms in patients with myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 63-77 31130260-1 2019 BACKGROUND: Upadacitinib, an oral Janus kinase (JAK)1-selective inhibitor, showed efficacy in combination with stable background conventional synthetic disease-modifying antirheumatic drugs (csDMARDs) in patients with rheumatoid arthritis who had an inadequate response to DMARDs. upadacitinib 12-24 Janus kinase 1 Homo sapiens 34-53 30997748-1 2019 Ruxolitinib, an orally bioavailable and selective inhibitor of Janus kinase 1 (JAK1) and JAK2, significantly reduces splenomegaly and disease-related symptoms in patients with myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 79-83 31059310-6 2019 Expert opinion: Peficitinib is a novel JAK3 inhibitor potently inhibiting JAK3 enzymatic activity and JAK1/3-mediated cell proliferation. peficitinib 16-27 Janus kinase 1 Homo sapiens 102-106 31093950-1 2019 Peficitinib [Smyraf (Astellas Pharma)] is a Janus kinase (JAK)1, JAK2, JAK3 and tyrosine kinase (Tyk)2 (pan-JAK) inhibitor recently approved in Japan for the treatment of rheumatoid arthritis. peficitinib 0-11 Janus kinase 1 Homo sapiens 45-64 31096817-1 2019 BACKGROUND: Tofacitinib is an oral Janus kinase (JAK) inhibitor that targets JAK1 and JAK3, and thus regulates immune response. tofacitinib 12-23 Janus kinase 1 Homo sapiens 77-81 30633369-1 2019 Upadacitinib is a novel selective Janus kinase 1 inhibitor developed for treatment of rheumatoid arthritis and other autoimmune diseases. upadacitinib 0-12 Janus kinase 1 Homo sapiens 34-48 30814061-7 2019 We found that ibrutinib decreases the CLL PFs and, interestingly, also reduces AID expression, which correlates with dampened AKT and Janus Kinase 1 signaling. ibrutinib 14-23 Janus kinase 1 Homo sapiens 134-148 31275057-11 2019 Focusing on IFN signaling, we showed that ligand, IFN receptor, the JAKs, and the STATs all undergo endocytosis and ATP-dependent nuclear translocation to promoters of genes specifically activated by IFNs. Adenosine Triphosphate 116-119 Janus kinase 1 Homo sapiens 68-72 30981183-5 2019 CAG predominantly caused negative regulation of STAT3 phosphorylation at tyrosine 705 through the abrogation of Src and Janus-activated kinases (JAK1/2) activation. cycloastragenol 0-3 Janus kinase 1 Homo sapiens 145-151 30990343-8 2019 The results of dual-luciferase reporter assay indicated that miR-1225 targeted the 3"-untranslated region of JAK1 for silencing. mir-1225 61-69 Janus kinase 1 Homo sapiens 109-113 30990343-9 2019 Silencing of JAK1 expression counteracted the suppressive influence of miR-1225 depletion in PC cells. mir-1225 71-79 Janus kinase 1 Homo sapiens 13-17 30999933-2 2019 Baricitinib is an oral, selective Janus kinase (JAK) 1/JAK 2 inhibitor and is approved for the treatment of moderately to severely active RA in adults in over 50 countries including European countries, the USA, and Japan. baricitinib 0-11 Janus kinase 1 Homo sapiens 34-54 30688081-8 2019 A mixture of animal model studies and human case studies have reported the use of baricitinib (JAK 1/2), ruxolitinib (JAK 1/2), and tofacitinib (JAK 1/3) for the management of AA. baricitinib 82-93 Janus kinase 1 Homo sapiens 95-102 30688081-8 2019 A mixture of animal model studies and human case studies have reported the use of baricitinib (JAK 1/2), ruxolitinib (JAK 1/2), and tofacitinib (JAK 1/3) for the management of AA. tofacitinib 132-143 Janus kinase 1 Homo sapiens 145-152 31016396-5 2019 The JAK1/3 inhibitor, tofacitinib, was shown to both induce and maintain clinical remission and mucosal healing in ulcerative colitis (UC). tofacitinib 22-33 Janus kinase 1 Homo sapiens 4-10 30833158-3 2019 Simulation of water networks in combination with docking enabled us to identify the key waters and to optimize our primary hit into a low nanomolar JAK2 lead with promising selectivity over JAK1. Water 14-19 Janus kinase 1 Homo sapiens 190-194 29410014-1 2019 BACKGROUND: Baricitinib, an oral selective inhibitor of Janus kinase 1 and Janus kinase 2, modulates proinflammatory cytokine signaling. baricitinib 12-23 Janus kinase 1 Homo sapiens 56-70 33911570-1 2019 Ruxolitinib is a Janus kinase (JAK)1 and JAK2 inhibitor approved for the treatment of myelofibrosis and for polycythemia patients who are resistant or intolerant to hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-36 33911570-1 2019 Ruxolitinib is a Janus kinase (JAK)1 and JAK2 inhibitor approved for the treatment of myelofibrosis and for polycythemia patients who are resistant or intolerant to hydroxyurea. Hydroxyurea 165-176 Janus kinase 1 Homo sapiens 17-36 30843659-3 2019 The JAK1/2 inhibitor ruxolitinib was prescribed to 12 CLL patients with abnormal serum beta-2 microglobulin levels after 6 months or persistent lymphadenopathy or splenomegaly after 12 months on ibrutinib using a 3 + 3 phase 1 trial design (NCT02912754). ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 30961670-12 2019 Expressions of JAK1,2, STAT3 PD-L1 and ATM were increased in A549CisR and H157CisR cells and could by induced by cisplatin in parental lung cancer cells. Cisplatin 115-124 Janus kinase 1 Homo sapiens 15-21 30760472-13 2019 Blocking IL-21R or using the JAK1/2 inhibitor ruxolitinib reduced the Tfh cells" capacity to stimulate the plasmablasts and decreased the Ig production. ruxolitinib 46-57 Janus kinase 1 Homo sapiens 29-35 30760472-15 2019 The IL-21 pathway or JAK1/2 blockade by ruxolitinib could be a promising strategy in the treatment of SSc. ruxolitinib 40-51 Janus kinase 1 Homo sapiens 21-25 30931929-2 2019 Iron directly binds CDK1, which is upregulated in several cancers, thereby promoting JAK1 phosphorylation and activation of STAT3 signaling to promote colorectal carcinogenesis. Iron 0-4 Janus kinase 1 Homo sapiens 85-89 30609183-0 2019 Expression of pro-inflammatory cytokines and mediators induced by Bisphenol A via ERK-NFkappaB and JAK1/2-STAT3 pathways in macrophages. bisphenol A 66-77 Janus kinase 1 Homo sapiens 99-105 30609183-10 2019 Phosphorylation of JAK1 and JAK2 was also significantly induced by BPA in a concentration-dependent manner (P < 0.05). bisphenol A 67-70 Janus kinase 1 Homo sapiens 19-23 30201397-4 2019 Ruxolitinib, a selective JAK1/2 inhibitor, has recently gained favor as a second-line approach in patients with steroid-refractory cGVHD. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 25-31 30930775-8 2019 Tofacitinib, a JAK inhibitor targeting predominantly JAK1 and JAK3, has been approved for the treatment of ulcerative colitis (UC), and there are other specific JAK inhibitors under development that may be effective in Crohn"s. tofacitinib 0-11 Janus kinase 1 Homo sapiens 53-57 30639623-1 2019 Ruxolitinib is a JAK-1/JAK-2 inhibitor indicated for the treatment of polycythemia vera and primary or secondary myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-22 30500075-1 2019 Upadacitinib is a novel selective oral Janus kinase 1 (JAK) inhibitor being developed for treatment of several inflammatory diseases. upadacitinib 0-12 Janus kinase 1 Homo sapiens 39-53 30500075-1 2019 Upadacitinib is a novel selective oral Janus kinase 1 (JAK) inhibitor being developed for treatment of several inflammatory diseases. upadacitinib 0-12 Janus kinase 1 Homo sapiens 55-58 30715158-0 2019 Reply: Janus kinase 1/2 inhibition with baricitinib in the treatment of juvenile dermatomyositis. baricitinib 40-51 Janus kinase 1 Homo sapiens 7-21 30571852-1 2019 Myeloproliferative neoplasms (MPNs) are developing resistance to therapy by JAK1/2 inhibitor ruxolitinib. ruxolitinib 93-104 Janus kinase 1 Homo sapiens 76-82 30571852-2 2019 To explore the mechanism of ruxolitinib"s limited effect, we examined the JAK1/2 mediated induction of proliferation related ERK1/2 and AKT signaling by proinflammatory interleukin-6 (IL-6) in MPN granulocytes and JAK2V617F mutated human erythroleukemia (HEL) cells. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 74-80 30571852-5 2019 Only JAK1/2 inhibitor ruxolitinib largely activated ERK1/2 signaling in essential thrombocythemia and PMF (up to 4.6 fold), with a more prominent activation in JAK2V617F positive granulocytes. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 5-11 30357932-3 2019 OBJECTIVE: Our aim was to address the direct impact of kinase inhibition of the JAK1/3 pathways by tofacitinib on keratinocyte immune function and barrier formation in atopic dermatitis (AD) and psoriasis. tofacitinib 99-110 Janus kinase 1 Homo sapiens 80-84 31327403-2 2019 To date, three JAK inhibitors have been tested in patients with moderate-to-severe CD: tofacitinib (pan-JAK inhibitor), filgotinib (JAK1 inhibitor) and upadacitinib (JAK1 inhibitor). upadacitinib 152-164 Janus kinase 1 Homo sapiens 166-170 30675650-1 2019 OPINION STATEMENT: Seven years after the approval of the Janus kinase 1/2 (JAK1/2) inhibitor ruxolitinib, it remains the only drug licensed for the treatment of myelofibrosis. ruxolitinib 93-104 Janus kinase 1 Homo sapiens 75-81 30675650-4 2019 The JAK2-selective inhibitor fedratinib has recently been resurrected, and there has been a resurgence of interest in the failed JAK1/2 inhibitor momelotinib, which possibly improves anemia. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 146-157 Janus kinase 1 Homo sapiens 129-135 30670049-9 2019 Momelotinib, an inhibitor of JAK1/JAK2, consistently abrogated the STAT5/LY6G6D axis in vitro, sensitizing MSS cancer cells with an intact JAK-STAT signaling, to efficiently respond to trametinib, a MEK inhibitor used in clinical setting. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 29-33 30670049-9 2019 Momelotinib, an inhibitor of JAK1/JAK2, consistently abrogated the STAT5/LY6G6D axis in vitro, sensitizing MSS cancer cells with an intact JAK-STAT signaling, to efficiently respond to trametinib, a MEK inhibitor used in clinical setting. trametinib 185-195 Janus kinase 1 Homo sapiens 29-33 30621055-4 2019 We found that OMT can inhibit the constitutive activation of STAT5 by suppressing the activation of JAK1/2 and c-Src, nuclear localization, as well as STAT5 binding to DNA in A549 cells and abrogated IL-6-induced STAT5 phosphorylation in H1299 cells. oxymatrine 14-17 Janus kinase 1 Homo sapiens 100-106 30806707-2 2019 Tofacitinib is a selective JAK1, 3 inhibitor with less activity against JAK2 and TYK2 and baricitinib is a selective, oral JAK1, 2 inhibitor with moderate activity against TYK2 and significantly less activity against JAK3. tofacitinib 0-11 Janus kinase 1 Homo sapiens 27-31 30806707-2 2019 Tofacitinib is a selective JAK1, 3 inhibitor with less activity against JAK2 and TYK2 and baricitinib is a selective, oral JAK1, 2 inhibitor with moderate activity against TYK2 and significantly less activity against JAK3. baricitinib 90-101 Janus kinase 1 Homo sapiens 123-127 30394138-8 2019 Expert commentary: Upadacitinib has displayed a rapid and favorable efficacy profile in RA but despite being a selective JAK1 inhibitor appears to have a similar safety profile to less-selective Jakinibs. upadacitinib 19-31 Janus kinase 1 Homo sapiens 121-125 29714141-11 2019 Bazedoxifene also inhibited JAK1 binding to IL-6/IL-6R/GP130 complexes and STAT3 phosphorylation. bazedoxifene 0-12 Janus kinase 1 Homo sapiens 28-32 33094033-1 2019 Introduction: The Janus kinase (JAK)1/2 inhibitor ruxolitinib provides rapid, sustained and often dramatic benefits to patients with myelofibrosis, inducing spleen shrinkage and ameliorating symptoms, and improves survival. ruxolitinib 50-61 Janus kinase 1 Homo sapiens 18-39 30394138-2 2019 Upadacitinib selectively inhibits Janus Kinase 1 (JAK1) which could potentially reduce JAK2 and JAK3-related side effects. upadacitinib 0-12 Janus kinase 1 Homo sapiens 34-48 30030153-5 2019 After intermittent UVB exposure, melanocytes treated with the JAK inhibitor ruxolitinib reduced expression of HMGB1 and MX1 as well as activation of JAK1 (pJAK1) and signal transducer and activator of transcription 1 (pSTAT1). ruxolitinib 76-87 Janus kinase 1 Homo sapiens 149-153 30394138-2 2019 Upadacitinib selectively inhibits Janus Kinase 1 (JAK1) which could potentially reduce JAK2 and JAK3-related side effects. upadacitinib 0-12 Janus kinase 1 Homo sapiens 50-54 30115734-5 2019 METHODS: This phase Ib/II dose-optimization study assessed itacitinib, a selective JAK1 inhibitor, combined with nab-paclitaxel plus gemcitabine in adults with treatment-naive advanced/metastatic disease (Part 1) or pancreatic adenocarcinoma (Parts 2/2A; NCT01858883). INCB039110 59-69 Janus kinase 1 Homo sapiens 83-87 31288716-1 2019 The search for inhibitors of the Janus kinase family (JAK1, JAK2, JAK3 and TYK2) has been ongoing for several decades and has resulted in a number of JAK inhibitors being approved for use in patients, such as tofacitinib for the treatment of autoimmune diseases such as Rheumatoid Arthritis (RA). tofacitinib 209-220 Janus kinase 1 Homo sapiens 54-58 31288716-2 2019 Although initially thought to be a JAK3 selective inhibitor, tofacitinib was subsequently found to possess significant activity to inhibit JAK1 and JAK2 which has contributed to some adverse side effects. tofacitinib 61-72 Janus kinase 1 Homo sapiens 139-143 30219772-1 2019 OBJECTIVE: Baricitinib is an oral, once-daily selective Janus kinase (JAK1/JAK2) inhibitor for adults with moderately to severely active rheumatoid arthritis (RA). baricitinib 11-22 Janus kinase 1 Homo sapiens 70-74 30558676-5 2018 Ruxolitinib is a tyrosine kinase inhibitor which inhibits JAK1 and JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 58-62 31484895-4 2019 The Jak1/2 inhibitor ruxolitinib can simultaneously inhibit the signaling pathway of multiple cytokines with relevance for GvHD, such as interferon (IFN-gamma), IL-2, and IL-6. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 30058112-1 2018 OBJECTIVE: Baricitinib is an orally administered inhibitor of JAK1 and JAK2 that has been shown to be effective in treating rheumatoid arthritis (RA). baricitinib 11-22 Janus kinase 1 Homo sapiens 62-66 30526546-8 2018 Curcumin suppressed the phosphorylation levels of JAK1, STAT1, and STAT3, while curcumin did not inhibit the activation of JAK/STAT pathway when miR-99a was knocked down. Curcumin 0-8 Janus kinase 1 Homo sapiens 50-54 30558329-7 2018 Based on QPCR data, the action of EGCG on p-STAT1 seems to be mediated via downregulation of the expression of JAK2 but not JAK1 leading to the inhibition of human leukocyte antigens (HLA-DR and HLA-B) expression probably via IRF-1. epigallocatechin gallate 34-38 Janus kinase 1 Homo sapiens 124-128 30360969-0 2018 Efficacy and safety of filgotinib, a selective Janus kinase 1 inhibitor, in patients with active psoriatic arthritis (EQUATOR): results from a randomised, placebo-controlled, phase 2 trial. GLPG0634 23-33 Janus kinase 1 Homo sapiens 47-61 30088677-0 2018 Influence of age and renal impairment on the steady state pharmacokinetics of filgotinib, a selective JAK1 inhibitor. GLPG0634 78-88 Janus kinase 1 Homo sapiens 102-106 30088677-1 2018 AIMS: Filgotinib (GS-6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthritis and with Crohn"s disease. GLPG0634 6-16 Janus kinase 1 Homo sapiens 68-82 30088677-1 2018 AIMS: Filgotinib (GS-6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthritis and with Crohn"s disease. GLPG0634 6-16 Janus kinase 1 Homo sapiens 84-88 30088677-1 2018 AIMS: Filgotinib (GS-6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthritis and with Crohn"s disease. Filgotinib maleate 18-25 Janus kinase 1 Homo sapiens 68-82 30088677-1 2018 AIMS: Filgotinib (GS-6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthritis and with Crohn"s disease. Filgotinib maleate 18-25 Janus kinase 1 Homo sapiens 84-88 30088677-1 2018 AIMS: Filgotinib (GS-6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthritis and with Crohn"s disease. GLPG0634 36-44 Janus kinase 1 Homo sapiens 68-82 30088677-1 2018 AIMS: Filgotinib (GS-6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthritis and with Crohn"s disease. GLPG0634 36-44 Janus kinase 1 Homo sapiens 84-88 30360969-2 2018 We aimed to investigate the efficacy and safety of filgotinib, a selective JAK1 inhibitor, for the treatment of psoriatic arthritis. GLPG0634 51-61 Janus kinase 1 Homo sapiens 75-79 30360970-0 2018 Efficacy and safety of filgotinib, a selective Janus kinase 1 inhibitor, in patients with active ankylosing spondylitis (TORTUGA): results from a randomised, placebo-controlled, phase 2 trial. GLPG0634 23-33 Janus kinase 1 Homo sapiens 47-61 30360970-2 2018 The TORTUGA trial investigated the efficacy and safety of filgotinib, an oral selective Janus kinase 1 (JAK1) inhibitor, for the treatment of patients with active ankylosing spondylitis. GLPG0634 58-68 Janus kinase 1 Homo sapiens 88-102 30360970-2 2018 The TORTUGA trial investigated the efficacy and safety of filgotinib, an oral selective Janus kinase 1 (JAK1) inhibitor, for the treatment of patients with active ankylosing spondylitis. GLPG0634 58-68 Janus kinase 1 Homo sapiens 104-108 30519495-1 2018 Ruxolitinib is an oral selective Janus-associated kinase 1 (JAK1) and JAK2 inhibitor that was initially approved by the FDA in 2014 for treatment of myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 60-64 30519664-0 2018 Fungal metabolite (+)-terrein suppresses IL-6/sIL-6R-induced CSF1 secretion by inhibiting JAK1 phosphorylation in human gingival fibroblasts. terrein 18-29 Janus kinase 1 Homo sapiens 90-94 30519664-5 2018 In this study, we provided the possibility of novel action that (+)-terrein inhibits activation of Janus-activated kinase 1 (JAK1), which has a central function in IL-6 signaling cascade, and alters expression of mRNAs and proteins induced by IL-6/soluble IL-6 receptor (sIL-6R) stimulation in HGFs. terrein 64-75 Janus kinase 1 Homo sapiens 99-123 30519664-5 2018 In this study, we provided the possibility of novel action that (+)-terrein inhibits activation of Janus-activated kinase 1 (JAK1), which has a central function in IL-6 signaling cascade, and alters expression of mRNAs and proteins induced by IL-6/soluble IL-6 receptor (sIL-6R) stimulation in HGFs. terrein 64-75 Janus kinase 1 Homo sapiens 125-129 30519664-8 2018 Next, to test the effect of (+)-terrein on IL-6/sIL-6R signaling cascade, we demonstrated whether (+)-terrein affects phosphorylation of JAK1 and its downstream proteins, Akt and SHP-2. terrein 98-109 Janus kinase 1 Homo sapiens 137-141 30519664-9 2018 Western blotting revealed that (+)-terrein inhibited IL-6/sIL-6R-induced phosphorylation of JAK1, Akt, and SHP-2. terrein 31-42 Janus kinase 1 Homo sapiens 92-96 30519664-10 2018 Therefore, (+)-terrein suppresses IL-6/sIL-6R-induced expression of CSF1 and VEGF via inhibition of JAK1, Akt, and SHP-2. terrein 11-22 Janus kinase 1 Homo sapiens 100-104 30453910-4 2018 Ruxolitinib is a small molecule inhibitor of JAK1 and JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 45-49 30519495-1 2018 Ruxolitinib is an oral selective Janus-associated kinase 1 (JAK1) and JAK2 inhibitor that was initially approved by the FDA in 2014 for treatment of myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 33-58 29939445-14 2018 Ruxolitinib also significantly inhibited the production of IL-6, TNF-alpha and MCP-1 as induced by A23817 and substance P. Selective STAT5 inhibition with pimozide resulted in diminished degranulation and inhibition of cytokine production as induced by A23817 and substance P. CONCLUSIONS & CLINICAL RELEVANCE: This study demonstrates that the JAK1/JAK2 inhibitor ruxolitinib can inhibit MCactivity, possibly through prevention of STAT5 activation. Pimozide 155-163 Janus kinase 1 Homo sapiens 344-348 30123970-2 2018 This study evaluated the addition of ruxolitinib, a potent JAK1/2 inhibitor, to regorafenib in patients with relapsed/refractory metastatic CRC. ruxolitinib 37-48 Janus kinase 1 Homo sapiens 59-65 29939445-0 2018 The JAK1/JAK2- inhibitor ruxolitinib inhibits mast cell degranulation and cytokine release. ruxolitinib 25-36 Janus kinase 1 Homo sapiens 4-8 29939445-7 2018 Ruxolitinib, a JAK1/JAK2 inhibitor, indeed decreases symptoms like pruritus and fatigue in patients with myeloproliferative neoplasms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-19 29939445-9 2018 OBJECTIVE: To investigate the effect of JAK1/2-inhibition with ruxolitinib in the human mast cell lines LAD2 and HMC1. ruxolitinib 63-74 Janus kinase 1 Homo sapiens 40-46 29939445-14 2018 Ruxolitinib also significantly inhibited the production of IL-6, TNF-alpha and MCP-1 as induced by A23817 and substance P. Selective STAT5 inhibition with pimozide resulted in diminished degranulation and inhibition of cytokine production as induced by A23817 and substance P. CONCLUSIONS & CLINICAL RELEVANCE: This study demonstrates that the JAK1/JAK2 inhibitor ruxolitinib can inhibit MCactivity, possibly through prevention of STAT5 activation. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 344-348 30324817-1 2018 INTRODUCTION: Despite the dramatic progress made in the treatment of patients with myelofibrosis since the introduction of the JAK1/2 inhibitor ruxolitinib, a therapeutic option that can modify the natural history of the disease and prevent evolution to blast-phase is still lacking. ruxolitinib 144-155 Janus kinase 1 Homo sapiens 127-133 30536347-14 2018 During this process, the activations of NF-kappaB and JAK1/STAT3 pathways were inhibited after interaction of ROR and miR-26. mir-26 118-124 Janus kinase 1 Homo sapiens 54-58 29691471-6 2018 Furthermore, baricitinib (an inhibitor of Janus kinases 1 and 2 (JAK1/JAK2) downstream of IFNgammaR/IL6R) completely prevented GvHD; expanded regulatory T cells by preserving JAK3-STAT5 signaling; downregulated CXCR3 and helper T cells 1 and 2 while preserving allogeneic antigen-presenting cell-stimulated T-cell proliferation; and suppressed the expression of major histocompatibility complex II (I-Ad), CD80/86, and PD-L1 on host antigen-presenting cells. baricitinib 13-24 Janus kinase 1 Homo sapiens 42-63 29691471-6 2018 Furthermore, baricitinib (an inhibitor of Janus kinases 1 and 2 (JAK1/JAK2) downstream of IFNgammaR/IL6R) completely prevented GvHD; expanded regulatory T cells by preserving JAK3-STAT5 signaling; downregulated CXCR3 and helper T cells 1 and 2 while preserving allogeneic antigen-presenting cell-stimulated T-cell proliferation; and suppressed the expression of major histocompatibility complex II (I-Ad), CD80/86, and PD-L1 on host antigen-presenting cells. baricitinib 13-24 Janus kinase 1 Homo sapiens 65-69 30035369-9 2018 Moreover, STAT1 knockdown significantly reduced EGF-mediated PD-L1 expression, and ruxolitinib, a JAK1/JAK2 inhibitor, significantly inhibited STAT1 phosphorylation to reduce the IFNr-mediated PD-L1 axis. ruxolitinib 83-94 Janus kinase 1 Homo sapiens 98-102 29481660-0 2018 JAK1/JAK2 inhibition by baricitinib in diabetic kidney disease: results from a Phase 2 randomized controlled clinical trial. baricitinib 24-35 Janus kinase 1 Homo sapiens 0-4 29481660-2 2018 Baricitinib is an oral, reversible, selective inhibitor of JAK1 and JAK2. baricitinib 0-11 Janus kinase 1 Homo sapiens 59-63 32004164-2 2018 Ruxolitinib is a selective inhibitor of JAK-1 and JAK-2 used to treat PMF. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 40-45 30257946-7 2018 Treating CD4+ T cells with Ruxolitinib, an inhibitor of JAK1 and JAK2, effectively blocked IL-15-induced SAMHD1 phosphorylation and protected CD4+ T cells from HIV infection. ruxolitinib 27-38 Janus kinase 1 Homo sapiens 56-60 30257946-11 2018 Time-limited interventions with JAK1 inhibitors, such as Ruxolitinib, should prevent the inactivation of the endogenous restriction factor SAMHD1 and protect this long-lived CD4+ T-memory cell population from HIV infection. ruxolitinib 57-68 Janus kinase 1 Homo sapiens 32-36 30145050-3 2018 Here, we describe the identification of the novel orally bioavailable JAK inhibitor 18, peficitinib (also known as ASP015K), which showed moderate selectivity for JAK3 over JAK1, JAK2, and TYK2 in enzyme assays. peficitinib 88-99 Janus kinase 1 Homo sapiens 173-177 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 98-109 Janus kinase 1 Homo sapiens 53-57 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. 1H-pyrrolo[2,3-b]pyridine-5-carboxamide 133-172 Janus kinase 1 Homo sapiens 53-57 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 185-196 Janus kinase 1 Homo sapiens 53-57 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. Hydrogen 210-218 Janus kinase 1 Homo sapiens 53-57 30145050-6 2018 Interestingly, the binding modes of peficitinib in the ATP-binding pockets differed among JAK1, JAK2, JAK3, and TYK2. peficitinib 36-47 Janus kinase 1 Homo sapiens 90-94 30145050-6 2018 Interestingly, the binding modes of peficitinib in the ATP-binding pockets differed among JAK1, JAK2, JAK3, and TYK2. Adenosine Triphosphate 55-58 Janus kinase 1 Homo sapiens 90-94 30145050-7 2018 WaterMap analysis of the crystal structures suggests that unfavorable water molecules are the likely reason for the difference in orientation of the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold to the hinge region among JAKs. Water 70-75 Janus kinase 1 Homo sapiens 224-228 30145050-7 2018 WaterMap analysis of the crystal structures suggests that unfavorable water molecules are the likely reason for the difference in orientation of the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold to the hinge region among JAKs. 1H-pyrrolo[2,3-b]pyridine-5-carboxamide 149-188 Janus kinase 1 Homo sapiens 224-228 30006916-2 2018 Baricitinib is an oral, selective JAK 1 and 2 inhibitor which has been shown to be effective in the treatment of RA in several clinical trials. baricitinib 0-11 Janus kinase 1 Homo sapiens 34-45 30185657-4 2018 Herein, we found that CSA drives SCC proliferation and tumor growth through IL-22 and JAK/STAT pathway induction. Cyclosporine 22-25 Janus kinase 1 Homo sapiens 86-89 30010187-2 2018 Ruxolitinib is a JAK1/2 inhibitor that may control myelofibrosis (MF)-related splenomegaly and symptoms and can be prescribed regardless of age. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-23 30245189-4 2018 Since ruxolitinib, a JAK1/JAK2 inhibitor, suppresses NF-kB expression, we conducted a phase 1 dose-escalation study to determine the safety and efficacy of ruxolitinib in previously treated lower-risk MDS patients with evidence of NF-kB activation. ruxolitinib 6-17 Janus kinase 1 Homo sapiens 21-25 30590943-14 2018 JAK1/JAK2 inhibitor ruxolitinib is approved for hydroxyurea resistant/intolerant patients. ruxolitinib 20-31 Janus kinase 1 Homo sapiens 0-4 30590943-14 2018 JAK1/JAK2 inhibitor ruxolitinib is approved for hydroxyurea resistant/intolerant patients. Hydroxyurea 48-59 Janus kinase 1 Homo sapiens 0-4 30949000-0 2018 Successful treatment of atopic dermatitis with the JAK1 inhibitor oclacitinib. oclacitinib 66-77 Janus kinase 1 Homo sapiens 51-55 30949000-1 2018 We report the first case of atopic dermatitis successfully treated with the oral Janus kinase-1 (JAK1) inhibitor oclacitinib. oclacitinib 113-124 Janus kinase 1 Homo sapiens 81-95 30949000-1 2018 We report the first case of atopic dermatitis successfully treated with the oral Janus kinase-1 (JAK1) inhibitor oclacitinib. oclacitinib 113-124 Janus kinase 1 Homo sapiens 97-101 30185657-5 2018 We in turn inhibited SCC growth with an FDA-approved JAK1/2 inhibitor, ruxolitinib. ruxolitinib 71-82 Janus kinase 1 Homo sapiens 53-59 30185657-8 2018 JAK/STAT pathway genes were highly expressed in tumors from a cohort of CSA-exposed OTRs and in SCC with high risk for metastasis. Cyclosporine 72-75 Janus kinase 1 Homo sapiens 0-3 30185657-10 2018 In nude mice engrafted with human A431 cells, IL-22 and CSA treatment increased tumor growth and upregulated IL-22 receptor, JAK1, and STAT1/3 expression. Cyclosporine 56-59 Janus kinase 1 Homo sapiens 125-129 29945795-3 2018 Selective JAK1/2 inhibitor, ruxolitinib (3), and pan-HDAC inhibitor vorinostat (4) were linked together by a single nitrogen atom to create a new series of compounds with very potent JAK2 and HDAC6 inhibition with selectivity against HDAC1. Nitrogen 116-124 Janus kinase 1 Homo sapiens 10-16 30078086-1 2018 The objective of this study was to evaluate structural damage progression based on clinical response in rheumatoid arthritis patients with no or limited prior disease-modifying anti-rheumatic drug treatment receiving the Janus kinase (JAK)1/JAK2 inhibitor baricitinib 4 mg, methotrexate (MTX), or the combination. baricitinib 256-267 Janus kinase 1 Homo sapiens 221-240 30207045-6 2018 In this study, as a JAK1 and JAK3 inhibitor, tofacitinib has been proposed for the treatment of refractory pemphigus patients. tofacitinib 45-56 Janus kinase 1 Homo sapiens 20-24 29681434-2 2018 We evaluated the JAK1/JAK2 inhibitor ruxolitinib plus pemetrexed/cisplatin first-line in patients with stage IIIB/IV or recurrent nonsquamous NSCLC with systemic inflammation (modified Glasgow prognostic score [mGPS] 1/2). ruxolitinib 37-48 Janus kinase 1 Homo sapiens 17-21 30001163-1 2018 INTRODUCTION: Treatment with ruxolitinib, a selective JAK1/2 inhibitor, has significantly improved the lives of patients with myelofibrosis. ruxolitinib 29-40 Janus kinase 1 Homo sapiens 54-60 30043249-1 2018 The oral Janus associated kinase (JAK1/2) inhibitor ruxolitinib has been available for treatment of patients with intermediate or high-risk myelofibrosis in Europe since 2012. ruxolitinib 52-63 Janus kinase 1 Homo sapiens 34-40 30114348-5 2018 Currently ruxolitinib, a JAK1/JAK2 inhibitor, is also approved for PV patients with hydroxyurea resistance or intolerance. ruxolitinib 10-21 Janus kinase 1 Homo sapiens 25-29 30159126-5 2018 Therefore in this study we investigated whether inhibiting both JAK1/2 and CDK4/6, using LEE011 and ruxolitinib respectively is effective in NKTL. ribociclib 89-95 Janus kinase 1 Homo sapiens 64-70 30159126-5 2018 Therefore in this study we investigated whether inhibiting both JAK1/2 and CDK4/6, using LEE011 and ruxolitinib respectively is effective in NKTL. ruxolitinib 100-111 Janus kinase 1 Homo sapiens 64-70 29616317-2 2018 Ruxolitinib, a JAK1/2 inhibitor, is the lone therapy approved for MF, offering a clear symptom and spleen benefit at the expense of treatment-related cytopenias. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 29616317-3 2018 Pacritinib (PAC), a multi-kinase inhibitor with specificity for JAK2, FLT3, and IRAK1 but sparing JAK1, has demonstrated clinical activity in MF with minimal myelosuppression. 11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,26-triazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene 0-10 Janus kinase 1 Homo sapiens 98-102 29076110-1 2018 BACKGROUND AND OBJECTIVES: Upadacitinib is a janus kinase (JAK) 1 inhibitor being developed for the treatment of rheumatoid arthritis (RA) and other inflammatory diseases. upadacitinib 27-39 Janus kinase 1 Homo sapiens 45-65 29672897-0 2018 Evaluation of a Janus kinase 1 inhibitor, PF-04965842, in healthy subjects: A phase 1, randomized, placebo-controlled, dose-escalation study. Abrocitinib 42-53 Janus kinase 1 Homo sapiens 16-30 29672897-1 2018 AIMS: To determine the safety, tolerability, pharmacokinetics and pharmacodynamics of the Janus kinase 1-selective inhibitor, PF-04965842. Abrocitinib 126-137 Janus kinase 1 Homo sapiens 90-104 29870712-7 2018 In addition, DHHL suppressed IL-4-induced STAT-6 and JAK-1 tyrosine phosphorylation, suggesting that this compound inhibited M2 polarization by suppressing the JAK-STAT signaling pathway. Tyrosine 59-67 Janus kinase 1 Homo sapiens 53-58 29675680-2 2018 This randomized phase 2 trial evaluated the efficacy and safety of the addition of ruxolitinib, a JAK1/JAK2 inhibitor, to capecitabine in patients with HER2-negative advanced breast cancer and high systemic inflammation (modified Glasgow Prognostic Score [mGPS] >= 1). ruxolitinib 83-94 Janus kinase 1 Homo sapiens 98-102 29134648-1 2018 Population pharmacokinetic (popPK) modeling was used to characterize the PK profile of the oral Janus kinase (JAK)1/JAK2 inhibitor, baricitinib, in 18 patients with Mendelian interferonopathies who are enrolled in a compassionate use program. baricitinib 132-143 Janus kinase 1 Homo sapiens 96-115 29508247-1 2018 Background Ruxolitinib, a Janus kinase 1 (JAK1)/JAK2 inhibitor, plus capecitabine improved overall survival (OS) vs capecitabine in a subgroup analysis of patients with metastatic pancreatic cancer and systemic inflammation (C-reactive protein [CRP] >13 mg/dL) in the randomized phase II RECAP study. ruxolitinib 11-22 Janus kinase 1 Homo sapiens 42-46 30058088-13 2018 JAK1/JAK2 inhibitor ruxolitinib is approved for hydroxyurea resistant/intolerant patients. ruxolitinib 20-31 Janus kinase 1 Homo sapiens 0-4 29693289-14 2018 Finally, we proved that ATB increased phosphorylated levels of AKT, JAK1, and STAT3, and those increases were all reversed by miR-494 overexpression. atb 24-27 Janus kinase 1 Homo sapiens 68-72 30058088-13 2018 JAK1/JAK2 inhibitor ruxolitinib is approved for hydroxyurea resistant/intolerant patients. Hydroxyurea 48-59 Janus kinase 1 Homo sapiens 0-4 30043749-2 2018 Baricitinib is an oral selective Janus kinase (JAK)1 and JAK2 inhibitor that we hypothesised might have therapeutic benefit in patients with systemic lupus erythematosus. baricitinib 0-11 Janus kinase 1 Homo sapiens 33-52 30123428-7 2018 Next, we investigated the effects of ruxolitinib, an inhibitor of both JAK1 and JAK2, which phosphorylates and activates STAT3. ruxolitinib 37-48 Janus kinase 1 Homo sapiens 71-75 29934865-11 2018 CONCLUSION: JAK1/2 inhibition with ruxolitinib represents a viable option for treatment of refractory CMC, if HSCT is not considered. ruxolitinib 35-46 Janus kinase 1 Homo sapiens 12-18 29695516-0 2018 Phase 1 study of the PI3Kdelta inhibitor INCB040093 +- JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma. INCB039110 70-80 Janus kinase 1 Homo sapiens 55-59 29789426-3 2018 Herein we identified that the Janus kinase 1 (JAK1) interacts with Sirt1 and catalyzes its phosphorylation at the tyrosine residues of 280 and 301, both of which are highly conserved and located in the histone deacetylase catalytic domain of Sirt1. Tyrosine 114-122 Janus kinase 1 Homo sapiens 30-44 29789426-3 2018 Herein we identified that the Janus kinase 1 (JAK1) interacts with Sirt1 and catalyzes its phosphorylation at the tyrosine residues of 280 and 301, both of which are highly conserved and located in the histone deacetylase catalytic domain of Sirt1. Tyrosine 114-122 Janus kinase 1 Homo sapiens 46-50 29649002-0 2018 JAK1/2 inhibition with baricitinib in the treatment of autoinflammatory interferonopathies. baricitinib 23-34 Janus kinase 1 Homo sapiens 0-4 29622655-6 2018 Surprisingly, we found that ruxolitinib, an FDA approved agent targeting JAK1 and JAK2, did not lead to the same anti-myeloma effects. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 73-77 29908669-1 2018 BACKGROUND: Upadacitinib is a selective inhibitor of Janus kinase 1 and was efficacious in phase 2 studies in patients with moderate-to-severe rheumatoid arthritis. upadacitinib 12-24 Janus kinase 1 Homo sapiens 53-67 29645296-2 2018 The JAK1/2 inhibitor Ruxolitinib has remarkable clinical efficacy, including spleen reduction, improvement of constitutional symptoms, and bone marrow (BM) fibrosis reversal. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 29908670-1 2018 BACKGROUND: Phase 2 studies with upadacitinib, a selective Janus kinase 1 (JAK1) inhibitor, have shown safety and efficacy in the treatment of patients with active rheumatoid arthritis. upadacitinib 33-45 Janus kinase 1 Homo sapiens 59-73 29908670-1 2018 BACKGROUND: Phase 2 studies with upadacitinib, a selective Janus kinase 1 (JAK1) inhibitor, have shown safety and efficacy in the treatment of patients with active rheumatoid arthritis. upadacitinib 33-45 Janus kinase 1 Homo sapiens 75-79 31723782-5 2018 Ruxolitinib, a Janus Kinase (JAK) 1/JAK2 inhibitor, has demonstrated efficacy in patients with both myelofibrosis (MF) and polycythemia vera and is well tolerated. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-35 29942363-7 2018 Of note, the success of tofacitinib has spurred the development of JAK1, JAK2 and other JAK3-selective small molecule inhibitors, some of which have also entered the clinical setting, whereas other JAK inhibitors are currently being evaluated in RA clinical trials. tofacitinib 24-35 Janus kinase 1 Homo sapiens 67-71 29459227-4 2018 SiRNA silencing of JAK1, STAT3 and NOX4 diminished the hypoxia-mediated effect while a role of HIF1alpha could be clearly ruled out by the response to hypoxia-mimetics and competition experiments with a plasmid harboring the oxygen-dependent degradation domain of HIF1alpha. Oxygen 225-231 Janus kinase 1 Homo sapiens 19-23 29785143-4 2018 Although JAK2 inhibitors, such as the JAK1/2 inhibitor ruxolitinib and the JAK2/FLT3/CSF1R/IRAK1 inhibitor pacritinib suppress abnormal clone expansion in myelofibrosis, ruxolitinib does not appear to prevent or reverse bone-marrow fibrosis in most patients. ruxolitinib 55-66 Janus kinase 1 Homo sapiens 38-44 28762476-3 2018 Upadacitinib is a Janus kinase 1 inhibitor currently being evaluated in phase III rheumatoid arthritis trials. upadacitinib 0-12 Janus kinase 1 Homo sapiens 18-32 29761158-0 2018 Phase II study of ruxolitinib, a selective JAK1/2 inhibitor, in patients with metastatic triple-negative breast cancer. ruxolitinib 18-29 Janus kinase 1 Homo sapiens 43-49 29761158-2 2018 Ruxolitinib is an orally bioavailable receptor tyrosine inhibitor targeting JAK1 and JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 76-80 29761158-2 2018 Ruxolitinib is an orally bioavailable receptor tyrosine inhibitor targeting JAK1 and JAK2. Tyrosine 47-55 Janus kinase 1 Homo sapiens 76-80 29254929-5 2018 We have examined whether persistent vessel wall inflammation is maintained by lesional T cells, including the newly identified tissue-resident memory T cells, and whether such T cells are sensitive to the cytokine-signaling inhibitor tofacitinib, a Janus kinase (JAK) inhibitor targeting JAK3 and JAK1. tofacitinib 234-245 Janus kinase 1 Homo sapiens 297-301 29468276-10 2018 The JAK1/2 inhibitor ruxolitinib also seems to be effective across a range of patient ages. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 29452839-0 2018 Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor. (r)-3-(3-(methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile 79-170 Janus kinase 1 Homo sapiens 176-180 29452839-1 2018 A series of 3(R)-aminopyrrolidine derivatives were designed and synthesized for JAK1-selective inhibitors through the modification of tofacitinib"s core structure, (3R,4R)-3-amino-4-methylpiperidine. 3(r)-aminopyrrolidine 12-33 Janus kinase 1 Homo sapiens 80-84 29452839-1 2018 A series of 3(R)-aminopyrrolidine derivatives were designed and synthesized for JAK1-selective inhibitors through the modification of tofacitinib"s core structure, (3R,4R)-3-amino-4-methylpiperidine. tofacitinib 134-145 Janus kinase 1 Homo sapiens 80-84 29452839-1 2018 A series of 3(R)-aminopyrrolidine derivatives were designed and synthesized for JAK1-selective inhibitors through the modification of tofacitinib"s core structure, (3R,4R)-3-amino-4-methylpiperidine. (3r,4r)-3-amino-4-methylpiperidine 164-198 Janus kinase 1 Homo sapiens 80-84 29452839-4 2018 Compound 6 showed improved selectivity for JAK1 compared to that of tofacitinib (IC50 11, 2.4 x 102, 2.8 x 103, and 1.1 x 102 nM for JAK1, JAK2, JAK3, and TYK2, respectively). tofacitinib 68-79 Janus kinase 1 Homo sapiens 133-137 29522138-2 2018 Thrombocytopenia is a poor prognostic feature and limits use of Janus kinase 1 (JAK1)/Janus kinase 2 (JAK2) inhibitor ruxolitinib. ruxolitinib 118-129 Janus kinase 1 Homo sapiens 64-78 29687421-1 2018 Baricitinib (Olumiant ) is an oral, targeted synthetic DMARD that inhibits JAK1 and JAK2, which are implicated in the pathogenesis of rheumatoid arthritis (RA). baricitinib 0-11 Janus kinase 1 Homo sapiens 75-79 29351986-0 2018 A phase II study of the oral JAK1/JAK2 inhibitor ruxolitinib in advanced relapsed/refractory Hodgkin lymphoma. ruxolitinib 49-60 Janus kinase 1 Homo sapiens 29-33 29351986-3 2018 In this phase II study we assessed the safety and efficacy of ruxolitinib, an oral JAK1/2 inhibitor, in patients with relapsed/refractory Hodgkin lymphoma. ruxolitinib 62-73 Janus kinase 1 Homo sapiens 83-89 29731870-6 2018 Furthermore, piceatannol (a JAK1 inhibitor) or small interfering RNA against STAT3 reduced the extent of the increased expression of MMP-11 induced by IGF-1 in SGC-7901 cells. 3,3',4,5'-tetrahydroxystilbene 13-24 Janus kinase 1 Homo sapiens 28-32 29731870-7 2018 Piceatannol treatment induced the dose-dependent decline in the enhancement of STAT3 phosphorylation induced by IGF-1, indicating that the JAK1/STAT3 pathway may be implicated in the elevated expression of MMP-11 induced by IGF-1 in SGC-7901 cells. 3,3',4,5'-tetrahydroxystilbene 0-11 Janus kinase 1 Homo sapiens 139-143 29750040-2 2018 This Phase Ib study evaluated ruxolitinib, a potent JAK1/2 inhibitor, in combination with gemcitabine with or without nab-paclitaxel in patients with advanced solid tumors. ruxolitinib 30-41 Janus kinase 1 Homo sapiens 52-58 29494851-7 2018 These results provided insights into the effects of dasatinib on JAK/STAT signaling in NK cells in vivo and the mechanisms underlying NK cell activation induced by dasatinib therapy. Dasatinib 52-61 Janus kinase 1 Homo sapiens 65-68 29515238-6 2018 Regarding key differences of therapy recommendations, both recombinant interferon alpha and the JAK1/JAK2 inhibitor ruxolitinib are recommended as second-line therapies for PV patients who are intolerant or have inadequate response to hydroxyurea. ruxolitinib 116-127 Janus kinase 1 Homo sapiens 96-100 29515238-6 2018 Regarding key differences of therapy recommendations, both recombinant interferon alpha and the JAK1/JAK2 inhibitor ruxolitinib are recommended as second-line therapies for PV patients who are intolerant or have inadequate response to hydroxyurea. Hydroxyurea 235-246 Janus kinase 1 Homo sapiens 96-100 29805309-8 2018 Here, we show that liver cancer cells also exhibit heterogeneous sensitivities to sorafenib induced cell death, which co-relates with the STAT3-Y705 phosphorylation levels and JAK1/2 expression levels in Hep3B, Huh7 and HepG2 cells. Sorafenib 82-91 Janus kinase 1 Homo sapiens 176-182 29805309-10 2018 Finally, both inhibitors of STAT3 SH2 domain (S3i-201) or STAT3 upstream kinases JAKs (JAK inhibitor I) could synergistically enhance sorafenib induced cell death. Sorafenib 134-143 Janus kinase 1 Homo sapiens 81-85 29666307-6 2018 IL-2-JAK1/3 signaling pathways thus increased the abundance of nutrient transporters, nutrient sensors, and critical oxygen-sensing molecules. Oxygen 117-123 Janus kinase 1 Homo sapiens 5-9 29235894-2 2018 A few years ago, the first-in-class JAK1/JAK2 inhibitor ruxolitinib, demonstrated reductions in both constitutional symptoms and splenomegaly, leading to the US FDA approval. ruxolitinib 56-67 Janus kinase 1 Homo sapiens 36-40 29266308-0 2018 The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF-06700841) in Healthy Subjects and Patients With Plaque Psoriasis. pyrazofurin 91-93 Janus kinase 1 Homo sapiens 75-79 29436642-1 2018 The Janus kinase (JAK)1 and JAK2 inhibitor, ruxolitinib, and the active form of vitamin D (calcitriol) were previously reported to possess anticancer effects in breast cancer. Calcitriol 91-101 Janus kinase 1 Homo sapiens 4-23 29263442-0 2018 Long-term efficacy and safety of momelotinib, a JAK1 and JAK2 inhibitor, for the treatment of myelofibrosis. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 33-44 Janus kinase 1 Homo sapiens 48-52 28969943-7 2018 The Jak 1/2 inhibitor ruxolitinib, the mTOR inhibitor rapamycin and the PI3 kinase inhibitor LY294002 all prevented the potentiation of cell death by IL-13. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 4-11 29566740-0 2018 Effect of filgotinib, a selective JAK 1 inhibitor, with and without methotrexate in patients with rheumatoid arthritis: patient-reported outcomes. GLPG0634 10-20 Janus kinase 1 Homo sapiens 34-39 29544547-2 2018 The oral Janus kinase (JAK) 1/JAK2 inhibitor ruxolitinib has been shown to improve splenomegaly, symptom burden, and overall survival in patients with intermediate-2 or high-risk MF compared with placebo or best available therapy (BAT). ruxolitinib 45-56 Janus kinase 1 Homo sapiens 9-29 29189896-1 2018 Ruxolitinib is a JAK1/2 inhibitor that is effective in managing symptoms and splenomegaly related to myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-23 29480036-7 2018 Ruxolitinib, a potent oral JAK1/JAK2 inhibitor remains the only Food and Drug Administration (FDA)-approved medicinal therapy for the treatment of MF. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 27-31 29311136-1 2018 Momelotinib (MMB), a small-molecule inhibitor of Janus kinase (JAK)1/2 and of activin A receptor type 1 (ACVR1), is in clinical development for the treatment of myeloproliferative neoplasms. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 49-70 29311136-1 2018 Momelotinib (MMB), a small-molecule inhibitor of Janus kinase (JAK)1/2 and of activin A receptor type 1 (ACVR1), is in clinical development for the treatment of myeloproliferative neoplasms. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 13-16 Janus kinase 1 Homo sapiens 49-70 29311136-7 2018 The major circulating human metabolite, M21 (a morpholino lactam), is a potent inhibitor of JAK1/2 and ACVR1 in vitro. morpholino lactam 47-64 Janus kinase 1 Homo sapiens 92-98 29298069-0 2018 Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. Abrocitinib 18-105 Janus kinase 1 Homo sapiens 133-137 29471605-9 2018 Tofacitinib is an oral, small molecule that inhibits JAK1, JAK3 and in a lesser extent, JAK2. tofacitinib 0-11 Janus kinase 1 Homo sapiens 53-57 29472557-2 2018 The lack of complete response in most patients treated with the JAK1/2 inhibitor ruxolitinib indicates the need for identifying novel therapeutic strategies. ruxolitinib 81-92 Janus kinase 1 Homo sapiens 64-70 29298069-0 2018 Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. Abrocitinib 107-118 Janus kinase 1 Homo sapiens 133-137 29298069-4 2018 Through modification of the 3-aminopiperidine linker in tofacitinib, we discovered highly selective JAK1 inhibitors with nanomolar potency in a human whole blood assay. Piperidin-3-amine 28-45 Janus kinase 1 Homo sapiens 100-104 29298069-4 2018 Through modification of the 3-aminopiperidine linker in tofacitinib, we discovered highly selective JAK1 inhibitors with nanomolar potency in a human whole blood assay. tofacitinib 56-67 Janus kinase 1 Homo sapiens 100-104 29056075-0 2018 An updated review of the JAK1/2 inhibitor (ruxolitinib) in the Philadelphia-negative myeloproliferative neoplasms. ruxolitinib 43-54 Janus kinase 1 Homo sapiens 25-31 29162613-3 2018 In the present study, we investigated whether ruxolitinib, a small drug acting as a JAK1/2 inhibitor and currently used in the treatment of myeloproliferative neoplasms, may also counteract the repressing effects of IL-6 toward hepatic detoxifying systems. ruxolitinib 46-57 Janus kinase 1 Homo sapiens 84-90 28956263-1 2018 Ruxolitinib, a potent JAK1/JAK2 inhibitor, was found to be superior to the best available therapy (BAT) in controlling hematocrit, reducing splenomegaly, and improving symptoms in the phase 3 RESPONSE study of patients with polycythemia vera with splenomegaly who experienced an inadequate response to or adverse effects from hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-26 29128627-0 2018 Inhibition of JAK1 by microRNA-708 promotes SH-SY5Y neuronal cell survival after oxygen and glucose deprivation and reoxygenation. Oxygen 81-87 Janus kinase 1 Homo sapiens 14-18 29399328-6 2018 Ten years after the beginning of clinical trials, only two drugs have been approved by the US Food and Drug Administration: one JAK2/JAK1 inhibitor (ruxolitinib) in intermediate-2 and high-risk myelofibrosis and hydroxyurea-resistant or -intolerant polycythemia vera and one JAK1/JAK3 inhibitor (tofacitinib) in methotrexate-resistant rheumatoid arthritis. ruxolitinib 149-160 Janus kinase 1 Homo sapiens 133-137 29127481-2 2018 Once the JAKs are activated, a cascade of further signaling events is triggered involving phosphorylation of selected receptor chain tyrosines, binding of signal transducer and activator of transcription (STAT) proteins and phosphorylation of these STATs. Tyrosine 133-142 Janus kinase 1 Homo sapiens 9-13 29741513-5 2018 Considerable advancements have been made in the understanding of MPN pathogenesis, in particular recognition of the driver mutations JAK2 V617F, CALR, and MPL, which has led to the development of ruxolitinib, an inhibitor of Janus kinase 1 (JAK1) and JAK2 that has transformed therapy for myelofibrosis. ruxolitinib 196-207 Janus kinase 1 Homo sapiens 225-239 29741513-5 2018 Considerable advancements have been made in the understanding of MPN pathogenesis, in particular recognition of the driver mutations JAK2 V617F, CALR, and MPL, which has led to the development of ruxolitinib, an inhibitor of Janus kinase 1 (JAK1) and JAK2 that has transformed therapy for myelofibrosis. ruxolitinib 196-207 Janus kinase 1 Homo sapiens 241-245 29162613-0 2018 The JAK1/2 Inhibitor Ruxolitinib Reverses Interleukin-6-Mediated Suppression of Drug-Detoxifying Proteins in Cultured Human Hepatocytes. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 29849942-5 2018 We investigated the therapeutic potential of ruxolitinib, a JAK1/JAK2 inhibitor that has been FDA-approved for the treatment of myelofibrosis, to treat ovarian cancer either alone or in combination with conventional chemotherapy agents. ruxolitinib 45-56 Janus kinase 1 Homo sapiens 60-64 29056075-1 2018 Ruxolitinib (Rux), a JAK1/2 inhibitor, has been approved for patients with myelofibrosis and in polycythemia vera with inadequate response/intolerance to hydroxycarbamide. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-27 29056075-1 2018 Ruxolitinib (Rux), a JAK1/2 inhibitor, has been approved for patients with myelofibrosis and in polycythemia vera with inadequate response/intolerance to hydroxycarbamide. ruxolitinib 0-3 Janus kinase 1 Homo sapiens 21-27 29202299-0 2018 Repression of interferon beta-regulated cytokines by the JAK1/2 inhibitor ruxolitinib in inflammatory human macrophages. ruxolitinib 74-85 Janus kinase 1 Homo sapiens 57-63 29202299-1 2018 Ruxolitinib is a Janus kinase (JAK) 1/2 inhibitor, currently used in the treatment of myeloproliferative neoplasms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-39 30079384-9 2018 We present an index case of a patient with T-PLL with a clonal JAK1 V658F mutation that responded to ruxolitinib therapy. ruxolitinib 101-112 Janus kinase 1 Homo sapiens 63-67 28986762-1 2018 Ruxolitinib, a potent JAK1/JAK2 inhibitor, improved splenomegaly and myelofibrosis-associated symptoms and prolonged survival compared with placebo and best available therapy in the phase 3 COMFORT studies. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-26 29214116-1 2017 Background: Ruxolitinib is a potent inhibitor of JAK1/2 with proven efficacy in myelofibrosis. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 49-53 30069628-1 2018 Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of Janus kinase (JAK) 1 and JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 97-117 30069628-1 2018 Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of Janus kinase (JAK) 1 and JAK2. ruxolitinib 31-41 Janus kinase 1 Homo sapiens 97-117 30069628-1 2018 Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of Janus kinase (JAK) 1 and JAK2. ruxolitinib 45-51 Janus kinase 1 Homo sapiens 97-117 29042365-2 2017 Current treatment options for MPNs include cytoreduction by hydroxyurea and JAK1/2 inhibition by ruxolitinib, both of which are not curative. ruxolitinib 97-108 Janus kinase 1 Homo sapiens 76-82 29139090-1 2017 Tofacitinib (Xeljanz ) is a potent, selective JAK inhibitor that preferentially inhibits Janus kinase (JAK) 1 and JAK3. tofacitinib 0-11 Janus kinase 1 Homo sapiens 89-109 28891251-1 2017 Baricitinib is an oral inhibitor of Janus kinases (JAKs), selective for JAK1 and 2. baricitinib 0-11 Janus kinase 1 Homo sapiens 51-55 28891251-1 2017 Baricitinib is an oral inhibitor of Janus kinases (JAKs), selective for JAK1 and 2. baricitinib 0-11 Janus kinase 1 Homo sapiens 72-82 29098608-4 2017 The only approved therapy for MF, JAK1/2 inhibitor ruxolitinib, can ameliorate splenomegaly, improve symptoms, and prolong survival in some patients. ruxolitinib 51-62 Janus kinase 1 Homo sapiens 34-38 29139090-1 2017 Tofacitinib (Xeljanz ) is a potent, selective JAK inhibitor that preferentially inhibits Janus kinase (JAK) 1 and JAK3. tofacitinib 13-20 Janus kinase 1 Homo sapiens 89-109 29074595-3 2017 MAJIC (ISRCTN61925716) is a randomized phase 2 trial of ruxolitinib (JAK1/2 inhibitor) vs best available therapy (BAT) in ET and polycythemia vera patients resistant or intolerant to HC. ruxolitinib 56-67 Janus kinase 1 Homo sapiens 69-75 28879797-7 2017 Amorfrutin A also inhibited activation of the upstream kinases Janus-activated kinase 1 (JAK1), JAK2 and Src signaling pathways. amorfrutin A 0-12 Janus kinase 1 Homo sapiens 63-87 28879797-7 2017 Amorfrutin A also inhibited activation of the upstream kinases Janus-activated kinase 1 (JAK1), JAK2 and Src signaling pathways. amorfrutin A 0-12 Janus kinase 1 Homo sapiens 89-93 28722170-9 2017 This effect was inhibited by the JAK1/2 inhibitor of the JAK/STAT3 pathway ruxolitinib. ruxolitinib 75-86 Janus kinase 1 Homo sapiens 33-39 28757617-5 2017 Nilotinib also suppressed endothelial cell proliferation, migration and tube-formation and bound to a distinct set of target-kinases, relevant to angiogenesis and atherosclerosis, including angiopoietin receptor-1 TEK, ABL-2, JAK1 and MAP-kinases. nilotinib 0-9 Janus kinase 1 Homo sapiens 226-230 28484265-7 2017 The combination of the GC dexamethasone and the JAK1/2 inhibitor ruxolitinib altered the balance between pro- and anti-apoptotic factors in samples with IL7-dependent GC resistance, but not in samples with IL7-independent GC resistance. ruxolitinib 65-76 Janus kinase 1 Homo sapiens 48-54 28994166-11 2017 Ruxolitinib is a selective inhibitor of JAK1 and JAK2 kinases and the JAK-STAT signaling pathway. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 40-44 28960447-4 2017 AZD1480 and CYT387 are novel JAK1/2 inhibitors that have been used in clinical trials for treating various hematologic cancers in humans. AZD 1480 0-7 Janus kinase 1 Homo sapiens 29-35 28960447-4 2017 AZD1480 and CYT387 are novel JAK1/2 inhibitors that have been used in clinical trials for treating various hematologic cancers in humans. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 12-18 Janus kinase 1 Homo sapiens 29-35 29228628-7 2017 Luminespib decreased the phosphorylation of mutant STAT3 at Y705, whereas JAK1/JAK2 inhibitor ruxolitinib had reduced efficacy on mutant STAT3 phosphorylation. ruxolitinib 94-105 Janus kinase 1 Homo sapiens 74-78 28838249-5 2017 Here we review the pharmacology and clinical trial data for efficacy and safety of filgotinib, an investigational selective JAK1 inhibitor. GLPG0634 83-93 Janus kinase 1 Homo sapiens 124-128 28953386-4 2017 A preferred pyrazole substituted pyrrolopyrimidine, 24, inhibits JAK1 and HDACs 1, 2, 3, 6, and 10 with IC50 values of less than 20 nM, is <100 nM potent against JAK2 and HDAC11, and is selective for the JAK family against a panel of 97 kinases. pyrazole 12-20 Janus kinase 1 Homo sapiens 65-69 28953386-4 2017 A preferred pyrazole substituted pyrrolopyrimidine, 24, inhibits JAK1 and HDACs 1, 2, 3, 6, and 10 with IC50 values of less than 20 nM, is <100 nM potent against JAK2 and HDAC11, and is selective for the JAK family against a panel of 97 kinases. pyrrolopyrimidine 33-50 Janus kinase 1 Homo sapiens 65-69 28622463-0 2017 Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Filgotinib, a Selective JAK-1 Inhibitor, After Short-Term Treatment of Rheumatoid Arthritis: Results of Two Randomized Phase IIa Trials. GLPG0634 60-70 Janus kinase 1 Homo sapiens 84-89 28622463-14 2017 CONCLUSION: Selective inhibition of JAK-1 with filgotinib shows initial efficacy in RA with an encouraging safety profile in these exploratory studies. GLPG0634 47-57 Janus kinase 1 Homo sapiens 36-41 28277287-3 2017 The discovery of a JAK2 point mutation (JAK2 V617F) as the main cause of polycythemia vera lead to the development and FDA approval of a JAK1/2 inhibitor, ruxolitinib, in 2011. ruxolitinib 155-166 Janus kinase 1 Homo sapiens 137-143 28953386-3 2017 Herein the core features of ruxolitinib (1), a marketed JAK1/2 inhibitor, have been merged with the HDAC inhibitor vorinostat (2), leading to new molecules that are bispecific targeted JAK/HDAC inhibitors. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 56-62 29262601-2 2017 Ruxolitinib is a pyrrolo[2.3-d]pyrimidine derivative with inhibitory activity against JAK1 and JAK2, moderate activity against TYK2, and minor activity against JAK3. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 86-90 29262601-2 2017 Ruxolitinib is a pyrrolo[2.3-d]pyrimidine derivative with inhibitory activity against JAK1 and JAK2, moderate activity against TYK2, and minor activity against JAK3. Pyrrolo(2,3-d)pyrimidine 17-41 Janus kinase 1 Homo sapiens 86-90 29085766-4 2017 These descriptors correlate with the anti-RA activity with R2 values for JAK3, JAK2 and JAK1 are 0.9811, 0.8620 and 0.9740, respectively. Radium 42-44 Janus kinase 1 Homo sapiens 88-92 28503781-0 2017 Assessment of effect of CYP3A inhibition, CYP induction, OATP1B inhibition, and high-fat meal on pharmacokinetics of the JAK1 inhibitor upadacitinib. upadacitinib 136-148 Janus kinase 1 Homo sapiens 121-125 29025600-3 2017 Furthermore, we show that primary ALL mononuclear cells harboring the JAK2 R938Q mutation display reduced sensitivity to the JAK1/2 ATP-competitive inhibitor ruxolitinib in vitro, compared to ALL cells that carry a more common JAK2 pseudokinase domain mutation. Adenosine Triphosphate 132-135 Janus kinase 1 Homo sapiens 125-131 29025600-3 2017 Furthermore, we show that primary ALL mononuclear cells harboring the JAK2 R938Q mutation display reduced sensitivity to the JAK1/2 ATP-competitive inhibitor ruxolitinib in vitro, compared to ALL cells that carry a more common JAK2 pseudokinase domain mutation. ruxolitinib 158-169 Janus kinase 1 Homo sapiens 125-131 28829236-1 2017 INTRODUCTION: Tofacitinib is a pan JAK inhibitor with specificity for JAK3 over JAK1 over JAK2, which is approved in many countries for the treatment of rheumatoid arthritis (RA), including the United States and the European Union, either as monotherapy or in combination with conventional synthetic disease modifying anti-arthritis drugs (csDMARDs). tofacitinib 14-25 Janus kinase 1 Homo sapiens 80-84 28838249-7 2017 Expert opinion: The selectivity of filgotinib for JAK1 may have theoretical advantages in terms of limiting toxicity. GLPG0634 35-45 Janus kinase 1 Homo sapiens 50-54 28729401-9 2017 The selective JAK1 inhibitor filgotinib effectively suppressed STAT3 activation and OSMR expression, and cotargeting inhibition of the oncogenic pathway and JAK1 reversed resistance to targeted drugs. GLPG0634 29-39 Janus kinase 1 Homo sapiens 14-18 28823882-4 2017 OBJECTIVE: To evaluate the efficacy of the JAK 1/3 inhibitor tofacitinib in the treatment of vitiligo. tofacitinib 61-72 Janus kinase 1 Homo sapiens 43-48 28962635-2 2017 This analysis evaluated the long-term survival benefit with ruxolitinib, a Janus kinase (JAK)1/JAK2 inhibitor, in patients with intermediate-2 (int-2) or high-risk MF. ruxolitinib 60-71 Janus kinase 1 Homo sapiens 75-94 29051788-12 2017 For example, the JAK1 blocker filgotinib was tested in Crohn"s disease, whereas the JAK1/3 inhibitor tofacitinib was tested in clinical trials for both Crohn"s disease and ulcerative colitis. tofacitinib 101-112 Janus kinase 1 Homo sapiens 84-88 28794380-2 2017 We herein present the case of a post-polycythemia vera (PV) myelofibrosis patient with massive splenomegaly who developed laboratory TLS after treatment with ruxolitinib, a potent JAK1/JAK2 inhibitor. ruxolitinib 158-169 Janus kinase 1 Homo sapiens 180-184 28737053-5 2017 Expert opinion: Baricitinib is an oral targeted synthetic (ts) disease-modifying antirheumatic drug (DMARD) that mainly inhibits JAK1 and JAK2. baricitinib 16-27 Janus kinase 1 Homo sapiens 129-133 29026328-5 2017 However, the combination of rhIL-6 and ruxolitinib, a JAK1/JAK2-selective inhibitor, was a less effective inhibitor of STAT protein activation. ruxolitinib 39-50 Janus kinase 1 Homo sapiens 54-58 28824063-2 2017 Ruxolitinib (RUXO), a novel JAK1/2 inhibitor, can be used as a bridging therapy until allo-SCT can be performed to reduce TRM. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 28-34 28824063-2 2017 Ruxolitinib (RUXO), a novel JAK1/2 inhibitor, can be used as a bridging therapy until allo-SCT can be performed to reduce TRM. ruxolitinib 13-17 Janus kinase 1 Homo sapiens 28-34 28649004-5 2017 STAT signaling inhibition by the JAK1/2 inhibitor ruxolitinib mimicked MACC1 knockdown-mediated molecular signatures and apoptosis sensitization to Fas activation. ruxolitinib 50-61 Janus kinase 1 Homo sapiens 33-39 28656237-0 2017 Matrine increases the inhibitory effects of afatinib on H1975 cells via the IL-6/JAK1/STAT3 signaling pathway. Afatinib 44-52 Janus kinase 1 Homo sapiens 81-85 28684419-6 2017 Enhancement is accompanied by an increase in signal transducer and activator of transcription 5 (STAT5) phosphorylation and is abrogated by treatment with C188-9, a STAT3/5 inhibitor, or with ruxolitinib, a Janus kinase 1/2 (JAK1/2) inhibitor. C188-9 155-161 Janus kinase 1 Homo sapiens 225-231 28684419-6 2017 Enhancement is accompanied by an increase in signal transducer and activator of transcription 5 (STAT5) phosphorylation and is abrogated by treatment with C188-9, a STAT3/5 inhibitor, or with ruxolitinib, a Janus kinase 1/2 (JAK1/2) inhibitor. ruxolitinib 192-203 Janus kinase 1 Homo sapiens 225-231 28622623-0 2017 A phase 2 study of momelotinib, a potent JAK1 and JAK2 inhibitor, in patients with polycythemia vera or essential thrombocythemia. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 19-30 Janus kinase 1 Homo sapiens 41-45 28622623-1 2017 Momelotinib is a potent inhibitor of JAK1 and JAK2 that demonstrated efficacy in patients with primary and secondary myelofibrosis. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 37-41 28619982-8 2017 Moreover, the JAK1/2 inhibitor ruxolitinib restored sensitivity to the BCL2 inhibitor venetoclax in AML patient cells ex vivo in different model systems and in vivo in an AML xenograft mouse model. ruxolitinib 31-42 Janus kinase 1 Homo sapiens 14-20 29296813-6 2017 In vitro screening using a panel of tyrosine kinase inhibitors against 14 different kinase alterations identified the ABL1-inhibitor, dasatinib, as a potent inhibitor of ABL-class fusions (ABL1, ABL2, CSF1R, PDGFRB), whereas the JAK1/JAK2 inhibitor ruxolitinib, was most effective against JAK-STAT-activating alterations (JAK1, JAK2, JAK3, IL7R, IL2RB), but not TYK2. Dasatinib 134-143 Janus kinase 1 Homo sapiens 229-233 29296813-6 2017 In vitro screening using a panel of tyrosine kinase inhibitors against 14 different kinase alterations identified the ABL1-inhibitor, dasatinib, as a potent inhibitor of ABL-class fusions (ABL1, ABL2, CSF1R, PDGFRB), whereas the JAK1/JAK2 inhibitor ruxolitinib, was most effective against JAK-STAT-activating alterations (JAK1, JAK2, JAK3, IL7R, IL2RB), but not TYK2. Dasatinib 134-143 Janus kinase 1 Homo sapiens 322-326 28619982-8 2017 Moreover, the JAK1/2 inhibitor ruxolitinib restored sensitivity to the BCL2 inhibitor venetoclax in AML patient cells ex vivo in different model systems and in vivo in an AML xenograft mouse model. venetoclax 86-96 Janus kinase 1 Homo sapiens 14-20 28550731-8 2017 In addition, xanthotoxin significantly reduced the phosphorylation at signal transducers and activators of transcription 1 (STAT1, Ser 727 and Tyr 701) and STAT3 (Tyr 705), as well as Janus kinase (JAK) 1 and 2 in LPS-induced RAW 264.7 macrophages. Methoxsalen 13-24 Janus kinase 1 Homo sapiens 184-210 28790099-0 2017 GSK2586184, a JAK1 selective inhibitor, in two patients with ulcerative colitis. GSK2586184 0-10 Janus kinase 1 Homo sapiens 14-18 28790099-2 2017 Tofacitinib inhibits cytokine signalling through blockade of JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2). tofacitinib 0-11 Janus kinase 1 Homo sapiens 61-65 28790099-7 2017 The JAK1 selective inhibitor GSK2586184 was well tolerated and induced clinical and endoscopic response in two patients with moderate-to-severe UC. GSK2586184 29-39 Janus kinase 1 Homo sapiens 4-8 28478401-9 2017 Treatment with combined JAK1/JAK2 inhibitors or with JAK2 inhibitors in combination with HSP90 inhibitors was more effective than monotherapy with JAK2 inhibitors in bleomycin-induced pulmonary fibrosis and in adTBR-induced dermal fibrosis. Bleomycin 166-175 Janus kinase 1 Homo sapiens 24-28 28478401-9 2017 Treatment with combined JAK1/JAK2 inhibitors or with JAK2 inhibitors in combination with HSP90 inhibitors was more effective than monotherapy with JAK2 inhibitors in bleomycin-induced pulmonary fibrosis and in adTBR-induced dermal fibrosis. adtbr 210-215 Janus kinase 1 Homo sapiens 24-28 28853089-0 2017 Role of JAK1, JAK2, and JAK3 in Functional Stimulation of Mesenchymal Precursor Cells by Alkaloid Songorine. Alkaloids 89-97 Janus kinase 1 Homo sapiens 8-12 28382662-6 2017 The oral JAK1/JAK3 inhibitor, tofacitinib, is currently approved for rheumatoid arthritis and is in clinical trials for other chronic inflammatory disorders. tofacitinib 30-41 Janus kinase 1 Homo sapiens 9-13 28673391-4 2017 The Food and Drug Administration approved the JAK1/JAK2 inhibitor, ruxolitinib, for the treatment of myelofibrosis and polycythemia vera. ruxolitinib 67-78 Janus kinase 1 Homo sapiens 46-50 28039266-8 2017 Transient blockade of CD11b+ cell expansion using a JAK 1/2 Inhibitor (AZD1480) impaired mobilization of these cells and was associated with a reduction in tumor volume, maintenance of a low-grade tumor phenotype, and prolongation in survival.Conclusions: We demonstrate that impaired recruitment of CD11b+ myeloid cells with a JAK1/2 inhibitor inhibits glioma progression in vivo and prolongs survival in a murine glioma model. AZD 1480 71-78 Janus kinase 1 Homo sapiens 52-59 28322434-2 2017 A 2014 study implicated the JAK1/JAK2 inhibitor, ruxolitinib in short-term treatment of alopecia, however little information exists about the long-term use in otherwise healthy individuals in the community setting. ruxolitinib 49-60 Janus kinase 1 Homo sapiens 28-32 28721333-1 2017 We present the case of a 79-year-old man who showed multiple pulmonary nodules on chest computed tomography (CT) after being treated for 6 months with ruxolitinib, an inhibitor of Janus kinase (JAK) 1 and 2, to treat primary myelofibrosis. ruxolitinib 151-162 Janus kinase 1 Homo sapiens 180-206 28760302-1 2017 The unprecedented success of the Janus kinase (JAK) 1/2 inhibitor ruxolitinib in myelofibrosis (MF) provided much-needed impetus for clinical drug development for the Philadelphia chromosome-negative myeloproliferative neoplasms. ruxolitinib 66-77 Janus kinase 1 Homo sapiens 33-53 28677798-10 2017 In addition, JAK1 knockdown showed similar effects of miR-448 on the metastasis of PDAC cells. pdac 83-87 Janus kinase 1 Homo sapiens 13-17 28677798-12 2017 Taken together, these findings suggest that miR-448 functions as a tumor suppressor in the development of PDAC through targeting the JAK1/STAT3 pathway. pdac 106-110 Janus kinase 1 Homo sapiens 133-137 28500170-1 2017 Since its approval in 2011, the Janus kinase 1/2 (JAK1/2) inhibitor ruxolitinib has evolved to become the centerpiece of therapy for myelofibrosis (MF), and its use in patients with hydroxyurea resistant or intolerant polycythemia vera (PV) is steadily increasing. ruxolitinib 68-79 Janus kinase 1 Homo sapiens 50-56 28158411-8 2017 GSK2586184, a Janus kinase 1 selective inhibitor, induced clinical and endoscopic response in ulcerative colitis; however, the study was discontinued at an early stage due to liver toxicity observed in systemic lupus patients receiving the drug. GSK2586184 0-10 Janus kinase 1 Homo sapiens 14-28 28158411-9 2017 Filgotinib, a Janus kinase 1 selective inhibitor investigated in treatment of Crohn"s disease, was superior to placebo. GLPG0634 0-10 Janus kinase 1 Homo sapiens 14-28 28039266-8 2017 Transient blockade of CD11b+ cell expansion using a JAK 1/2 Inhibitor (AZD1480) impaired mobilization of these cells and was associated with a reduction in tumor volume, maintenance of a low-grade tumor phenotype, and prolongation in survival.Conclusions: We demonstrate that impaired recruitment of CD11b+ myeloid cells with a JAK1/2 inhibitor inhibits glioma progression in vivo and prolongs survival in a murine glioma model. AZD 1480 71-78 Janus kinase 1 Homo sapiens 328-334 27993828-0 2017 Filgotinib (GLPG0634/GS-6034), an oral selective JAK1 inhibitor, is effective as monotherapy in patients with active rheumatoid arthritis: results from a randomised, dose-finding study (DARWIN 2). GLPG0634 0-10 Janus kinase 1 Homo sapiens 49-53 27993828-1 2017 OBJECTIVES: To evaluate the efficacy and safety of different doses of filgotinib, an oral Janus kinase 1 inhibitor, as monotherapy in patients with active rheumatoid arthritis (RA) and previous inadequate response to methotrexate (MTX). GLPG0634 70-80 Janus kinase 1 Homo sapiens 90-104 27993829-0 2017 Filgotinib (GLPG0634/GS-6034), an oral JAK1 selective inhibitor, is effective in combination with methotrexate (MTX) in patients with active rheumatoid arthritis and insufficient response to MTX: results from a randomised, dose-finding study (DARWIN 1). GLPG0634 0-10 Janus kinase 1 Homo sapiens 39-43 27993829-1 2017 OBJECTIVES: To evaluate the efficacy and safety of different doses and regimens of filgotinib, an oral Janus kinase 1 inhibitor, as add-on treatment to methotrexate (MTX) in patients with active rheumatoid arthritis (RA) and inadequate response to MTX. GLPG0634 83-93 Janus kinase 1 Homo sapiens 103-117 28410228-5 2017 Moreover, a high sensitivity to the JAK1/2 inhibitor ruxolitinib was observed in S646P mutant model. ruxolitinib 53-64 Janus kinase 1 Homo sapiens 36-42 28441920-4 2017 NS-018 and INCB039110, selective inhibitors of JAK2 and JAK1, respectively, are also discussed. NS-018 0-6 Janus kinase 1 Homo sapiens 56-60 28441920-4 2017 NS-018 and INCB039110, selective inhibitors of JAK2 and JAK1, respectively, are also discussed. INCB039110 11-21 Janus kinase 1 Homo sapiens 56-60 28302714-0 2017 Ruxolitinib, a potent JAK1/JAK2 inhibitor, induces temporary reductions in the allelic burden of concurrent CSF3R mutations in chronic neutrophilic leukemia. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-26 28318222-2 2017 Here, we report that not only is PF-956980 a pan-JAK ATP-competitive inhibitor but it also causes selective reduction of endogenous JAK2 and JAK3 protein levels in human primary immune cells (in a time-dependent manner), leaving the other JAK family members (JAK1 and TYK2) unchanged. pyrazofurin 33-35 Janus kinase 1 Homo sapiens 259-263 29228564-1 2017 Inhibition of the constitutively activated JAK/STAT pathway in JAK2V617F mutated cells by the JAK1/JAK2 inhibitor ruxolitinib resulted in clinical benefits in patients with myeloproliferative neoplasms. ruxolitinib 114-125 Janus kinase 1 Homo sapiens 43-46 29228564-1 2017 Inhibition of the constitutively activated JAK/STAT pathway in JAK2V617F mutated cells by the JAK1/JAK2 inhibitor ruxolitinib resulted in clinical benefits in patients with myeloproliferative neoplasms. ruxolitinib 114-125 Janus kinase 1 Homo sapiens 94-98 28332364-9 2017 Moreover, the expressions of STAT1, JAK1, and c-Met in H460 cells were decreased by SIM-89 treatment, and c-Met phosphorylation was suppressed in A549, H441, H1299, and B16F10 cells by the treatment. sim-89 84-90 Janus kinase 1 Homo sapiens 36-40 27889820-1 2017 Ruxolitinib, a JAK1 and JAK2 inhibitor, has been tested and approved for the treatment of primary and secondary myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-19 27740634-2 2017 Ruxolitinib is an oral Janus-activated kinase 1 (JAK1)/JAK2 inhibitor approved for the treatment of patients with myelofibrosis based on the results of two randomized clinical trials. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 23-47 27740634-2 2017 Ruxolitinib is an oral Janus-activated kinase 1 (JAK1)/JAK2 inhibitor approved for the treatment of patients with myelofibrosis based on the results of two randomized clinical trials. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 49-53 27458171-4 2017 Capz also inhibited activation of the upstream kinases JAK1/2 and c-Src. capsazepine 0-4 Janus kinase 1 Homo sapiens 55-61 28356514-12 2017 Finally, ruxolitinib, a JAK1/2 inhibitor, was effective in vivo in a xenograft ALK- ALCL model. ruxolitinib 9-20 Janus kinase 1 Homo sapiens 24-30 28053127-7 2017 Suppression of JAK1/2 by ruxolitinib prevented STAT3-mediated transcription of ZEB1, SNAI1 and OSMR, as well as the emergence of a mesenchymal/CSC phenotype. ruxolitinib 25-36 Janus kinase 1 Homo sapiens 15-21 28188131-2 2017 Results from a phase 2 study for the treatment of MF with the Janus kinase 1/2 (JAK1/2) inhibitor momelotinib (MMB) demonstrated that MMB treatment ameliorated anemia, which was unexpected for a JAK1/2 inhibitor, because erythropoietin-mediated JAK2 signaling is essential for erythropoiesis. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 98-109 Janus kinase 1 Homo sapiens 80-86 28188131-2 2017 Results from a phase 2 study for the treatment of MF with the Janus kinase 1/2 (JAK1/2) inhibitor momelotinib (MMB) demonstrated that MMB treatment ameliorated anemia, which was unexpected for a JAK1/2 inhibitor, because erythropoietin-mediated JAK2 signaling is essential for erythropoiesis. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 111-114 Janus kinase 1 Homo sapiens 80-86 28188131-2 2017 Results from a phase 2 study for the treatment of MF with the Janus kinase 1/2 (JAK1/2) inhibitor momelotinib (MMB) demonstrated that MMB treatment ameliorated anemia, which was unexpected for a JAK1/2 inhibitor, because erythropoietin-mediated JAK2 signaling is essential for erythropoiesis. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 134-137 Janus kinase 1 Homo sapiens 80-86 28579852-3 2017 However, more recently, the discovery of JAK2 mutations has also led to the development of small-molecule JAK1/2 inhibitors, the first of which, ruxolitinib, has been approved for the treatment of MF in the United States and Europe. ruxolitinib 145-156 Janus kinase 1 Homo sapiens 106-112 27723271-1 2017 OBJECTIVE: We undertook this phase III study to evaluate baricitinib, an orally administered JAK-1/JAK-2 inhibitor, as monotherapy or combined with methotrexate (MTX) compared to MTX monotherapy in patients with active rheumatoid arthritis (RA) who had received no or minimal conventional synthetic disease-modifying antirheumatic drugs (DMARDs) and who were naive to biologic DMARDs. baricitinib 57-68 Janus kinase 1 Homo sapiens 93-98 27832516-1 2017 Ruxolitinib is a potent JAK1/JAK2 inhibitor that has demonstrated durable improvements in splenomegaly, symptoms, and overall survival in controlled clinical trials in patients with myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 24-28 28028027-1 2017 There has been a major revolution in the management of patients with myeloproliferative neoplasms (MPN), and in particular those with myelofibrosis and extensive splenomegaly and symptomatic burden, after the introduction of the JAK1 and JAK2 inhibitor ruxolitinib. ruxolitinib 253-264 Janus kinase 1 Homo sapiens 229-233 28260257-1 2017 Ruxolitinib is a dual janus kinase 1 (JAK1)/JAK2 inhibitor used to treat splenomegaly and symptoms associated with myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-36 28260257-1 2017 Ruxolitinib is a dual janus kinase 1 (JAK1)/JAK2 inhibitor used to treat splenomegaly and symptoms associated with myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-42 28228106-1 2017 BACKGROUND: The randomized, double-blind, placebo-controlled, phase 3 COMFORT-I trial evaluated the JAK1/JAK2 inhibitor ruxolitinib in patients with intermediate-2/high-risk myelofibrosis. ruxolitinib 120-131 Janus kinase 1 Homo sapiens 100-104 28199814-1 2017 BACKGROUND: Baricitinib is an oral, reversible inhibitor of the Janus kinases JAK1 and JAK2 that may have therapeutic value in patients with rheumatoid arthritis. baricitinib 12-23 Janus kinase 1 Homo sapiens 78-82 27983880-1 2017 INTRODUCTION: Ruxolitinib is a potent and selective JAK1/JAK2 inhibitor that has shown superiority as compared to available conventional chemotherapies, in terms of reduction in splenomegaly and improvement of symptoms and quality of life. ruxolitinib 14-25 Janus kinase 1 Homo sapiens 52-56 27785927-0 2017 Momelotinib in myelofibrosis: JAK1/2 inhibitor with a role in treating and understanding the anemia. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 30-36 27785927-4 2017 The JAK1/2 inhibitor momelotinib unexpectedly resulted in reduction of anemia in MF patients during Phase I/II trials. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 21-32 Janus kinase 1 Homo sapiens 4-10 27930945-2 2017 Ruxolitinib, an oral JAK1/2 inhibitor, is highly effective in ameliorating systemic symptoms and reducing splenomegaly. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-27 27916398-1 2017 BACKGROUND: In the pivotal RESPONSE study, ruxolitinib, a Janus kinase (JAK)1 and JAK2 inhibitor, was superior to best available therapy at controlling haematocrit and improving splenomegaly and symptoms in patients with polycythaemia vera with splenomegaly who were inadequately controlled with hydroxyurea. ruxolitinib 43-54 Janus kinase 1 Homo sapiens 58-77 27882812-2 2017 Ruxolitinib, a JAK1/2 inhibitor, is currently the only drug approved for the treatment of patients with intermediate or high risk MF. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 26705936-7 2017 MCF-7 cells cocultured with M2 TAM showed activated JAK1/STAT3 and Raf/MEK/JNK pathways contributing to tyrosine and serine phophorylation of STAT3, respectively. tam 31-34 Janus kinase 1 Homo sapiens 52-56 26705936-7 2017 MCF-7 cells cocultured with M2 TAM showed activated JAK1/STAT3 and Raf/MEK/JNK pathways contributing to tyrosine and serine phophorylation of STAT3, respectively. Tyrosine 104-112 Janus kinase 1 Homo sapiens 52-56 28674362-0 2017 The Amelioration of Myelofibrosis with Thrombocytopenia by a JAK1/2 Inhibitor, Ruxolitinib, in a Post-polycythemia Vera Myelofibrosis Patient with a JAK2 Exon 12 Mutation. ruxolitinib 79-90 Janus kinase 1 Homo sapiens 61-67 28674362-3 2017 We describe how treatment with a JAK1/2 inhibitor, ruxolitinib, led to the rapid amelioration of marrow fibrosis, erythrocytosis and thrombocytopenia in a 77-year-old man with post-PV MF who carried a JAK2 exon 12 mutation (JAK2H538QK539L). ruxolitinib 51-62 Janus kinase 1 Homo sapiens 33-39 27988142-1 2017 BACKGROUND: Filgotinib (GLPG0634, GS-6034) is a once-daily, orally administered, Janus kinase 1 (JAK1)-selective inhibitor. GLPG0634 12-22 Janus kinase 1 Homo sapiens 81-95 27988142-1 2017 BACKGROUND: Filgotinib (GLPG0634, GS-6034) is a once-daily, orally administered, Janus kinase 1 (JAK1)-selective inhibitor. GLPG0634 12-22 Janus kinase 1 Homo sapiens 97-101 27923824-9 2017 These results demonstrate that ruxolitinib"s nonselective inhibition of JAK1/2 results in profound NK-cell dysfunction by blocking downstream pSTAT5, hence providing a persuasive rationale for the development of selective JAK2 inhibitors for immunotherapeutic applications. ruxolitinib 31-42 Janus kinase 1 Homo sapiens 72-78 27634203-1 2017 Momelotinib, a small-molecule inhibitor of Janus kinase 1 and Janus kinase 2, has demonstrated efficacy in myelofibrosis patients with 300 mg, once-daily dosing. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 43-57 27286739-3 2016 In this study, we examine the expression of the interleukin-6/Janus kinase/STAT3 (IL-6/JAK/STAT3) pathway components in PA and ca-ex-PA. ca-ex-pa 127-135 Janus kinase 1 Homo sapiens 87-90 27659251-5 2017 Although there is a high sequence homology and structural identity of JAK1 and JAK2, such as a very similar binding mode of inhibitors at the ATPbinding site of enzymes, obvious differences surrounding the JAK1 and JAK2 ATP-binding sites provide a platform for the rational design of JAK2- and JAK1-specific inhibitors. atpbinding 142-152 Janus kinase 1 Homo sapiens 70-74 27659251-5 2017 Although there is a high sequence homology and structural identity of JAK1 and JAK2, such as a very similar binding mode of inhibitors at the ATPbinding site of enzymes, obvious differences surrounding the JAK1 and JAK2 ATP-binding sites provide a platform for the rational design of JAK2- and JAK1-specific inhibitors. Adenosine Triphosphate 142-145 Janus kinase 1 Homo sapiens 70-74 27997540-8 2016 Our analysis revealed that mutations in JAK1 and KRAS, two genes encoding components of the interleukin 7 receptor (IL7R) signaling pathway, were associated with steroid resistance and poor outcome. Steroids 162-169 Janus kinase 1 Homo sapiens 40-44 27997540-13 2016 We found that expressing mutant IL7R, JAK1, or NRAS, or wild-type NRAS or AKT, specifically induced steroid resistance without affecting sensitivity to vincristine or L-asparaginase. Steroids 100-107 Janus kinase 1 Homo sapiens 38-42 27286739-8 2016 CONCLUSION: The IL-6/JAK/STAT3 pathway is overexpressed in PA, and this overexpression was even more pronounced in ca-ex-PA, with a shift in the JAKs mediating STAT3 phosphorylation. ca-ex-pa 115-123 Janus kinase 1 Homo sapiens 21-24 27286739-9 2016 Future studies are needed to clarify whether PA and ca-ex-PA could be treated with targeted therapy directed against components of the IL-6/JAK/STAT3 pathway. ca-ex-pa 52-60 Janus kinase 1 Homo sapiens 140-143 27286739-7 2016 Overexpression of phosphorylated JAK1 (p-JAK1) and cyclin D1 was significantly overexpressed in ductal cells compared with myoepithelial cells in PA. A shift from p-JAK1 to p-JAK2 and p-Tyk2 overexpression was seen between PA and ca-ex-PA, combined with a high p-STAT3 expression in the latter. ca-ex-pa 230-238 Janus kinase 1 Homo sapiens 33-37 27157043-7 2016 In a CMML patient with splenomegaly, who was treated with the JAK1/2 inhibitor ruxolitinib off label, we can demonstrate a spleen response and the disappearance of constitutional symptoms which was associated with a decrease in autonomous CFU-GM formation ex vivo. ruxolitinib 79-90 Janus kinase 1 Homo sapiens 62-68 27389975-0 2016 A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy. upadacitinib 21-28 Janus kinase 1 Homo sapiens 42-47 27389975-1 2016 OBJECTIVE: To compare the efficacy and safety of ABT-494, a novel selective JAK-1 inhibitor, with placebo in patients with moderate-to-severe rheumatoid arthritis (RA) and an inadequate response or intolerance to at least 1 anti-tumor necrosis factor (anti-TNF) agent. upadacitinib 49-56 Janus kinase 1 Homo sapiens 76-81 27390150-0 2016 Efficacy and Safety of ABT-494, a Selective JAK-1 Inhibitor, in a Phase IIb Study in Patients With Rheumatoid Arthritis and an Inadequate Response to Methotrexate. upadacitinib 23-30 Janus kinase 1 Homo sapiens 44-49 27390150-1 2016 OBJECTIVE: To evaluate the efficacy and safety of ABT-494, a selective JAK-1 inhibitor, in patients with moderate-to-severe rheumatoid arthritis (RA) and an inadequate response to methotrexate (MTX). upadacitinib 50-57 Janus kinase 1 Homo sapiens 71-76 27272171-0 2016 Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Subjects with Rheumatoid Arthritis. upadacitinib 45-52 Janus kinase 1 Homo sapiens 72-77 27272171-1 2016 BACKGROUND: ABT-494 is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders, with potential for an improved safety profile compared with non-selective JAK inhibitors. upadacitinib 12-19 Janus kinase 1 Homo sapiens 46-66 27774820-4 2016 Areas covered: Current pharmacologic therapy of MF revolves around the Janus kinase 1/2 (JAK1/2) inhibitor ruxolitinib, which dramatically improves constitutional symptoms and splenomegaly in the majority of patients, and improves overall survival (OS). ruxolitinib 107-118 Janus kinase 1 Homo sapiens 89-95 27579615-4 2016 The JAK1/2 inhibitor ruxolitinib blocked STAT3-phosphorylation and partially improved DEX-mediated killing of stimulated CLL cells in vitro but not in CLL patients in vivo. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 27788604-11 2016 The Z"-LYTE kinase assay showed a reduction in the activities of JAK1, JAK3 and TYK2 by pirfenidone. pirfenidone 89-100 Janus kinase 1 Homo sapiens 66-70 27086927-6 2016 Importantly, Ruxolitinib, a JAK1 inhibitor, could rescue the phenotypic changes induced by miR-23a, -27a and -24 inhibitors. ruxolitinib 13-24 Janus kinase 1 Homo sapiens 28-32 27799566-1 2016 Janus kinases (JAKs) classically signal by activating STAT transcription factors but can also regulate gene expression by epigenetically phosphorylating histone H3 on tyrosine 41 (H3Y41-P). Tyrosine 167-175 Janus kinase 1 Homo sapiens 15-19 27579615-4 2016 The JAK1/2 inhibitor ruxolitinib blocked STAT3-phosphorylation and partially improved DEX-mediated killing of stimulated CLL cells in vitro but not in CLL patients in vivo. Dexamethasone 86-89 Janus kinase 1 Homo sapiens 4-10 27827355-0 2016 Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system. Metals 97-102 Janus kinase 1 Homo sapiens 78-82 27919027-7 2016 Clinically used AMPK activators metformin and salicylate enhanced the inhibitory phosphorylation of endogenous JAK1 and inhibited STAT3 phosphorylation in primary vascular endothelial cells. Metformin 32-41 Janus kinase 1 Homo sapiens 111-115 27919027-7 2016 Clinically used AMPK activators metformin and salicylate enhanced the inhibitory phosphorylation of endogenous JAK1 and inhibited STAT3 phosphorylation in primary vascular endothelial cells. Salicylates 46-56 Janus kinase 1 Homo sapiens 111-115 27827355-1 2016 Crystals of phosphorylated JAK1 kinase domain were initially generated in complex with nucleotide (ADP) and magnesium. Adenosine Diphosphate 99-102 Janus kinase 1 Homo sapiens 27-31 27827355-1 2016 Crystals of phosphorylated JAK1 kinase domain were initially generated in complex with nucleotide (ADP) and magnesium. Magnesium 108-117 Janus kinase 1 Homo sapiens 27-31 27555284-0 2016 The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3. triazole-pyrrolopyrimidine 32-58 Janus kinase 1 Homo sapiens 112-116 27555284-3 2016 We discovered a potent and highly selective inhibitor of JAK2 over JAK1 and -3 based on the structure of 4-(2,5-triazole)-pyrrolopyrimidine. 4-(2,5-triazole)-pyrrolopyrimidine 105-139 Janus kinase 1 Homo sapiens 67-78 27244086-0 2016 Molecular docking, 3D QSAR and dynamics simulation studies of imidazo-pyrrolopyridines as janus kinase 1 (JAK 1) inhibitors. imidazo-pyrrolopyridines 62-86 Janus kinase 1 Homo sapiens 90-104 27577235-9 2016 Results of phase III clinical trials using a JAK1/2 inhibitor, baricitinib, have shown feasible efficacy and tolerable safety. baricitinib 63-74 Janus kinase 1 Homo sapiens 45-51 27577235-11 2016 In addition, clinical phase III trials using filgotinib and ABT-494, specific JAK1 inhibitors, are currently underway. GLPG0634 45-55 Janus kinase 1 Homo sapiens 78-82 27577235-11 2016 In addition, clinical phase III trials using filgotinib and ABT-494, specific JAK1 inhibitors, are currently underway. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 60-63 Janus kinase 1 Homo sapiens 78-82 27690665-4 2016 Areas covered: Several JAK inhibitors such as tofacitinib and baricitinib are oral synthetic DMARD that inhibit JAK1, 2 and 3. tofacitinib 46-57 Janus kinase 1 Homo sapiens 112-125 27690665-4 2016 Areas covered: Several JAK inhibitors such as tofacitinib and baricitinib are oral synthetic DMARD that inhibit JAK1, 2 and 3. baricitinib 62-73 Janus kinase 1 Homo sapiens 112-125 27771575-5 2016 The results have highlighted spirocyclic pyrrolopyrimidines with submicromolar JAK1 IC50 values and a preference for JAK1 over JAK2 as potential starting points in developing a novel class of JAK1 inhibitors. spirocyclic pyrrolopyrimidines 29-59 Janus kinase 1 Homo sapiens 79-83 27055521-0 2016 Safety, tolerability, efficacy and pharmacodynamics of the selective JAK1 inhibitor GSK2586184 in patients with systemic lupus erythematosus. GSK2586184 84-94 Janus kinase 1 Homo sapiens 69-73 27055521-1 2016 We aimed to evaluate the pharmacodynamics, efficacy, safety and tolerability of the JAK1 inhibitor GSK2586184 in adults with systemic lupus erythematosus (SLE). GSK2586184 99-109 Janus kinase 1 Homo sapiens 84-88 27244086-0 2016 Molecular docking, 3D QSAR and dynamics simulation studies of imidazo-pyrrolopyridines as janus kinase 1 (JAK 1) inhibitors. imidazo-pyrrolopyridines 62-86 Janus kinase 1 Homo sapiens 106-111 27244086-3 2016 Docking, 3D quantitative structure activity relationship (3D-QSAR) and molecular dynamics (MD) studies were performed on a series of Imidazo-pyrrolopyridine derivatives reported as JAK 1 inhibitors. imidazo-pyrrolopyridine 133-156 Janus kinase 1 Homo sapiens 181-186 27910962-4 2016 Baricitinib (LY-3009104, INCB-028050), a new potent and selective tyrosine-protein kinase JAK1/JAK2 inhibitor, has shown clinical efficacy in patients with RA refractory to aggressive standard-of-care treatment (with both conventional DMARDs and bDMARDs) when administered orally at 4 mg q.d. baricitinib 0-11 Janus kinase 1 Homo sapiens 90-94 27910962-4 2016 Baricitinib (LY-3009104, INCB-028050), a new potent and selective tyrosine-protein kinase JAK1/JAK2 inhibitor, has shown clinical efficacy in patients with RA refractory to aggressive standard-of-care treatment (with both conventional DMARDs and bDMARDs) when administered orally at 4 mg q.d. baricitinib 13-23 Janus kinase 1 Homo sapiens 90-94 27910962-4 2016 Baricitinib (LY-3009104, INCB-028050), a new potent and selective tyrosine-protein kinase JAK1/JAK2 inhibitor, has shown clinical efficacy in patients with RA refractory to aggressive standard-of-care treatment (with both conventional DMARDs and bDMARDs) when administered orally at 4 mg q.d. baricitinib 25-36 Janus kinase 1 Homo sapiens 90-94 27268955-8 2016 In early clinical trials, the pentoxifylline derivative CTP-499, the CCR2 inhibitor CCX140-B, the CCL2 inhibitor emapticap pegol and the JAK1/JAK2 inhibitor baricitinib were the most promising drugs for diabetic kidney disease. baricitinib 157-168 Janus kinase 1 Homo sapiens 137-141 27738655-6 2016 We showed that in vitro this antiviral state could be reverted by combining VSV-GP with the JAK1/2-inhibitor ruxolitinib. ruxolitinib 109-120 Janus kinase 1 Homo sapiens 92-96 27729820-5 2016 Ruxolitinib, a JAK 1 and 2 inhibitor, has already proven to be efficient in relieving symptoms in primary myelofibrosis and PV. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-26 27699253-4 2016 Here, we investigated the use of the oral JAK1/2 inhibitor ruxolitinib in the treatment of patients with moderate-to-severe AA. ruxolitinib 59-70 Janus kinase 1 Homo sapiens 42-48 27427830-5 2016 Five phase 3 trials of Baricitinib, a JAK1 and JAK2 inhibitor, have been performed and showed high clinical efficacy in patients with active RA and naive to sDMARDs or an inadequate response to sDMARDs, MTX or bDMARDs. baricitinib 23-34 Janus kinase 1 Homo sapiens 38-42 27460897-3 2016 The JAK inhibitor SHR0302 is a synthetic molecule that potently inhibits all members of the JAK family, particularly JAK1. ivarmacitinib 18-25 Janus kinase 1 Homo sapiens 117-121 27272942-6 2016 The increased IL-7 was secreted by mesenchymal stem cells (MSC) in the bone marrow, which may protect leukemic cells from apoptosis induced by imatinib through JAK1/STAT5 signaling pathway. Imatinib Mesylate 143-151 Janus kinase 1 Homo sapiens 160-164 27572962-2 2016 The US FDA -approved JAK1-3 inhibitor tofacitinib also potently inhibits PRK1 in vitro. tofacitinib 38-49 Janus kinase 1 Homo sapiens 21-25 27163538-3 2016 Tofacitinib, an oral Janus kinase inhibitor that targets Jak1/Jak3 dependent Stat activation, has been assessed as a substitute for calcineurin inhibitor therapy after low-to-moderate risk kidney transplantation in 3 randomized trials. tofacitinib 0-11 Janus kinase 1 Homo sapiens 57-61 30209928-0 2016 [Sodium Aescinate Induced Apoptosis of BGC-823 and AGS Cells by Inhibiting JAK-1/STAT-1 Signaling Pathway]. sodium aescinate 1-17 Janus kinase 1 Homo sapiens 75-80 30209928-4 2016 Conclusion: Sodium aescinate inhibit the proliferation and induce apoptosis in the gastric cancer BGC-823 cells and AGS cells, and this process can be implemented by inhibiting the JAK-1/STAT-1 signaling pathway. sodium aescinate 12-28 Janus kinase 1 Homo sapiens 181-186 27774135-0 2016 Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1H)-pyrazole Derivatives as JAKs Inhibitors. 4-amino-(1h)-pyrazole 47-68 Janus kinase 1 Homo sapiens 84-88 27774135-2 2016 Herein, we designed and synthesized a series of 4-amino-(1H)-pyrazole derivatives as potent JAKs inhibitors for cancer treatment. 4-amino-(1h)-pyrazole 48-69 Janus kinase 1 Homo sapiens 92-96 27774135-6 2016 It is worth noting that both 3f and 11b showed more potent antiproliferative activities than the approved JAKs inhibitor Ruxolitinib. ruxolitinib 121-132 Janus kinase 1 Homo sapiens 106-110 27570458-7 2016 In clinical trials, the JAK1/JAK2 inhibitor ruxolitinib - the first therapy approved for MF worldwide - improved disease-related splenomegaly and symptoms independent of JAK2 (V617F) mutational status, and prolonged survival compared with placebo or standard therapy in patients with advanced MF. ruxolitinib 44-55 Janus kinase 1 Homo sapiens 24-28 27473820-12 2016 Tofacitinib is a pan-JAK inhibitor that is approved by the FDA for the treatment of rheumatoid arthritis and ruxolitinib is a JAK1/2 inhibitor that is approved for the treatment of polycythemia vera and myelofibrosis. ruxolitinib 109-120 Janus kinase 1 Homo sapiens 126-132 26979390-2 2016 In this issue, ruxolitinib, a JAK1 and -2 inhibitory drug, is shown to induce objective responses in chronic myelomonocytic leukemia patients. ruxolitinib 15-26 Janus kinase 1 Homo sapiens 30-41 27502249-7 2016 Ruxolitinib, a JAK1/2 inhibitor approved for intermediate-2/high-risk myelofibrosis, was recently employed in SR-GvHD with encouraging overall response rates. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 26858309-1 2016 PURPOSE: To conduct a phase I clinical trial exploring the safety and efficacy of ruxolitinib, a JAK1/2 inhibitor, for chronic myelomonocytic leukemia (CMML). ruxolitinib 82-93 Janus kinase 1 Homo sapiens 97-103 27137359-0 2016 Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. 1H-Pyrazol-4-amine 59-74 Janus kinase 1 Homo sapiens 107-111 26769332-2 2016 OBJECTIVE: To evaluate the safety and efficacy of the oral selective JAK1 inhibitor INCB039110 in stable, chronic plaque psoriasis. INCB039110 84-94 Janus kinase 1 Homo sapiens 69-73 27102499-1 2016 RESPONSE is an open-label phase 3 study evaluating the Janus kinase 1/Janus kinase 2 inhibitor ruxolitinib versus best available therapy for efficacy/safety in hydroxyurea-resistant or intolerant patients with polycythemia vera. Hydroxyurea 160-171 Janus kinase 1 Homo sapiens 55-69 27175602-14 2016 Quercetin reduced the expression of phospho-JAK1 and phospho-STAT3 and decreased STAT3-dependent luciferase reporter gene activity in the BT-474 cells. Quercetin 0-9 Janus kinase 1 Homo sapiens 44-48 27211272-1 2016 Ruxolitinib is a Janus kinase (JAK) (JAK1/JAK2) inhibitor that has demonstrated superiority over placebo and best available therapy (BAT) in the Controlled Myelofibrosis Study with Oral JAK Inhibitor Treatment (COMFORT) studies. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 37-41 27261178-0 2016 Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability. benzimidazole 21-34 Janus kinase 1 Homo sapiens 6-10 27261178-1 2016 The previously identified Janus kinase 1 (JAK1)-selective inhibitor, 1-(2-aminoethyl)-2-(piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxamide (2), suffered from low cell permeability, which resulted in poor pharmacokinetic properties. 1-(2-aminoethyl)-2-(piperidin-4-yl)-1H-benzo(d)imidazole-5-carboxamide 69-139 Janus kinase 1 Homo sapiens 26-40 27261178-1 2016 The previously identified Janus kinase 1 (JAK1)-selective inhibitor, 1-(2-aminoethyl)-2-(piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxamide (2), suffered from low cell permeability, which resulted in poor pharmacokinetic properties. 1-(2-aminoethyl)-2-(piperidin-4-yl)-1H-benzo(d)imidazole-5-carboxamide 69-139 Janus kinase 1 Homo sapiens 42-46 27259268-6 2016 Overexpression of constitutively active STAT3 partly reversed the anti cancer effects of (-)-oleocanthal, which inhibited STAT3 activation by decreasing the activities of JAK1 and JAK2 and increasing the activity of SHP-1. oleocanthal 89-104 Janus kinase 1 Homo sapiens 171-175 27137359-2 2016 We designed and synthesized a novel series of 4-aminopyrazole derivatives, which showed inhibitory potency against various JAKs. 1H-Pyrazol-4-amine 46-61 Janus kinase 1 Homo sapiens 123-127 27371847-0 2016 [Astaxanthin inhibits proliferation and promotes apoptosis of A549 lung cancer cells via blocking JAK1/STAT3 pathway]. astaxanthine 1-12 Janus kinase 1 Homo sapiens 98-102 27017614-5 2016 Ruxolitinib, an oral JAK1/JAK2 inhibitor, is approved in the USA for the treatment of patients with intermediate- or high-risk MF and patients with PV who have had an inadequate response to or are intolerant of hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-25 26800231-0 2016 A randomized phase 2b trial of baricitinib, an oral Janus kinase (JAK) 1/JAK2 inhibitor, in patients with moderate-to-severe psoriasis. baricitinib 31-42 Janus kinase 1 Homo sapiens 52-72 26800231-2 2016 OBJECTIVES: To evaluate the safety and efficacy of baricitinib, an oral Janus kinase (JAK) 1/JAK2 inhibitor, in patients with moderate-to-severe psoriasis in a randomized, double-blind, placebo-controlled, dose-ranging phase 2b study. baricitinib 51-62 Janus kinase 1 Homo sapiens 72-92 27371847-6 2016 Western blotting showed that astaxanthin up-regulated the expression of Bax and down-regulated the expressions of Bcl-2, STAT3 and JAK1. astaxanthine 29-40 Janus kinase 1 Homo sapiens 131-135 27371847-7 2016 Conclusion Astaxanthin functions as a potent inhibitor of A549 lung cancer cell growth by targeting JAK1/STAT3 signaling pathway. astaxanthine 11-22 Janus kinase 1 Homo sapiens 100-104 27045723-4 2016 In Filgotinib group, the specific inhibitor of Janus kinase 1 (JAK1), Filgotinib, was used to detect the role of JAK1/signal transducer and activator of transcription 1 (STAT1) signaling pathway in LPS challenge, and the aqueous physiological buffer group was used as the control. GLPG0634 3-13 Janus kinase 1 Homo sapiens 47-61 31360077-6 2016 Ruxolitinib is an orally available small-molecule tyrosine kinase inhibitor that is a potent and selective inhibitor of JAK1/JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 120-124 26910327-0 2016 The Selective JAK1/3-Inhibitor R507 Mitigates Obliterative Airway Disease Both With Systemic Administration and Aerosol Inhalation. r507 31-35 Janus kinase 1 Homo sapiens 14-18 26927423-0 2016 Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors. (benz)imidazole pyridones 42-67 Janus kinase 1 Homo sapiens 71-75 26927423-5 2016 Concurrent crystallography-driven exploration of the ribose pocket and the solvent front led to analogs with optimized kinome and JAK1 selectivities over the JAK2 isoform by targeting several residues unique to JAK1, such as Arg-879 and Glu-966. Ribose 53-59 Janus kinase 1 Homo sapiens 130-134 26927423-5 2016 Concurrent crystallography-driven exploration of the ribose pocket and the solvent front led to analogs with optimized kinome and JAK1 selectivities over the JAK2 isoform by targeting several residues unique to JAK1, such as Arg-879 and Glu-966. Ribose 53-59 Janus kinase 1 Homo sapiens 211-215 26927423-5 2016 Concurrent crystallography-driven exploration of the ribose pocket and the solvent front led to analogs with optimized kinome and JAK1 selectivities over the JAK2 isoform by targeting several residues unique to JAK1, such as Arg-879 and Glu-966. Arginine 225-228 Janus kinase 1 Homo sapiens 211-215 26927423-5 2016 Concurrent crystallography-driven exploration of the ribose pocket and the solvent front led to analogs with optimized kinome and JAK1 selectivities over the JAK2 isoform by targeting several residues unique to JAK1, such as Arg-879 and Glu-966. Glutamic Acid 237-240 Janus kinase 1 Homo sapiens 211-215 26785220-0 2016 Investigation of selective JAK1 inhibitor GSK2586184 for the treatment of psoriasis in a randomized placebo-controlled phase IIa study. GSK2586184 42-52 Janus kinase 1 Homo sapiens 27-31 26785220-1 2016 BACKGROUND: GSK2586184 is a selective oral Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis. GSK2586184 12-22 Janus kinase 1 Homo sapiens 43-62 27053336-0 2016 Piperlongumine inhibits gastric cancer cells via suppression of the JAK1,2/STAT3 signaling pathway. piperlonguminine 0-14 Janus kinase 1 Homo sapiens 68-74 27053336-5 2016 In addition, PL reduced the phosphorylation of Janus kinase (JAK)1, JAK2 and signal transducer and activator of transcription (STAT)3 in a concentration-dependent manner, as indicated by western blot analysis, and decreased the expression of STAT3-dependent tumor-associated genes in GC cells, as revealed by PCR analysis. piperlonguminine 13-15 Janus kinase 1 Homo sapiens 47-66 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). Dimethyl Fumarate 157-174 Janus kinase 1 Homo sapiens 74-91 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). Dimethyl Fumarate 157-174 Janus kinase 1 Homo sapiens 93-97 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). Dimethyl Fumarate 176-179 Janus kinase 1 Homo sapiens 74-91 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). Dimethyl Fumarate 176-179 Janus kinase 1 Homo sapiens 93-97 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). citraconic acid 252-272 Janus kinase 1 Homo sapiens 74-91 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). citraconic acid 252-272 Janus kinase 1 Homo sapiens 93-97 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). citraconic acid 274-277 Janus kinase 1 Homo sapiens 74-91 26981780-1 2016 We determined whether the myelofibrosis drug ruxolitinib, an inhibitor of Janus kinases 1/2 (JAK1 and JAK2), could interact with the multiple sclerosis drug dimethyl-fumarate (DMF) to kill tumor cells; studies used the in vivo active form of the drug, mono-methyl fumarate (MMF). citraconic acid 274-277 Janus kinase 1 Homo sapiens 93-97 27045723-4 2016 In Filgotinib group, the specific inhibitor of Janus kinase 1 (JAK1), Filgotinib, was used to detect the role of JAK1/signal transducer and activator of transcription 1 (STAT1) signaling pathway in LPS challenge, and the aqueous physiological buffer group was used as the control. GLPG0634 3-13 Janus kinase 1 Homo sapiens 63-67 27045723-4 2016 In Filgotinib group, the specific inhibitor of Janus kinase 1 (JAK1), Filgotinib, was used to detect the role of JAK1/signal transducer and activator of transcription 1 (STAT1) signaling pathway in LPS challenge, and the aqueous physiological buffer group was used as the control. GLPG0634 70-80 Janus kinase 1 Homo sapiens 47-61 27045723-4 2016 In Filgotinib group, the specific inhibitor of Janus kinase 1 (JAK1), Filgotinib, was used to detect the role of JAK1/signal transducer and activator of transcription 1 (STAT1) signaling pathway in LPS challenge, and the aqueous physiological buffer group was used as the control. GLPG0634 70-80 Janus kinase 1 Homo sapiens 63-67 26755644-2 2016 However, the lack of complete response in most patients treated with the JAK1/2 inhibitor, ruxolitinib, indicates the need for identifying pathways that cooperate with JAK2. ruxolitinib 91-102 Janus kinase 1 Homo sapiens 73-79 26717494-4 2016 Over the last decade, the molecular pathogenesis of MPNs has been elucidated considerably, and the Janus kinase (JAK) 1/2 inhibitor ruxolitinib is the first drug specifically approved by the US Food and Drug Administration to treat patients with intermediate-risk and high-risk myelofibrosis. ruxolitinib 132-143 Janus kinase 1 Homo sapiens 99-119 26493563-5 2016 OS was 91% (95% CI, 69% to 98%) for those who experienced clinical improvement and 32% (95% CI, 8% to 59%) for those who developed LT on JAK1/2 inhibitors. Osmium 0-2 Janus kinase 1 Homo sapiens 137-141 26846873-3 2016 Ruxolitinib, a potent JAK1/2 inhibitor, initially approved for myelofibrosis, was recently approved for patients with polycythemia vera refractory or intolerant to hydroxycarbamide. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-28 26834213-1 2016 OBJECTIVE: To evaluate efficacy and safety, baricitinib [Janus kinase (JAK) 1/JAK2 inhibitor] was compared with placebo in Japanese patients with active rheumatoid arthritis (RA) despite background treatment with methotrexate (MTX). baricitinib 44-55 Janus kinase 1 Homo sapiens 57-77 26701727-8 2016 Furthermore,the sensitivity to the treatment of a JAK1/2 inhibitor, ruxolitinib, was observed in JAK1S703I mutant PDX model, but not in other non-activating mutant or wild type models. ruxolitinib 68-79 Janus kinase 1 Homo sapiens 50-56 26855781-2 2016 According to the literature, Ruxolitinib, a JAK1/JAK2 inhibitor, has been shown to reduce symptoms related to proinflammatory cytokine release in other myeloproliferative neoplasms. ruxolitinib 29-40 Janus kinase 1 Homo sapiens 44-48 26811457-5 2016 In the present study the JAK1/2 inhibitor ruxolitinib reduced phosphorylation of STAT3 and STAT6 and expression of c-Myc in the HL cell line HDLM-2. ruxolitinib 42-53 Janus kinase 1 Homo sapiens 25-31 27840748-1 2016 The Janus kinase (JAK) 1 and 2 inhibitor, ruxolitinib, was recently approved in Japan and has been effective in many patients with myelofibrosis (MF). ruxolitinib 42-53 Janus kinase 1 Homo sapiens 4-30 26701356-2 2016 High-throughput screening against TYK2 and JAK1-3 provided aminoindazole derivative 1 as a hit compound. 1H-Indazol-3-amine 59-72 Janus kinase 1 Homo sapiens 43-47 26682735-6 2016 Six compounds were identified and confirmed in vitro, with an indazole-based hit exhibiting promising selectivity for JAK2 vs JAK1. Indazoles 62-70 Janus kinase 1 Homo sapiens 126-130 26586478-6 2016 Concomitantly targeting the TGF-beta type I receptor (TbetaRI) kinase with SB505124 and JAK1-2 with ruxolitinib suppresses JAK1 phosphorylation and blocks proliferative cross-talk between human pancreatic cancer cells (PCCs) and human endothelial cells (ECs), and these anti-proliferative effects were mimicked by JAK1 silencing in ECs. ruxolitinib 100-111 Janus kinase 1 Homo sapiens 88-92 26586478-6 2016 Concomitantly targeting the TGF-beta type I receptor (TbetaRI) kinase with SB505124 and JAK1-2 with ruxolitinib suppresses JAK1 phosphorylation and blocks proliferative cross-talk between human pancreatic cancer cells (PCCs) and human endothelial cells (ECs), and these anti-proliferative effects were mimicked by JAK1 silencing in ECs. ruxolitinib 100-111 Janus kinase 1 Homo sapiens 123-127 26586478-6 2016 Concomitantly targeting the TGF-beta type I receptor (TbetaRI) kinase with SB505124 and JAK1-2 with ruxolitinib suppresses JAK1 phosphorylation and blocks proliferative cross-talk between human pancreatic cancer cells (PCCs) and human endothelial cells (ECs), and these anti-proliferative effects were mimicked by JAK1 silencing in ECs. ruxolitinib 100-111 Janus kinase 1 Homo sapiens 123-127 26693854-0 2016 Clinical Confirmation that the Selective JAK1 Inhibitor Filgotinib (GLPG0634) has a Low Liability for Drug-drug Interactions. GLPG0634 56-66 Janus kinase 1 Homo sapiens 41-45 26614408-0 2016 Identification of azabenzimidazoles as potent JAK1 selective inhibitors. 1H-imidazo(4,5-b)pyridine 18-35 Janus kinase 1 Homo sapiens 46-50 26614408-1 2016 We have identified a class of azabenzimidazoles as potent and selective JAK1 inhibitors. 1H-imidazo(4,5-b)pyridine 30-47 Janus kinase 1 Homo sapiens 72-76 26693854-1 2016 OBJECTIVE: The selective Janus kinase 1 inhibitor filgotinib (GLPG0634), which is currently in clinical development for the treatment of rheumatoid arthritis (RA) and Crohn"s disease, demonstrated encouraging safety and efficacy profiles in RA patients after 4 weeks of daily dosing. GLPG0634 50-60 Janus kinase 1 Homo sapiens 25-39 26648193-4 2015 In this article, we present our recommendations for the practical management of myelofibrosis with ruxolitinib, a selective inhibitor of both JAK1 and JAK2. ruxolitinib 99-110 Janus kinase 1 Homo sapiens 142-146 26482169-0 2015 Comment on: "Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modelling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection". GLPG0634 79-89 Janus kinase 1 Homo sapiens 114-118 26482170-0 2015 Author"s Reply to Srinivas: "Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection". GLPG0634 94-104 Janus kinase 1 Homo sapiens 129-133 26562526-6 2015 JI069 inhibited gp130 signaling by inducing dissociation between gp130 and JAK1. ji069 0-5 Janus kinase 1 Homo sapiens 75-79 26433906-10 2015 A recent phase 3 trial has shown the superiority of the JAK1/2 inhibitor ruxolitinib in comparison to best available treatment in HU-intolerant or -resistant patients. ruxolitinib 73-84 Janus kinase 1 Homo sapiens 56-62 26623653-2 2015 Targeted therapy with Ruxolitinib, a JAK1/2-specific inhibitor, achieves symptomatic improvement but does not eliminate the neoplastic clone. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 37-41 26455550-3 2015 Most importantly, myricetin interacts with oncoproteins such as protein kinase B (PKB) (Akt), Fyn, MEK1, and JAK1-STAT3 (Janus kinase-signal transducer and activator of transcription 3), and it attenuates the neoplastic transformation of cancer cells. myricetin 18-27 Janus kinase 1 Homo sapiens 109-113 26372653-0 2015 Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors. 6H-pyrrolo(2,3-e)(1,2,4)triazolo(4,3-a)pyrazine 35-83 Janus kinase 1 Homo sapiens 87-91 26375873-5 2015 In addition, resveratrol inhibited the phosphorylation of JAK1, JAK2, and Tyk2 and their downstream mediators, including STAT3 and STAT5. Resveratrol 13-24 Janus kinase 1 Homo sapiens 58-62 26443624-1 2015 The development of the dual Janus kinase 1/2 (JAK1/2) inhibitor ruxolitinib for the treatment of myeloproliferative neoplasms (MPNs) has led to studies of ruxolitinib in other clinical contexts, including JAK-mutated acute lymphoblastic leukemia (ALL). ruxolitinib 64-75 Janus kinase 1 Homo sapiens 46-52 26443624-1 2015 The development of the dual Janus kinase 1/2 (JAK1/2) inhibitor ruxolitinib for the treatment of myeloproliferative neoplasms (MPNs) has led to studies of ruxolitinib in other clinical contexts, including JAK-mutated acute lymphoblastic leukemia (ALL). ruxolitinib 155-166 Janus kinase 1 Homo sapiens 46-52 26552452-4 2015 The JAK1/2 inhibitor, ruxolitinib, was the first JAK inhibitor approved for patients with intermediate- to high-risk myelofibrosis and its effects in improving symptoms and survival benefits were demonstrated by randomized controlled trials. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 4-10 26356819-1 2015 The JAK/STAT pathway is constitutively activated in myeloproliferative neoplasms and can be inhibited by ruxolitinib, a selective JAK1/2 inhibitor. ruxolitinib 105-116 Janus kinase 1 Homo sapiens 130-136 26351728-0 2015 Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. benzimidazole 0-13 Janus kinase 1 Homo sapiens 36-40 26362333-1 2015 Ruxolitinib (Jakavi( ), Jakafi( )) is an orally administered, first-in-class Janus Kinase (JAK) 1 and 2 inhibitor that was recently approved for the treatment of patients with polycythaemia vera (PV) who have responded inadequately to or are intolerant of hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 77-103 26362333-2 2015 By inhibiting JAK 1 and 2, ruxolitinib reduces hyperactive JAK-signal transducers and activators of transcription (STAT) signalling that is implicated in the pathogenesis of PV. ruxolitinib 27-38 Janus kinase 1 Homo sapiens 14-25 25976292-1 2015 BACKGROUND: Ruxolitinib, an orally bioavailable JAK1/JAK2 inhibitor, may treat cancers with CRLF2 and/or JAK pathway mutations. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 48-52 26351728-4 2015 In this study, as part of our continued efforts to develop a selective JAK1 inhibitor, a series of 1,2-disubstituted benzimidazole-5-carboxamide derivatives was prepared and their inhibitory activities against all four JAK isozymes were evaluated. 1,2-disubstituted benzimidazole-5-carboxamide 99-144 Janus kinase 1 Homo sapiens 71-75 26351728-5 2015 A clear structure-activity relationship was observed with respect to JAK1 selectivity; this highlighted the importance of hydrogen bond donors at both N(1) and R2 positions located within a specific distance from the benzimidazole core. Hydrogen 122-130 Janus kinase 1 Homo sapiens 69-73 26351728-5 2015 A clear structure-activity relationship was observed with respect to JAK1 selectivity; this highlighted the importance of hydrogen bond donors at both N(1) and R2 positions located within a specific distance from the benzimidazole core. benzimidazole 217-230 Janus kinase 1 Homo sapiens 69-73 26351728-6 2015 One of the synthesized compounds, 1-(2-aminoethyl)-2-(piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxamide (5c), showed remarkable JAK1 selectivity (63-fold vs JAK2, 25-fold vs JAK3, and 74-fold vs Tyk2). 1-(2-aminoethyl)-2-(piperidin-4-yl)-1H-benzo(d)imidazole-5-carboxamide 34-104 Janus kinase 1 Homo sapiens 129-133 26351728-7 2015 Molecular docking revealed that the 2-aminoethyl and piperidin-4-yl substituents of 5c function as probes to differentiate the ATP-binding site of JAK1 from that of JAK2, resulting in preferential JAK1 binding. 2-aminoethyl and piperidin-4-yl 36-67 Janus kinase 1 Homo sapiens 147-151 26351728-7 2015 Molecular docking revealed that the 2-aminoethyl and piperidin-4-yl substituents of 5c function as probes to differentiate the ATP-binding site of JAK1 from that of JAK2, resulting in preferential JAK1 binding. 2-aminoethyl and piperidin-4-yl 36-67 Janus kinase 1 Homo sapiens 197-201 26351728-7 2015 Molecular docking revealed that the 2-aminoethyl and piperidin-4-yl substituents of 5c function as probes to differentiate the ATP-binding site of JAK1 from that of JAK2, resulting in preferential JAK1 binding. Adenosine Triphosphate 127-130 Janus kinase 1 Homo sapiens 147-151 26351728-7 2015 Molecular docking revealed that the 2-aminoethyl and piperidin-4-yl substituents of 5c function as probes to differentiate the ATP-binding site of JAK1 from that of JAK2, resulting in preferential JAK1 binding. Adenosine Triphosphate 127-130 Janus kinase 1 Homo sapiens 197-201 26232434-0 2015 Parafibromin Is a Component of IFN-gamma-Triggered Signaling Pathways That Facilitates JAK1/2-Mediated Tyrosine Phosphorylation of STAT1. Tyrosine 103-111 Janus kinase 1 Homo sapiens 87-91 26231159-3 2015 Stimulation with IFNalpha/beta leads to the tyrosine phosphorylation of the JAK1 and Tyk2 receptor-associated kinases with subsequent STATs activation, transmitting signals from the cell surface receptor to the nucleus. Tyrosine 44-52 Janus kinase 1 Homo sapiens 76-80 26152731-7 2015 Tofacitinib, a small product targeting JAK, inhibits phosphorylation of JAK1 and JAK3, subsequent Stat1 and expression of Stat1-inducible genes, which contribute to efficient propagation of its anti-inflammatory effects for the treatment of RA. tofacitinib 0-11 Janus kinase 1 Homo sapiens 72-76 25980454-4 2015 Ruxolitinib is an oral JAK1/JAK2 inhibitor that has been evaluated in Phase II and III clinical trials in patients with PV, who are intolerant of or resistant to hydroxyurea. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 23-27 26059596-2 2015 To identify JAK inhibitors, we focused on the 1H-pyrrolo[2,3-b]pyridine derivative 3, which exhibited moderate JAK3 and JAK1 inhibitory activities. pyrrolo(2, 3-b)pyridine 46-71 Janus kinase 1 Homo sapiens 120-124 25681059-0 2015 Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection. GLPG0634 65-75 Janus kinase 1 Homo sapiens 100-104 25681059-1 2015 BACKGROUND AND OBJECTIVES: Filgotinib (GLPG0634) is a selective inhibitor of Janus kinase 1 (JAK1) currently in development for the treatment of rheumatoid arthritis and Crohn"s disease. GLPG0634 27-37 Janus kinase 1 Homo sapiens 77-91 25681059-1 2015 BACKGROUND AND OBJECTIVES: Filgotinib (GLPG0634) is a selective inhibitor of Janus kinase 1 (JAK1) currently in development for the treatment of rheumatoid arthritis and Crohn"s disease. GLPG0634 27-37 Janus kinase 1 Homo sapiens 93-97 25915176-1 2015 Ruxolitinib, a JAK1 and JAK2 inhibitor, has been tested and approved for the treatment of primary and secondary myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-19 25959371-4 2015 Furthermore, this probe was applied to establish the selectivity profile of the JAK1/2 inhibitor momelotinib that is currently evaluated in clinical phase 3 studies. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 97-108 Janus kinase 1 Homo sapiens 80-86 26059596-3 2015 Optimization of 3 identified the tricyclic imidazo-pyrrolopyridinone derivative 19, which exhibited potent JAK3 and JAK1 inhibitory activities (IC50=1.1 nM, 1.5 nM, respectively) with favorable metabolic stability. tricyclic imidazo-pyrrolopyridinone 33-68 Janus kinase 1 Homo sapiens 116-120 26166037-0 2015 Homoharringtonine induces apoptosis and inhibits STAT3 via IL-6/JAK1/STAT3 signal pathway in Gefitinib-resistant lung cancer cells. Homoharringtonine 0-17 Janus kinase 1 Homo sapiens 64-68 25736380-8 2015 Inhibition of FGFR signaling and to a lesser extent JAK1/2 signaling profoundly enhanced OSU-03012/sildenafil lethality. OSU 03012 89-98 Janus kinase 1 Homo sapiens 52-56 25736380-8 2015 Inhibition of FGFR signaling and to a lesser extent JAK1/2 signaling profoundly enhanced OSU-03012/sildenafil lethality. Sildenafil Citrate 99-109 Janus kinase 1 Homo sapiens 52-56 25818476-7 2015 Finally, we demonstrated that JAK1, JAK2, and STAT1 were indispensable for the actual enhancement of PG production in response to IFN-gamma stimulation. Prostaglandins 101-103 Janus kinase 1 Homo sapiens 30-34 26288713-4 2015 The first of these agents to be approved was ruxolitinib, a JAK1/JAK2 inhibitor, which has been shown to improve both spleen size and symptoms in patients with MF. ruxolitinib 45-56 Janus kinase 1 Homo sapiens 60-64 26166037-0 2015 Homoharringtonine induces apoptosis and inhibits STAT3 via IL-6/JAK1/STAT3 signal pathway in Gefitinib-resistant lung cancer cells. Gefitinib 93-102 Janus kinase 1 Homo sapiens 64-68 26167286-1 2015 BACKGROUND: Ruxolitinib, a novel inhibitor of Janus kinases 1 and 2, was recently approved for the treatment of myelofibrosis but, recently, attention has been drawn to potential side effects and especially opportunistic infections and virus reactivations. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 46-67 25931145-4 2015 We demonstrate that strong stimuli (e.g. intact Escherichia coli or LPS in addition to IL-1beta) induce IL-12p70 via a ROS/RELA/CDK9 pathway that is inhibited by simultaneous JAK1/STAT3 signalling. ros 119-122 Janus kinase 1 Homo sapiens 175-179 25926026-3 2015 This new methodology was further applied in a highly efficient synthesis of JAK 1/2 inhibitor (R)-ruxolitinib. 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile 94-109 Janus kinase 1 Homo sapiens 76-83 25644746-5 2015 The JAK1/JAK2 inhibitor ruxolitinib is approved for the treatment of myelofibrosis and is currently under clinical development for polycythemia vera. ruxolitinib 24-35 Janus kinase 1 Homo sapiens 4-8 26121980-7 2015 Analysis of gene-expression with cytotoxicity identified JAK1 expression to be a significant predictor of triptolide sensitivity. triptolide 106-116 Janus kinase 1 Homo sapiens 57-61 25315076-2 2015 In the phase 3 Controlled Myelofibrosis Study with Oral JAK Inhibitor Treatment (COMFORT) studies, ruxolitinib, a potent Janus kinase 1 (JAK1)/JAK2 inhibitor, provided substantial improvements in splenomegaly, symptoms, quality-of-life measures and overall survival compared with placebo or best available therapy. ruxolitinib 99-110 Janus kinase 1 Homo sapiens 121-135 25315076-2 2015 In the phase 3 Controlled Myelofibrosis Study with Oral JAK Inhibitor Treatment (COMFORT) studies, ruxolitinib, a potent Janus kinase 1 (JAK1)/JAK2 inhibitor, provided substantial improvements in splenomegaly, symptoms, quality-of-life measures and overall survival compared with placebo or best available therapy. ruxolitinib 99-110 Janus kinase 1 Homo sapiens 137-141 26131691-18 2015 While the JAK1/2 inhibitor ruxolitinib is effective, a $43,200 annual cost precludes widespread adoption. ruxolitinib 27-38 Janus kinase 1 Homo sapiens 10-16 25398374-0 2015 The JAK inhibitor tofacitinib suppresses synovial JAK1-STAT signalling in rheumatoid arthritis. tofacitinib 18-29 Janus kinase 1 Homo sapiens 50-54 26056473-2 2015 Ruxolitinib, a JAK1/JAK2 tyrosine kinase inhibitor, is now widely used for first- and second-line therapy in persons with MPN-MF, especially those with disease-related splenomegaly, intermediate- or high-risk disease, and constitutional symptoms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-19 25824483-1 2015 Ruxolitinib (INCB018424) is the first JAK1/JAK2 inhibitor approved for treatment of myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-42 25824483-1 2015 Ruxolitinib (INCB018424) is the first JAK1/JAK2 inhibitor approved for treatment of myelofibrosis. ruxolitinib 13-23 Janus kinase 1 Homo sapiens 38-42 25917087-6 2015 The results indicate that, through Gi and JAK1 and 2 kinases activation, CXCL12 signaling cooperates to build the IS and to maintain adhesive contacts between APC and T cells, required for continuous TCR signaling. is 114-116 Janus kinase 1 Homo sapiens 42-52 26316485-1 2015 Ruxolitinib, a JAK1 and JAK2 inhibitor drug, has recently been approved for the treatment of patients with high- or intermediate-risk myelofibrosis with symptomatic splenomegaly. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-19 25724932-0 2015 DRESS syndrome and reversible liver function abnormalities in patients with systemic lupus erythematosus treated with the highly selective JAK-1 inhibitor GSK2586184. GSK2586184 155-165 Janus kinase 1 Homo sapiens 139-144 25515354-7 2015 In randomized controlled phase 3 studies, the JAK1/JAK2 inhibitor ruxolitinib provided rapid and lasting improvement in MF-related splenomegaly and symptom burden as well as a survival advantage compared with placebo or best available therapy. ruxolitinib 66-77 Janus kinase 1 Homo sapiens 46-50 25762644-5 2015 Conversely, STAT3 silencing or JAK1-2 inhibition with ruxolitinib blocks CM-enhanced EC proliferation. ruxolitinib 54-65 Janus kinase 1 Homo sapiens 31-35 25762644-8 2015 Thus, targeting JAK1-2 with ruxolitinib blocks a final pathway that is common to multiple pro-angiogenic factors, suppresses EC-mediated PCC proliferation, and may be useful in PDACs with a strong pro-angiogenic signature. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 16-20 25870379-3 2015 Biological advances in MPN have translated into the rapid development of novel therapeutics, culminating in the approval of the first treatment for MF, the JAK1/JAK2 inhibitor ruxolitinib. ruxolitinib 176-187 Janus kinase 1 Homo sapiens 156-160 25511866-1 2015 Momelotinib (a JAK1 and JAK2 inhibitor) induces both anaemia and spleen responses in myelofibrosis (MF). N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 15-19 25616577-1 2015 In the phase III COMFORT-I study, the Janus kinase 1 (JAK1)/JAK2 inhibitor ruxolitinib provided significant improvements in splenomegaly, key symptoms, and quality-of-life measures and was associated with an overall survival benefit relative to placebo in patients with intermediate-2 or high-risk myelofibrosis. ruxolitinib 75-86 Janus kinase 1 Homo sapiens 38-52 25616577-1 2015 In the phase III COMFORT-I study, the Janus kinase 1 (JAK1)/JAK2 inhibitor ruxolitinib provided significant improvements in splenomegaly, key symptoms, and quality-of-life measures and was associated with an overall survival benefit relative to placebo in patients with intermediate-2 or high-risk myelofibrosis. ruxolitinib 75-86 Janus kinase 1 Homo sapiens 54-58 25441108-0 2015 A phase I/II study of the Janus kinase (JAK)1 and 2 inhibitor ruxolitinib in patients with relapsed or refractory acute myeloid leukemia. ruxolitinib 62-73 Janus kinase 1 Homo sapiens 26-51 25441108-1 2015 BACKGROUND: Ruxolitinib is a potent and specific JAK1/JAK2 inhibitor recently approved for the treatment of myelofibrosis. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 49-53 26137574-0 2015 Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. baricitinib 74-85 Janus kinase 1 Homo sapiens 57-63 25810010-2 2015 AZD1480, an orally active pharmacologic inhibitor of JAK1/JAK2, has been tested in several cancer models. AZD 1480 0-7 Janus kinase 1 Homo sapiens 53-57 25638222-1 2015 Ruxolitinib is a potent Janus kinase (JAK) 1/JAK2 inhibitor that has demonstrated rapid and durable improvements in splenomegaly and symptoms and a survival benefit in 2 phase 3 trials in patients with myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 24-44 26137574-4 2015 METHODS: A patient with AA was enrolled in a clinical trial to examine the efficacy of baricitinib, a JAK1/2 inhibitor, to treat concomitant CANDLE syndrome. baricitinib 87-98 Janus kinase 1 Homo sapiens 102-108 24733674-0 2015 Cantharidin inhibits angiogenesis by suppressing VEGF-induced JAK1/STAT3, ERK and AKT signaling pathways. Cantharidin 0-11 Janus kinase 1 Homo sapiens 62-66 25431052-1 2015 OBJECTIVES: To investigate baricitinib (LY3009104, formerly INCB028050), a novel, oral inhibitor of JAK1/JAK2 in patients with moderate to severe rheumatoid arthritis (RA) despite treatment with methotrexate. baricitinib 27-38 Janus kinase 1 Homo sapiens 100-104 25431052-1 2015 OBJECTIVES: To investigate baricitinib (LY3009104, formerly INCB028050), a novel, oral inhibitor of JAK1/JAK2 in patients with moderate to severe rheumatoid arthritis (RA) despite treatment with methotrexate. baricitinib 40-49 Janus kinase 1 Homo sapiens 100-104 25576658-4 2015 Moreover, resveratrol pretreatment up-regulated the phosphorylated forms of JAK1 and STAT3, as well as suppressor of cytokine signaling (SOCS)3 protein expression in LPS activated cells, demonstrating that the JAK-STAT signaling pathway is involved in the anti-inflammatory effect exerted by resveratrol. Resveratrol 10-21 Janus kinase 1 Homo sapiens 76-80 25256963-2 2015 Ruxolitinib, a janus-activated kinase (JAK) 1/2 inhibitor, has proven to be beneficial in reduction of splenomegaly, improvement of constitutional symptoms, and possibly in overall survival. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-47 25601187-1 2015 Ruxolitinib (Jakavi( ), Jakafi( )) is an orally administered inhibitor of Janus kinases (JAK) 1 and 2 used in the management of patients with myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 74-101 26356267-1 2015 BACKGROUND/AIMS: The JAK1/JAK2 tyrosine kinase inhibitor ruxolitinib is widely used for the treatment of myeloproliferative neoplasm-associated myelofibrosis and other malignancies. ruxolitinib 57-68 Janus kinase 1 Homo sapiens 21-25 25504635-2 2015 The purpose of this study was to assess the preclinical efficacy of the JAK1/2 inhibitor AZD1480, both as a single agent and in combination with the MEK inhibitor selumetinib, against JAK-mutated patient-derived xenografts. AZD 1480 89-96 Janus kinase 1 Homo sapiens 72-76 25629741-1 2015 BACKGROUND: Ruxolitinib, a Janus kinase (JAK) 1 and 2 inhibitor, was shown to have a clinical benefit in patients with polycythemia vera in a phase 2 study. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 27-53 25482928-3 2015 Treatment with cucurbitacin-I depleted p-STAT3, p-STAT5, p-JAK1 and p-JAK2 levels, inhibited cell proliferation, and induced G2/M accumulation, DNA endoreduplication, and multipolar mitotic spindles. cucurbitacin I 15-29 Janus kinase 1 Homo sapiens 59-63 26315837-0 2015 Isoliquiritigenin Inhibits Interferon-gamma-Inducible Genes Expression in Hepatocytes through Down-Regulating Activation of JAK1/STAT1, IRF3/MyD88, ERK/MAPK, JNK/MAPK and PI3K/Akt Signaling Pathways. isoliquiritigenin 0-17 Janus kinase 1 Homo sapiens 124-128 25559089-4 2015 Protein kinases are highly attractive targets for drug discovery, as evidenced by the approval of almost 30 kinase inhibitors in oncology, and the successful development of the dual JAK1/2 (Janus kinase 1/2) inhibitor ruxolitinib for inflammatory indications. ruxolitinib 218-229 Janus kinase 1 Homo sapiens 182-188 26367195-1 2015 The first-in-class JAK1/JAK2 inhibitor ruxolitinib inhibits JAK/STAT signaling, inducing durable reductions in splenomegaly and constitutional symptoms in patients with myelofibrosis. ruxolitinib 39-50 Janus kinase 1 Homo sapiens 19-23 26389774-3 2015 Ruxolitinib, a JAK1 and 2 inhibitor, is the only currently approved agent. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-25 25757677-1 2015 The JAK1 and JAK2 inhibitor ruxolitinib has approved indications in myelofibrosis, a BCR-AB1-negative myeloproliferative neoplasm associated with progressive bone marrow fibrosis and shortened survival. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 4-8 25453808-3 2014 Incorporation of amino group to 3-position of the cyclopentane ring resulted in a series of JAK3 inhibitors (4g-4j) that potently inhibited IFNgamma production in an IL2-induced whole blood assay and displayed high functional selectivity for JAK3-JAK1 pathway relative to JAK2. Cyclopentanes 50-62 Janus kinase 1 Homo sapiens 247-251 25387665-5 2015 RESULTS: JTE-052 inhibited the JAK1, JAK2, JAK3, and tyrosine kinase (Tyk)2 enzymes in an adenosine triphosphate (ATP)-competitive manner and inhibited cytokine signaling evoked by IL-2, IL-6, IL-23, granulocyte/macrophage colony-stimulating factor, and IFN-alpha. Adenosine Triphosphate 114-117 Janus kinase 1 Homo sapiens 31-35 25586607-2 2015 Targeting of the JAK-STAT pathway has been the intense focus of therapeutic development and led to the approval of the JAK1/2 inhibitor, ruxolitinib. ruxolitinib 137-148 Janus kinase 1 Homo sapiens 119-125 25387665-5 2015 RESULTS: JTE-052 inhibited the JAK1, JAK2, JAK3, and tyrosine kinase (Tyk)2 enzymes in an adenosine triphosphate (ATP)-competitive manner and inhibited cytokine signaling evoked by IL-2, IL-6, IL-23, granulocyte/macrophage colony-stimulating factor, and IFN-alpha. delgocitinib 9-16 Janus kinase 1 Homo sapiens 31-35 25387665-5 2015 RESULTS: JTE-052 inhibited the JAK1, JAK2, JAK3, and tyrosine kinase (Tyk)2 enzymes in an adenosine triphosphate (ATP)-competitive manner and inhibited cytokine signaling evoked by IL-2, IL-6, IL-23, granulocyte/macrophage colony-stimulating factor, and IFN-alpha. Adenosine Triphosphate 90-112 Janus kinase 1 Homo sapiens 31-35 25453808-4 2014 Further modifications led to the discovery of an orally bioavailable (2-fluoro-2-methylcyclopentyl)amino analogue 5g which is a nanomolar inhibitor of both JAK3 and TYK2, functionally selective for the JAK3-JAK1 pathway versus JAK2, and active in a human whole blood assay. 2-fluoro-2-methylcyclopentyl 70-98 Janus kinase 1 Homo sapiens 207-211 25501025-1 2014 Ruxolitinib, a Janus kinase (JAK)-1 and JAK-2 inhibitor, is the first-in-class drug to be licensed in the United States for the treatment of high- and intermediate-risk myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-35 25320076-3 2014 The lead compound, CIMO, suppresses proliferation of HCC cells and achieves this effect by reducing both constitutive and inducible phosphorylation of JAK1, JAK2, and STAT3. cimo 19-23 Janus kinase 1 Homo sapiens 151-155 25696866-2 2014 Furthermore, the oral JAK1/JAK2 inhibitor ruxolitinib, rationally designed to target activated JAK2 signaling in MPN, has been approved by the Food and Drug Administration (FDA) of the United States for the past 3 years for the treatment of intermediate- and advanced-phase myelofibrosis. ruxolitinib 42-53 Janus kinase 1 Homo sapiens 22-26 25520049-3 2014 Ruxolitinib, a JAK-1/2 inhibitor, is effective at controlling splenomegaly and constitutional symptoms, but has limited benefit in reversing bone marrow fibrosis or inducing complete or partial remissions. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-22 24965573-0 2014 The pharmacokinetics, pharmacodynamics, and safety of baricitinib, an oral JAK 1/2 inhibitor, in healthy volunteers. baricitinib 54-65 Janus kinase 1 Homo sapiens 75-82 24965573-1 2014 Baricitinib (also known as LY3009104 or INCB028050), a novel and potent small molecule inhibitor of Janus kinase family of enzymes (JAKs) with selectivity for JAK1 and JAK2, is currently in clinical development for the treatment of rheumatoid arthritis (RA) and other inflammatory disorders. baricitinib 0-11 Janus kinase 1 Homo sapiens 132-136 24965573-1 2014 Baricitinib (also known as LY3009104 or INCB028050), a novel and potent small molecule inhibitor of Janus kinase family of enzymes (JAKs) with selectivity for JAK1 and JAK2, is currently in clinical development for the treatment of rheumatoid arthritis (RA) and other inflammatory disorders. baricitinib 0-11 Janus kinase 1 Homo sapiens 159-163 24965573-1 2014 Baricitinib (also known as LY3009104 or INCB028050), a novel and potent small molecule inhibitor of Janus kinase family of enzymes (JAKs) with selectivity for JAK1 and JAK2, is currently in clinical development for the treatment of rheumatoid arthritis (RA) and other inflammatory disorders. baricitinib 27-36 Janus kinase 1 Homo sapiens 132-136 24965573-1 2014 Baricitinib (also known as LY3009104 or INCB028050), a novel and potent small molecule inhibitor of Janus kinase family of enzymes (JAKs) with selectivity for JAK1 and JAK2, is currently in clinical development for the treatment of rheumatoid arthritis (RA) and other inflammatory disorders. baricitinib 27-36 Janus kinase 1 Homo sapiens 159-163 24013646-3 2014 In this study, the function of JAKs in DCs was investigated with tofacitinib. tofacitinib 65-76 Janus kinase 1 Homo sapiens 31-35 24013646-11 2014 CONCLUSIONS: Tofacitinib, a JAK1/JAK3 inhibitor, affected the activities of human DCs. tofacitinib 13-24 Janus kinase 1 Homo sapiens 28-32 25043171-2 2014 Ruxolitinib, the first-in-class oral small molecule JAK1/2 inhibitor, has demonstrated clinical efficacy and shown a potential overall survival benefit in two randomized phase III clinical trials. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 52-58 25369270-0 2014 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. triazolopyridines 0-17 Janus kinase 1 Homo sapiens 31-35 25369270-3 2014 Having identified JAK1 as a possible new target for arthritis at Galapagos, the compound library was screened against JAK1, resulting in the identification of a triazolopyridine-based series of inhibitors represented by 3. CP-808844 161-177 Janus kinase 1 Homo sapiens 18-22 25390891-7 2014 More specifically, the JAK1/2 inhibitor Ruxolitinib enhances the growth of viruses that are sensitive to IFN due to (i) loss of function of the viral IFN antagonist (due to mutation or species-specific constraints) or (ii) mutations/host cell constraints that slow virus spread such that it can be controlled by the IFN response. ruxolitinib 40-51 Janus kinase 1 Homo sapiens 23-29 25131802-0 2014 Initial solid tumor testing (stage 1) of AZD1480, an inhibitor of Janus kinases 1 and 2 by the pediatric preclinical testing program. AZD 1480 41-48 Janus kinase 1 Homo sapiens 66-87 25131802-1 2014 BACKGROUND: AZD1480 is an ATP competitive inhibitor of Janus kinases 1 and 2 (JAK1, 2) that has been shown to inhibit the growth of solid tumor models. AZD 1480 12-19 Janus kinase 1 Homo sapiens 55-76 25131802-1 2014 BACKGROUND: AZD1480 is an ATP competitive inhibitor of Janus kinases 1 and 2 (JAK1, 2) that has been shown to inhibit the growth of solid tumor models. AZD 1480 12-19 Janus kinase 1 Homo sapiens 78-82 25131802-1 2014 BACKGROUND: AZD1480 is an ATP competitive inhibitor of Janus kinases 1 and 2 (JAK1, 2) that has been shown to inhibit the growth of solid tumor models. Adenosine Triphosphate 26-29 Janus kinase 1 Homo sapiens 55-76 25131802-1 2014 BACKGROUND: AZD1480 is an ATP competitive inhibitor of Janus kinases 1 and 2 (JAK1, 2) that has been shown to inhibit the growth of solid tumor models. Adenosine Triphosphate 26-29 Janus kinase 1 Homo sapiens 78-82 25217444-3 2014 The Jak inhibitor tofacitinib (CP-690,550) which is an approved drug for rheumatoid arthritis was originally introduced as a selective Jak3 inhibitor, however, it also inhibits Jak1 and Jak2. tofacitinib 18-29 Janus kinase 1 Homo sapiens 177-181 25217444-3 2014 The Jak inhibitor tofacitinib (CP-690,550) which is an approved drug for rheumatoid arthritis was originally introduced as a selective Jak3 inhibitor, however, it also inhibits Jak1 and Jak2. tofacitinib 31-37 Janus kinase 1 Homo sapiens 177-181 25232526-2 2014 Tofacitinib, an orally administered Janus kinase (JAK) inhibitor, decreases T-cell activation, pro-inflammatory cytokine production, and cytokine signaling by inhibiting binding of type I cytokine receptors family and gamma-chain cytokines to paired JAK1/JAK3 receptors. tofacitinib 0-11 Janus kinase 1 Homo sapiens 250-254 25369270-3 2014 Having identified JAK1 as a possible new target for arthritis at Galapagos, the compound library was screened against JAK1, resulting in the identification of a triazolopyridine-based series of inhibitors represented by 3. CP-808844 161-177 Janus kinase 1 Homo sapiens 118-122 25369270-4 2014 Optimization within this chemical series led to identification of GLPG0634 (65, filgotinib), a selective JAK1 inhibitor currently in phase 2B development for RA and phase 2A development for Crohn"s disease (CD). GLPG0634 80-90 Janus kinase 1 Homo sapiens 105-109 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 Janus kinase 1 Homo sapiens 81-89 25526003-1 2014 Ruxolitinib, a small molecule JAK-1/2 inhibitor, was approved by the U.S. Food and Drug Administration (FDA) in November 2011, as the first therapeutic for the treatment of intermediate and high-risk myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 30-37 25101566-4 2014 The phosphorylation of Janus-activated kinases (JAKs) 1 and 2 and Src was also suppressed by lupeol. lupeol 93-99 Janus kinase 1 Homo sapiens 23-61 25226283-5 2014 DCE and CS can trigger S-glutathionylation of various substrates, including the transcription factor STAT3 and JAK1/2 proteins. dehydrocostus lactone 0-3 Janus kinase 1 Homo sapiens 111-117 25226283-5 2014 DCE and CS can trigger S-glutathionylation of various substrates, including the transcription factor STAT3 and JAK1/2 proteins. costunolide 8-10 Janus kinase 1 Homo sapiens 111-117 25197973-7 2014 Ruxolitinib was then docked into the ligand-binding pocket of a previously solved JAK1 structure. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 82-86 25197973-8 2014 From the docking result, Ruxolitinib also binds JAK1 as a type I inhibitor, with more interactions and a higher shape complementarity with the ligand-binding pocket of JAK1 compared to that of c-Src. ruxolitinib 25-36 Janus kinase 1 Homo sapiens 48-52 25197973-8 2014 From the docking result, Ruxolitinib also binds JAK1 as a type I inhibitor, with more interactions and a higher shape complementarity with the ligand-binding pocket of JAK1 compared to that of c-Src. ruxolitinib 25-36 Janus kinase 1 Homo sapiens 168-172 24814730-8 2014 Similarly, the synthetic allopregnanolone analog, ganaxolone (GNX), repressed GAT-2, JAK-1 and STAT-1 expression in activated macrophage lineage cells (p<0.05). Pregnanolone 25-41 Janus kinase 1 Homo sapiens 85-90 25129481-8 2014 Notably, three patients treated with oral ruxolitinib, an inhibitor of JAK1 and JAK2, achieved near-complete hair regrowth within 5 months of treatment, suggesting the potential clinical utility of JAK inhibition in human AA. ruxolitinib 42-53 Janus kinase 1 Homo sapiens 71-75 24818516-7 2014 JAK inhibitors differ in isoform specificity profiles, with good efficacy achievable by selective inhibition of either JAK1 (filgotinib or INCB-039110) or JAK3 (decernotinib). GLPG0634 125-135 Janus kinase 1 Homo sapiens 119-123 25180155-5 2014 Eventually, he was treated with ruxolitinib, an FDA-approved JAK1/2 inhibitor, which resulted in dramatic improvement of his blood counts. ruxolitinib 32-43 Janus kinase 1 Homo sapiens 61-67 24814730-8 2014 Similarly, the synthetic allopregnanolone analog, ganaxolone (GNX), repressed GAT-2, JAK-1 and STAT-1 expression in activated macrophage lineage cells (p<0.05). ganaxolone 50-60 Janus kinase 1 Homo sapiens 85-90 24814730-8 2014 Similarly, the synthetic allopregnanolone analog, ganaxolone (GNX), repressed GAT-2, JAK-1 and STAT-1 expression in activated macrophage lineage cells (p<0.05). ganaxolone 62-65 Janus kinase 1 Homo sapiens 85-90 24778152-6 2014 Incubation of CLL cells with the JAK1/2 inhibitor ruxolitinib inhibited IgM-induced STAT3 phosphorylation and induced apoptosis of IgM-stimulated but not unstimulated CLL cells in a dose- and time-dependent manner. ruxolitinib 50-61 Janus kinase 1 Homo sapiens 33-39 24867113-5 2014 Ruxolitinib, a Janus kinase (JAK) 1 and 2 inhibitor, is the first therapy to be approved by the U.S. Food and Drug Administration for intermediate- or high-risk MF. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-41 24813092-8 2014 Two of the five tumors displayed significantly altered kinase activity in the TMZ resistant xenolines and network modeling indicated PKC, JAK1, PI3K, CDK2, and VEGFR as potential mediators of this resistance. Temozolomide 78-81 Janus kinase 1 Homo sapiens 138-142 24766055-8 2014 Resultant research in targeting the JAK/STAT pathway led to the approval of ruxolitinib, a JAK1/JAK2 inhibitor with activity in MPNs. ruxolitinib 76-87 Janus kinase 1 Homo sapiens 91-95 24614195-9 2014 In conclusion, CTP-HBcAg(18-27)-Tapasin fusion protein could enhance not only the percentages of CTLs but also induce robust specific CTL activity and inhibits hepatitis B virus replication in vivo, which was associated with activation of the JAK/STAT signaling pathway. Cytidine Triphosphate 15-18 Janus kinase 1 Homo sapiens 243-246 24523387-9 2014 Oxalate treatment also activated the IL-2Rbeta signaling pathway (JAK1/STAT5 phosphorylation). Oxalates 0-7 Janus kinase 1 Homo sapiens 66-70 24764577-8 2014 Moreover, the JAK1/2 inhibitor ruxolitinib potently inhibited the anti-CD3-dependent production of IFN-gamma, a marker of the differentiation of Th cells along the tumor-inhibitory Th1 pathway. ruxolitinib 31-42 Janus kinase 1 Homo sapiens 14-20 24583800-6 2014 The JAK1/2 inhibitor ruxolitinib and the JAK3 inhibitor tofacitinib were recently approved for the treatment of myelofibrosis and rheumatoid arthritis, respectively, and additional ATP-competitive JAK inhibitors are in clinical development. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 24458439-1 2014 The JAK1/JAK2 inhibitor ruxolitinib produced significant reductions in splenomegaly and symptomatic burden and improved survival in patients with myelofibrosis (MF), irrespective of their JAK2 mutation status, in 2 phase III studies against placebo (COMFORT-I) and best available therapy (COMFORT-II). ruxolitinib 24-35 Janus kinase 1 Homo sapiens 4-8 24333736-6 2014 Treatment with the protein tyrosine phosphatase (PTP) inhibitor pervanadate treatment reversed the CPS-induced down-regulation of JAK1/2 and STAT3, thereby suggesting the involvement of a PTP. pervanadate 64-75 Janus kinase 1 Homo sapiens 130-136 24398382-0 2014 Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group. propargylic alcohol 7-26 Janus kinase 1 Homo sapiens 85-89 24386992-2 2014 In EP-2634185 Sareum claims 5-anilino-2-(2-halophenyl)-oxazole-4-carboxamide derivatives which are shown to be nanomolar potency Tyk2 inhibitors with 10 - 100-fold selectivity over JAK1, JAK2 and JAK3. 5-anilino-2-(2-halophenyl)-oxazole-4-carboxamide 28-76 Janus kinase 1 Homo sapiens 181-185 24258498-0 2014 A phase 2 study of ruxolitinib, an oral JAK1 and JAK2 Inhibitor, in patients with advanced polycythemia vera who are refractory or intolerant to hydroxyurea. ruxolitinib 19-30 Janus kinase 1 Homo sapiens 40-44 24258498-3 2014 Ruxolitinib, an oral JAK1/JAK2 inhibitor, is active in preclinical models of PV. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-25 24292520-1 2014 The Janus-activated kinase 1 (JAK1) and JAK2 inhibitor ruxolitinib is effective in decreasing symptomatic splenomegaly and myelofibrosis (MF)-related symptoms. ruxolitinib 55-66 Janus kinase 1 Homo sapiens 4-28 24589536-2 2014 SUMMARY: Ruxolitinib, an oral tyrosine kinase inhibitor that targets the Janus-associated kinases (JAKs) 1 and 2, has been recently approved for the treatment of patients with intermediate- or high-risk myelofibrosis. ruxolitinib 9-20 Janus kinase 1 Homo sapiens 73-112 24589536-10 2014 CONCLUSION: By directly targeting both JAK1 and JAK2 through small-molecule inhibition, ruxolitinib elicits a reduction in splenomegaly and disease-related symptoms in patients with intermediate- or high-risk myelofibrosis while maintaining an acceptable toxicity profile and a low treatment-discontinuation rate. ruxolitinib 88-99 Janus kinase 1 Homo sapiens 39-43 24398382-0 2014 Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group. 1H-Indazole-7-carboxamide 57-79 Janus kinase 1 Homo sapiens 85-89 24398382-2 2014 In this study, through pairwise comparison and 3D alignment of the JAK isozyme structures bound to the same inhibitor molecule, we reasoned that an alkynol functionality would serve as an isozyme-specific probe group, which would enable the resulting inhibitor to differentiate the ATP-binding site of JAK1 from those of other isozymes. alkynol 148-155 Janus kinase 1 Homo sapiens 302-306 24398382-2 2014 In this study, through pairwise comparison and 3D alignment of the JAK isozyme structures bound to the same inhibitor molecule, we reasoned that an alkynol functionality would serve as an isozyme-specific probe group, which would enable the resulting inhibitor to differentiate the ATP-binding site of JAK1 from those of other isozymes. Adenosine Triphosphate 282-285 Janus kinase 1 Homo sapiens 302-306 24398382-3 2014 The 3-alkynolyl-5-(4"-indazolyl)indazole-7-carboxamide derivatives were thus prepared, and in vitro evaluation of their inhibitory activity against the JAK isozymes revealed that the propargyl alcohol functionality endowed the 5-(4"-indazolyl)indazole-7-carboxamide scaffold with JAK1 selectivity over other JAK isozymes, particularly JAK2. 3-alkynolyl-5-(4"-indazolyl)indazole-7-carboxamide 4-54 Janus kinase 1 Homo sapiens 280-284 24398382-3 2014 The 3-alkynolyl-5-(4"-indazolyl)indazole-7-carboxamide derivatives were thus prepared, and in vitro evaluation of their inhibitory activity against the JAK isozymes revealed that the propargyl alcohol functionality endowed the 5-(4"-indazolyl)indazole-7-carboxamide scaffold with JAK1 selectivity over other JAK isozymes, particularly JAK2. propargyl alcohol 183-200 Janus kinase 1 Homo sapiens 280-284 24398382-3 2014 The 3-alkynolyl-5-(4"-indazolyl)indazole-7-carboxamide derivatives were thus prepared, and in vitro evaluation of their inhibitory activity against the JAK isozymes revealed that the propargyl alcohol functionality endowed the 5-(4"-indazolyl)indazole-7-carboxamide scaffold with JAK1 selectivity over other JAK isozymes, particularly JAK2. 5-(4"-indazolyl)indazole-7-carboxamide 16-54 Janus kinase 1 Homo sapiens 280-284 24501543-7 2014 The JAK1/JAK2 inhibitor ruxolitinib is effective in improving splenomegaly, MF-related symptoms, and quality-of-life measures. ruxolitinib 24-35 Janus kinase 1 Homo sapiens 4-8 24261748-1 2014 Selective JAK1 inhibitors based on a 3-aminopyrazole-4-carboxamide scaffold. 3-Amino-1H-pyrazole-4-carboxamide 37-66 Janus kinase 1 Homo sapiens 10-14 24754420-8 2014 Ruxolitinib, an oral selective inhibitor of JAK1 and JAK2 kinases, has shown high efficacy in patients with high-risk PMF (or with myelofibrosis following polycythemia vera or essential thrombocythemia) to ameliorate disease symptoms and to reduce splenomegaly in randomized trials COMFORT-I and COMFORT-II. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 44-48 24763226-8 2014 Moreover, uPAR-mediated growth and motility is partially abolished upon treatment with the Jak1/Jak2 inhibitor INCB018424. ruxolitinib 111-121 Janus kinase 1 Homo sapiens 91-95 23387973-8 2014 Among genes up-regulated by Y15 and temozolomide more significantly than by each agent alone were: COX7B; interferon, gamma-inducible transcript: IFI16; DDIT4; GADD45G and down-regulated: KIF3A, AKT1; ABL; JAK1, GLI3 and ALDH1A3. Temozolomide 36-48 Janus kinase 1 Homo sapiens 206-210 24419350-2 2014 Ruxolitinib and tofacitinib are JAK1/2 inhibitors that are FDA approved for rheumatoid arthritis and myelofibrosis, respectively, but their therapeutic application for treatment of HIV infection was unexplored. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 32-36 24419350-2 2014 Ruxolitinib and tofacitinib are JAK1/2 inhibitors that are FDA approved for rheumatoid arthritis and myelofibrosis, respectively, but their therapeutic application for treatment of HIV infection was unexplored. tofacitinib 16-27 Janus kinase 1 Homo sapiens 32-36 24583775-0 2014 4-Amino-pyrrolopyridine-5-carboxamide: a novel scaffold for JAK1-selective inhibitors. 4-amino-pyrrolopyridine-5-carboxamide 0-37 Janus kinase 1 Homo sapiens 60-64 24583775-2 2014 In this study, a novel 4-amino-1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold was designed through structural modification of the potent JAK1-selective inhibitor, C2-methyl imidazopyrrolopyridine. SCHEMBL12876743 23-70 Janus kinase 1 Homo sapiens 139-143 24583775-2 2014 In this study, a novel 4-amino-1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold was designed through structural modification of the potent JAK1-selective inhibitor, C2-methyl imidazopyrrolopyridine. c2-methyl imidazopyrrolopyridine 165-197 Janus kinase 1 Homo sapiens 139-143 24583775-3 2014 Among the series studied, the 4-(2-aminoethyl)amino-pyrrolopyridine derivative, 2j, exhibited a significant 24.7-fold JAK1/JAK2 selectivity along with reasonable inhibitory activity against JAK1 (IC50=2.2 microM). 4-(2-aminoethyl)amino-pyrrolopyridine 30-67 Janus kinase 1 Homo sapiens 118-122 24583775-3 2014 Among the series studied, the 4-(2-aminoethyl)amino-pyrrolopyridine derivative, 2j, exhibited a significant 24.7-fold JAK1/JAK2 selectivity along with reasonable inhibitory activity against JAK1 (IC50=2.2 microM). 4-(2-aminoethyl)amino-pyrrolopyridine 30-67 Janus kinase 1 Homo sapiens 190-194 25027606-6 2014 Tofacitinib, an oral inhibitor of JAK3, JAK1, and, to a lesser degree, JAK2, approved for the treatment of rheumatoid arthritis in several countries, has demonstrated positive results in psoriasis in phase II studies. tofacitinib 0-11 Janus kinase 1 Homo sapiens 40-44 27128228-1 2014 Hepatic and renal impairment studies were conducted with ruxolitinib, a JAK1&2 inhibitor that is cleared predominantly by metabolism. ruxolitinib 57-68 Janus kinase 1 Homo sapiens 72-82 24368888-1 2013 PURPOSE: Ruxolitinib is an oral Janus kinase (JAK) 1/JAK2 inhibitor approved in the US for the treatment of intermediate-or high-risk myelofibrosis (MF). ruxolitinib 9-20 Janus kinase 1 Homo sapiens 32-52 24147573-1 2014 A series of pyrrolo[2,3-d]pyrimidine derivatives have previously been claimed as Janus kinase (JAK) 1 selective inhibitors. Pyrrolo(2,3-d)pyrimidine 12-36 Janus kinase 1 Homo sapiens 81-101 24883332-4 2014 Tofacitinib, an oral or topically administered JAK1 and JAK3 inhibitor, and ruxolitinib, a topical JAK1 and JAK2 inhibitor, have been most extensively studied in psoriasis, and both improved clinical symptoms of psoriasis. tofacitinib 0-11 Janus kinase 1 Homo sapiens 47-51 24883332-4 2014 Tofacitinib, an oral or topically administered JAK1 and JAK3 inhibitor, and ruxolitinib, a topical JAK1 and JAK2 inhibitor, have been most extensively studied in psoriasis, and both improved clinical symptoms of psoriasis. ruxolitinib 76-87 Janus kinase 1 Homo sapiens 99-103 24195509-11 2014 The inhibition of JAK1 phosphorylation seemed sufficient to allow INCB018424-mediated apoptosis. ruxolitinib 66-76 Janus kinase 1 Homo sapiens 18-22 24756798-1 2014 Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of JAK1 and JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 97-101 24756798-1 2014 Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of JAK1 and JAK2. ruxolitinib 31-41 Janus kinase 1 Homo sapiens 97-101 24756798-1 2014 Ruxolitinib, formerly known as INCB018424 or INC424, is a potent and selective oral inhibitor of JAK1 and JAK2. ruxolitinib 45-51 Janus kinase 1 Homo sapiens 97-101 24158701-3 2013 EXPERIMENTAL DESIGN: JAK1 and JAK2 were inhibited by AZD1480 or siRNAs, and the effect of inhibition of JAK gene family on SCLC cell viability was evaluated. AZD 1480 53-60 Janus kinase 1 Homo sapiens 21-25 24238036-3 2013 In 2 randomized phase III studies, the Janus kinase (JAK) 1/JAK2 inhibitor ruxolitinib significantly improved splenomegaly and disease-related symptoms compared with placebo (Controlled Myelofibrosis Study with Oral JAK Inhibitor Treatment [COMFORT-I]) or best available therapy (COMFORT-II) in patients with intermediate-2 or high-risk MF. ruxolitinib 75-86 Janus kinase 1 Homo sapiens 39-59 24174625-1 2013 Ruxolitinib is a potent Janus kinase (JAK)1/JAK2 inhibitor that has demonstrated rapid reductions in splenomegaly and marked improvement in disease-related symptoms and quality of life in patients with myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 24-43 23968543-6 2013 The JAK inhibitors CP-690,550 and INCB028050 both suppressed activation of JAK-1/-2/-3 and downstream STAT-1/-3/-5, as well as the expression levels of target proinflammatory genes (MCP-I, SAA1/2) in oncostatin-M (OSM)-stimulated rheumatoid synovial fibroblasts. tofacitinib 19-25 Janus kinase 1 Homo sapiens 75-80 23968543-6 2013 The JAK inhibitors CP-690,550 and INCB028050 both suppressed activation of JAK-1/-2/-3 and downstream STAT-1/-3/-5, as well as the expression levels of target proinflammatory genes (MCP-I, SAA1/2) in oncostatin-M (OSM)-stimulated rheumatoid synovial fibroblasts. baricitinib 34-44 Janus kinase 1 Homo sapiens 75-80 24501689-9 2013 In stark contrast, we showed that ruxolitinib, a JAK1/JAK2-selective tyrosine kinase inhibitor used to treat patients with myelofibrosis, dramatically impaired JAK1-STAT signaling downstream of all IHCA-associated gp130 mutants. ruxolitinib 34-45 Janus kinase 1 Homo sapiens 49-53 24056820-0 2013 Resolution of bone marrow fibrosis in a patient receiving JAK1/JAK2 inhibitor treatment with ruxolitinib. ruxolitinib 93-104 Janus kinase 1 Homo sapiens 58-62 24056820-1 2013 UNLABELLED: Ruxolitinib, a JAK1/JAK2 inhibitor, is currently the only pharmacological agent approved for the treatment of myelofibrosis. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 27-31 24326545-10 2013 In parallel, clinical trials have been initiated involving the Jak2/3 (Janus kinase-2/3) inhibitor tofacitinib and Jak1/2 inhibitor ruxolitinib to block IL-15 signaling. ruxolitinib 132-143 Janus kinase 1 Homo sapiens 115-121 24501689-9 2013 In stark contrast, we showed that ruxolitinib, a JAK1/JAK2-selective tyrosine kinase inhibitor used to treat patients with myelofibrosis, dramatically impaired JAK1-STAT signaling downstream of all IHCA-associated gp130 mutants. ruxolitinib 34-45 Janus kinase 1 Homo sapiens 160-164 24042009-0 2013 Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors. 8-oxo-pyridopyrimidine 31-53 Janus kinase 1 Homo sapiens 54-58 24021352-6 2013 Its 3-O-Me product, i.e. 8-hydroxy-5-isopropyl-3-methoxy-7-methylbenzo[cd]indol-2(1H)-one, named 3-O-methylthespesilactam, of which the structure was identified by NMR investigations and single-crystal X-ray diffraction analysis, was discovered as a new type of small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells, and selective and potent inhibitor of JAK1 and TYK2. 3-o-me 4-10 Janus kinase 1 Homo sapiens 380-384 24021352-6 2013 Its 3-O-Me product, i.e. 8-hydroxy-5-isopropyl-3-methoxy-7-methylbenzo[cd]indol-2(1H)-one, named 3-O-methylthespesilactam, of which the structure was identified by NMR investigations and single-crystal X-ray diffraction analysis, was discovered as a new type of small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells, and selective and potent inhibitor of JAK1 and TYK2. 8-hydroxy-5-isopropyl-3-methoxy-7-methylbenzo[cd]indol-2( 25-82 Janus kinase 1 Homo sapiens 380-384 24021352-6 2013 Its 3-O-Me product, i.e. 8-hydroxy-5-isopropyl-3-methoxy-7-methylbenzo[cd]indol-2(1H)-one, named 3-O-methylthespesilactam, of which the structure was identified by NMR investigations and single-crystal X-ray diffraction analysis, was discovered as a new type of small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells, and selective and potent inhibitor of JAK1 and TYK2. 1h)-one 82-89 Janus kinase 1 Homo sapiens 380-384 24021352-6 2013 Its 3-O-Me product, i.e. 8-hydroxy-5-isopropyl-3-methoxy-7-methylbenzo[cd]indol-2(1H)-one, named 3-O-methylthespesilactam, of which the structure was identified by NMR investigations and single-crystal X-ray diffraction analysis, was discovered as a new type of small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells, and selective and potent inhibitor of JAK1 and TYK2. 3-o-methylthespesilactam 97-121 Janus kinase 1 Homo sapiens 380-384 24042009-1 2013 A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. 8-oxo-pyridopyrimidine 33-55 Janus kinase 1 Homo sapiens 80-84 24042009-1 2013 A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. Pyridones 110-118 Janus kinase 1 Homo sapiens 80-84 23627915-3 2013 Tofacitinib is an oral janus kinase (JAK) inhibitor that inhibits JAK family kinase members, in particular JAK1 and JAK3, achieving a broad limitation of inflammation by interfering with several cytokine receptors. tofacitinib 0-11 Janus kinase 1 Homo sapiens 107-111 24030211-2 2013 Here, we evaluated VSV oncolysis of a panel of human head and neck cancer cells and showed that VSV resistance in SCC25 and SCC15 cells could be reversed with Janus kinase (JAK) 1/2 inhibitors (JAK inhibitor I and ruxolitinib). ruxolitinib 214-225 Janus kinase 1 Homo sapiens 159-179 24082147-3 2013 SOCS3, the major negative regulator of STAT3, is induced by tyrosine-phosphorylated STAT3 and terminates STAT3 phosphorylation about 2 h after initial exposure of cells to members of the IL-6 family of cytokines by binding cooperatively to the common receptor subunit gp130 and JAKs 1 and 2. Tyrosine 60-68 Janus kinase 1 Homo sapiens 244-290 24283870-1 2013 Ruxolitinib, an oral JAK1 and JAK2 inhibitor, is approved in the US for patients with intermediate or high-risk myelofibrosis (MF), a chronic neoplasm associated with aberrant myeloproliferation, progressive bone marrow fibrosis, splenomegaly, and burdensome symptoms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-25 23891156-4 2013 Reduced phosphorylation of STAT proteins and lower expression levels of the cellular janus kinases Jak1 and Tyk2 were observed in these cell populations, which may account for the impaired JAK-STAT signaling and reduced antiviral responses to rIFNlambda. rifnlambda 243-253 Janus kinase 1 Homo sapiens 99-103 24083419-3 2013 Ruxolitinib (INC424, INCB18424, Jakafi, Jakavi), a JAK1 and JAK2 inhibitor, was approved in November 2011 by the US FDA for the treatment of intermediate- or high-risk MF, and more recently in Europe and Canada for the treatment of MF-related splenomegaly or symptoms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 51-55 24290217-7 2013 Of much interest, a combination of everolimus and the JAK1/2 inhibitor, ruxolitinib, showed strong synergism in inducing cell cycle arrest and blockade of cell proliferation. ruxolitinib 72-83 Janus kinase 1 Homo sapiens 54-60 23639230-5 2013 Also, PTX inhibited phosphorylation of the upstream kinases JAK1 and JAK2 and increased the expression of pSHP2 phosphatase. Pentoxifylline 6-9 Janus kinase 1 Homo sapiens 60-64 23791841-2 2013 Chromosomal sequencing revealed a new Jak1 (p.Ser645Pro) point mutation at the conserved serine of the pseudokinase domain, corresponding to a somatic human mutation (p.Ser646Phe) inducing a constitutive activation of the Janus kinase (JAK)/STAT pathway. Serine 89-95 Janus kinase 1 Homo sapiens 38-42 23454584-3 2013 cAMP-increasing agents rapidly inhibited activation of JAK1 and its substrate STAT3. Cyclic AMP 0-4 Janus kinase 1 Homo sapiens 55-59 23672349-2 2013 Here, we report post-hoc analyses of the impact of ruxolitinib, a potent and selective JAK1 and JAK2 inhibitor, on disease-related symptoms and HRQoL in MF patients from the large phase 3 COMFORT-II study (N = 219). ruxolitinib 51-62 Janus kinase 1 Homo sapiens 87-91 22748021-0 2013 Progesterone activates Janus Kinase 1/2 and activators of transcription 1 (JAK1-2/STAT1) pathway in human spermatozoa. Progesterone 0-12 Janus kinase 1 Homo sapiens 75-81 22748021-6 2013 Progesterone (5 mum) leads to phosphorylation of JAK1, JAK2 and STAT1 in a time-dependent manner. Progesterone 0-12 Janus kinase 1 Homo sapiens 49-53 22748021-8 2013 We conclude that in human spermatozoa, the JAK1/2 pathway is activated upon capacitation and is further modulated by progesterone; the biological processes controlled by this pathway in sperm need to be elucidated. Progesterone 117-129 Janus kinase 1 Homo sapiens 43-49 23570265-4 2013 Tofacitinib is a novel synthetic DMARD that selectively inhibits Janus kinases (JAKs), particularly JAK1 and JAK3. tofacitinib 0-11 Janus kinase 1 Homo sapiens 80-84 23570265-4 2013 Tofacitinib is a novel synthetic DMARD that selectively inhibits Janus kinases (JAKs), particularly JAK1 and JAK3. tofacitinib 0-11 Janus kinase 1 Homo sapiens 100-104 23670175-2 2013 Of these, the JAK1/2 inhibitor, ruxolitinib (INCB018424, Incyte Corporation) was recently approved for the treatment of patients with myelofibrosis (MF). ruxolitinib 32-43 Janus kinase 1 Homo sapiens 14-20 23459451-2 2013 We conducted a Phase 1/2 trial of CYT387, a potent JAK1/2 inhibitor, in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia MF. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 34-40 Janus kinase 1 Homo sapiens 51-57 22717332-4 2013 IFN-alpha potently induced nitric oxide synthase (iNOS) and nitric oxide (NO) release and down-regulated haem oxygenase-1 (HO-1) expression, which could be dampened by Janus kinase 1 (JAK1) and c-Jun NH2-terminal kinase (JNK) inhibition, respectively. nitric 27-33 Janus kinase 1 Homo sapiens 168-182 23656643-7 2013 A patient with CNL carrying a JAK-activating CSF3R mutation had marked clinical improvement after the administration of the JAK1/2 inhibitor ruxolitinib. ruxolitinib 141-152 Janus kinase 1 Homo sapiens 124-130 23406773-4 2013 Ruxolitinib is an oral JAK1 and JAK2 inhibitor that has recently been approved for the treatment of myelofibrosis and has been tested against other hematologic malignancies. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 23-27 23367873-2 2013 Progression in the field has taken a recent step forward with the approval of ruxolitinib (Jakafi), a selective inhibitor of JAK1/2 and very recently tofacitinib (Xeljanz), a pan-JAK inhibitor. ruxolitinib 78-89 Janus kinase 1 Homo sapiens 125-131 23367873-12 2013 EXPERT OPINION: JAK inhibitor therapy is entering a significant new era with the advent on the market of the JAK1/2 inhibitor ruxolitinib and the pan-JAK inhibitor tofacitinib, with unprecedented speed of development. ruxolitinib 126-137 Janus kinase 1 Homo sapiens 109-115 22875628-2 2013 Here we assess the JAK1/2 inhibitor ruxolitinib as therapy for patients with JAK2-rearrangement associated myeloproliferative neoplasms (MPN). ruxolitinib 36-47 Janus kinase 1 Homo sapiens 19-25 22717332-4 2013 IFN-alpha potently induced nitric oxide synthase (iNOS) and nitric oxide (NO) release and down-regulated haem oxygenase-1 (HO-1) expression, which could be dampened by Janus kinase 1 (JAK1) and c-Jun NH2-terminal kinase (JNK) inhibition, respectively. nitric 27-33 Janus kinase 1 Homo sapiens 184-188 24252238-7 2013 Ruxolitinib (Jakafi), a non-selective inhibitor of JAK1 & 2, has been approved by FDA for patients with intermediate to high risk primary or secondary myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 51-55 23515130-5 2013 Tofacitinib is one of the first JAK inhibitors tested and mainly interacts with JAK1 and JAK3. tofacitinib 0-11 Janus kinase 1 Homo sapiens 80-84 24252238-7 2013 Ruxolitinib (Jakafi), a non-selective inhibitor of JAK1 & 2, has been approved by FDA for patients with intermediate to high risk primary or secondary myelofibrosis. Adenosine Monophosphate 57-60 Janus kinase 1 Homo sapiens 51-55 23847256-1 2013 BACKGROUND: AZD1480 is a novel agent that inhibits Janus-associated kinases 1 and 2 (JAK1 and JAK2). AZD 1480 12-19 Janus kinase 1 Homo sapiens 85-89 24319228-5 2013 The JAK1/JAK2 inhibitor ruxolitinib is approved for treatment of MF in North America and Europe and other lead JAK inhibitors discussed herein (fedratinib [SAR302503], momelotinib [CYT387], and pacritinib [SB1518]), have entered advanced phases of trial investigation. ruxolitinib 24-35 Janus kinase 1 Homo sapiens 4-8 23236554-4 2013 We show that the tyrosine phosphorylation of PKR induced by either bacterial RNA or poly I:C is impaired in mutant cells lacking TYK2, JAK1, or JAK2 kinases. Tyrosine 17-25 Janus kinase 1 Homo sapiens 135-139 23214979-2 2013 We optimized a new inhibitor scaffold, 3-amido-5-cyclopropylpyrrolopyrazines, to a potent example with reasonable kinome selectivity, including selectivity for JAK3 versus JAK1, and good biopharmaceutical properties. 3-amido-5-cyclopropylpyrrolopyrazines 39-76 Janus kinase 1 Homo sapiens 172-176 23124025-10 2013 As evidence of differential regulation of gene function by IL-4 and IL-13, we further report that MAO-A-mediated reactive oxygen species generation is influenced by different Jaks. Reactive Oxygen Species 113-136 Janus kinase 1 Homo sapiens 175-179 23307549-10 2013 Ruxolitinib is a small-molecule inhibitor of JAK1 and JAK2 and recently became the first drug approved by the United States Food and Drug Administration for the treatment of symptomatic intermediate- or high-risk myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 45-49 23061804-1 2012 Ruxolitinib is a selective inhibitor of Janus kinases (JAK) 1 and 2, which are involved in the signalling pathway of various cytokines and growth factors essential to haematopoiesis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 40-67 23107482-0 2012 Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2. imidazo-pyrrolopyridine 45-68 Janus kinase 1 Homo sapiens 69-73 23107482-1 2012 Herein we describe our successful efforts in obtaining C-2 substituted imidazo-pyrrolopyridines with improved JAK1 selectivity relative to JAK2 by targeting an amino acid residue that differs between the two isoforms (JAK1: E966; JAK2: D939). imidazo-pyrrolopyridines 71-95 Janus kinase 1 Homo sapiens 110-114 23107482-1 2012 Herein we describe our successful efforts in obtaining C-2 substituted imidazo-pyrrolopyridines with improved JAK1 selectivity relative to JAK2 by targeting an amino acid residue that differs between the two isoforms (JAK1: E966; JAK2: D939). imidazo-pyrrolopyridines 71-95 Janus kinase 1 Homo sapiens 218-222 22939972-0 2012 Depletion of cellular glutathione modulates LIF-induced JAK1-STAT3 signaling in cardiac myocytes. Glutathione 22-33 Janus kinase 1 Homo sapiens 56-60 22939972-3 2012 Therefore, the present study was undertaken to directly test the hypothesis that JAK1 signaling by the IL-6-type cytokines in cardiac myocytes is impaired by glutathione (GSH) depletion, since this tripeptide is one of the major anti-oxidant molecules and redox-buffers in cells. Glutathione 158-169 Janus kinase 1 Homo sapiens 81-85 22939972-3 2012 Therefore, the present study was undertaken to directly test the hypothesis that JAK1 signaling by the IL-6-type cytokines in cardiac myocytes is impaired by glutathione (GSH) depletion, since this tripeptide is one of the major anti-oxidant molecules and redox-buffers in cells. Glutathione 171-174 Janus kinase 1 Homo sapiens 81-85 23372833-6 2013 In addition, resveratrol suppressed constitutively active STAT3 in all the cell lines and inhibited JAK2 phosphorylation but had no effect on other upstream mediators of STAT3 activation, such as PTEN, TYK2, and JAK1. Resveratrol 13-24 Janus kinase 1 Homo sapiens 212-216 23391678-0 2013 Ruxolitinib: an oral Janus kinase 1 and Janus kinase 2 inhibitor in the management of myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-35 23391678-5 2013 In November 2011, ruxolitinib, an inhibitor of JAK1 and JAK2, was approved by the US Food and Drug Administration for the treatment of intermediate- or high-risk MF, including primary MF, post-PV MF, and post-ET MF. ruxolitinib 18-29 Janus kinase 1 Homo sapiens 47-51 23186315-3 2012 AREAS COVERED: This review describes the pathogenesis, clinical features and current treatment of MF, clinical data for ruxolitinib, a potent oral JAK1/JAK2 inhibitor and the only therapy approved for the treatment of MF, and agents in development for the treatment of MF. ruxolitinib 120-131 Janus kinase 1 Homo sapiens 147-151 22939972-3 2012 Therefore, the present study was undertaken to directly test the hypothesis that JAK1 signaling by the IL-6-type cytokines in cardiac myocytes is impaired by glutathione (GSH) depletion, since this tripeptide is one of the major anti-oxidant molecules and redox-buffers in cells. tripeptide K-26 198-208 Janus kinase 1 Homo sapiens 81-85 22939972-7 2012 Addition of glutathione monoethyl ester, which is cleaved intracellularly to GSH, prevented attenuation of LIF-induced JAK1 and STAT3 activation, as did the reductant N-acetyl-cysteine. S-ethyl glutathione 12-39 Janus kinase 1 Homo sapiens 119-123 22939972-7 2012 Addition of glutathione monoethyl ester, which is cleaved intracellularly to GSH, prevented attenuation of LIF-induced JAK1 and STAT3 activation, as did the reductant N-acetyl-cysteine. Glutathione 77-80 Janus kinase 1 Homo sapiens 119-123 22972985-8 2012 Finally, pharmacologic inhibition of IFNgammaR signaling with inhibitors of JAK1/JAK2, which are mediators of IFNgammaR signaling, results in the decreased expression of CXCR3 and reduced GVHD and improved survival after allo-HSCT and this effect is mediated by altered trafficking of Tconv to GVHD target organs. tconv 285-290 Janus kinase 1 Homo sapiens 76-80 22172707-5 2012 Following treatment with 5-FU, JAK1 and STAT5 immunoreactivities were decreased in MCF-7 cells in comparison with both gemcitabine-treated and non-treated groups. Fluorouracil 25-29 Janus kinase 1 Homo sapiens 31-35 22763125-6 2012 We also found that PTP-MEG2 DA mutant preferentially associated with Janus kinase 1 (JAK1) but not with other JAK kinases (Tyk2 and JAK2) present in ECs and regulated JAK1 tyrosine phosphorylation. Tyrosine 172-180 Janus kinase 1 Homo sapiens 69-83 23042420-13 2012 Ruxolitinib is the first JAK1/2 inhibitor approved by the Food and Drug Administration (FDA) for the treatment of patients with intermediate- or high-risk MF. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 25-31 23055361-3 2012 Most data are available on the JAK inhibitors, the so called "ATP mimetics" for the treatment of MF. Adenosine Triphosphate 62-65 Janus kinase 1 Homo sapiens 31-34 23055361-4 2012 Recent data from two large phase-III studies showed that the JAK1 /2 inhibitor Ruxolitinib is very effective in the reduction of spleen size and the improvement of quality of life in MF patients. ruxolitinib 79-90 Janus kinase 1 Homo sapiens 61-65 22971156-6 2012 EXPERT OPINION: The recent disclosure of the clinical efficacy of a selective JAK1 inhibitor (GLPG-0634) in rheumatoid arthritis and detailed disclosure of the some potent and highly selective JAK1 inhibitors provide a clear stimulus for further activity in this area. GLPG0634 94-103 Janus kinase 1 Homo sapiens 78-82 22971156-6 2012 EXPERT OPINION: The recent disclosure of the clinical efficacy of a selective JAK1 inhibitor (GLPG-0634) in rheumatoid arthritis and detailed disclosure of the some potent and highly selective JAK1 inhibitors provide a clear stimulus for further activity in this area. GLPG0634 94-103 Janus kinase 1 Homo sapiens 193-197 22763125-6 2012 We also found that PTP-MEG2 DA mutant preferentially associated with Janus kinase 1 (JAK1) but not with other JAK kinases (Tyk2 and JAK2) present in ECs and regulated JAK1 tyrosine phosphorylation. Tyrosine 172-180 Janus kinase 1 Homo sapiens 167-171 23051187-0 2012 Ruxolitinib, an oral JAK1 and JAK2 inhibitor, in myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-25 23051187-3 2012 Ruxolitinib is the first JAK1 and JAK2 inhibitor to be approved by the US Food and Drug Administration. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 25-29 23051187-7 2012 The JAK1 and JAK2 inhibitor ruxolitinib has shown promising results in pre-clinical and clinical trials. ruxolitinib 28-39 Janus kinase 1 Homo sapiens 4-8 22961117-6 2012 Inhibition of the signal transducer and activator of transcription 3 tyrosine phosphorylation was found to be achieved through suppression of JAK1 and JAK2. Tyrosine 69-77 Janus kinase 1 Homo sapiens 142-146 23170143-3 2012 Recent studies have shown that cerulein-activated nicotinamide adenine dinucleotide phosphate oxidase elicits reactive oxygen species, which trigger the phosphorylation of the JAK1, STAT1, and STAT3 proteins and induce the production of inflammatory cytokines, such as tumor necrosis factor-alpha, interleukin (IL)-1beta, and IL-6, in pancreatic acinar cells. Reactive Oxygen Species 110-133 Janus kinase 1 Homo sapiens 176-180 22281165-2 2012 INCB018424, a small molecule inhibitor of JAK1 and JAK2, inhibits cytokine-induced JAK/signal transducers and activators of transcription signaling and the resultant production of inflammatory proteins (eg, IL-17). ruxolitinib 0-10 Janus kinase 1 Homo sapiens 42-46 22891040-4 2012 Afatinib activated interleukin-6 receptor (IL-6R)/JAK1/STAT3 signaling via autocrine IL-6 secretion in both cells. Afatinib 0-8 Janus kinase 1 Homo sapiens 50-54 22891040-5 2012 Inhibition of IL-6R/JAK1/STAT3 signaling pathway increased the sensitivity to afatinib. Afatinib 78-86 Janus kinase 1 Homo sapiens 20-24 22891040-7 2012 Blockade of IL-6R/JAK1 significantly increased the sensitivity to afatinib through inhibition of afatinib-induced STAT3 activation augmented by the interaction with fibroblasts, suggesting a critical role of paracrine IL-6R/JAK1/STAT3 loop between fibroblasts and cancer cells in the development of drug resistance. Afatinib 66-74 Janus kinase 1 Homo sapiens 18-22 22891040-7 2012 Blockade of IL-6R/JAK1 significantly increased the sensitivity to afatinib through inhibition of afatinib-induced STAT3 activation augmented by the interaction with fibroblasts, suggesting a critical role of paracrine IL-6R/JAK1/STAT3 loop between fibroblasts and cancer cells in the development of drug resistance. Afatinib 66-74 Janus kinase 1 Homo sapiens 224-228 22891040-7 2012 Blockade of IL-6R/JAK1 significantly increased the sensitivity to afatinib through inhibition of afatinib-induced STAT3 activation augmented by the interaction with fibroblasts, suggesting a critical role of paracrine IL-6R/JAK1/STAT3 loop between fibroblasts and cancer cells in the development of drug resistance. Afatinib 97-105 Janus kinase 1 Homo sapiens 18-22 22891040-7 2012 Blockade of IL-6R/JAK1 significantly increased the sensitivity to afatinib through inhibition of afatinib-induced STAT3 activation augmented by the interaction with fibroblasts, suggesting a critical role of paracrine IL-6R/JAK1/STAT3 loop between fibroblasts and cancer cells in the development of drug resistance. Afatinib 97-105 Janus kinase 1 Homo sapiens 224-228 22891040-8 2012 The enhancement of afatinib sensitivity by inhibition of IL-6R/JAK1/STAT3 signaling was confirmed in in vivo PC9-GR xenograft model. Afatinib 19-27 Janus kinase 1 Homo sapiens 63-67 22891040-9 2012 Similar to afatinib, de novo resistance to dacomitinib in H1975 and PC9-GR cells was also mediated by dacomitinib-induced JAK1/STAT3 activation. dacomitinib 43-54 Janus kinase 1 Homo sapiens 122-126 22891040-9 2012 Similar to afatinib, de novo resistance to dacomitinib in H1975 and PC9-GR cells was also mediated by dacomitinib-induced JAK1/STAT3 activation. dacomitinib 102-113 Janus kinase 1 Homo sapiens 122-126 22261016-3 2012 The new small drug molecule and JAK1/3 inhibitor, tofacitinib, is currently being tested in phase II and III clinical trials for rheumatoid arthritis, psoriasis and in organ transplantation. tofacitinib 50-61 Janus kinase 1 Homo sapiens 32-38 22763125-6 2012 We also found that PTP-MEG2 DA mutant preferentially associated with Janus kinase 1 (JAK1) but not with other JAK kinases (Tyk2 and JAK2) present in ECs and regulated JAK1 tyrosine phosphorylation. Tyrosine 172-180 Janus kinase 1 Homo sapiens 85-89 22698084-1 2012 Herein we report the discovery of the C-2 methyl substituted imidazopyrrolopyridine series and its optimization to provide potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. imidazopyrrolopyridine 61-83 Janus kinase 1 Homo sapiens 154-158 22812580-0 2012 Evaluation of WO2012037132 - a novel scaffold for selective JAK1 inhibition. wo2012037132 14-26 Janus kinase 1 Homo sapiens 60-64 22812580-1 2012 Novel 1-anilino-4-phenylphthalazine derivatives, compositions containing them, and their use as JAK1 inhibitors and for the treatment of cancer, inflammatory and autoimmune diseases are claimed. 1-anilino-4-phenylphthalazine 6-35 Janus kinase 1 Homo sapiens 96-100 22718840-0 2012 Long-term outcomes of 107 patients with myelofibrosis receiving JAK1/JAK2 inhibitor ruxolitinib: survival advantage in comparison to matched historical controls. ruxolitinib 84-95 Janus kinase 1 Homo sapiens 64-68 22718840-1 2012 Ruxolitinib is JAK1/JAK2 inhibitor with established clinical benefit in myelofibrosis (MF). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-19 22852872-6 2012 In November 2011, the US Food and Drug Administration approved the use of the JAK1- and JAK2-selective inhibitor ruxolitinib for the treatment of patients with intermediate or high-risk myelofibrosis, including PMF, post-PV MF, and post-ET MF. ruxolitinib 113-124 Janus kinase 1 Homo sapiens 78-82 22700718-1 2012 The discovery of JAK2617F mutation paved the way for the development of small molecule inhibitors of JAK1/2 resulting in first approved JAK1/2 inhibitor, ruxolitinib, for the treatment of patients with myelofibrosis (MF). ruxolitinib 154-165 Janus kinase 1 Homo sapiens 101-107 22700718-1 2012 The discovery of JAK2617F mutation paved the way for the development of small molecule inhibitors of JAK1/2 resulting in first approved JAK1/2 inhibitor, ruxolitinib, for the treatment of patients with myelofibrosis (MF). ruxolitinib 154-165 Janus kinase 1 Homo sapiens 136-142 22894574-2 2012 One additional treatment may be tofacitinib (CP-690,550), an oral inhibitor of Janus kinases 1, 2, and 3 with in vitro functional specificity for kinases 1 and 3 over kinase 2, which is expected to block signaling involving gamma chain-containing cytokines including interleukins 2, 4, 7, 9, 15, and 21. tofacitinib 32-43 Janus kinase 1 Homo sapiens 79-104 22894574-2 2012 One additional treatment may be tofacitinib (CP-690,550), an oral inhibitor of Janus kinases 1, 2, and 3 with in vitro functional specificity for kinases 1 and 3 over kinase 2, which is expected to block signaling involving gamma chain-containing cytokines including interleukins 2, 4, 7, 9, 15, and 21. tofacitinib 45-51 Janus kinase 1 Homo sapiens 79-104 23238141-2 2012 Ruxolitinib (INCB018424, Jakafi) is a potent dual JAK1 and JAK2 inhibitor. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 50-54 23238141-2 2012 Ruxolitinib (INCB018424, Jakafi) is a potent dual JAK1 and JAK2 inhibitor. ruxolitinib 13-23 Janus kinase 1 Homo sapiens 50-54 22555804-4 2012 Inhibitor 2 (E)-2-cyano-N-[(S)-1-phenylethyl]-3-(pyridin-2-yl)acrylamide was the most effective in inhibition of JAK/STAT3 signaling and at doses >= 25 muM significantly reduced the level of phosphorylated JAK1, JAK2 and STAT3 (at Tyr705) and downregulated the expression of known STAT3 targets. (e)-2-cyano-n-[(s)-1-phenylethyl]-3-(pyridin-2-yl)acrylamide 12-72 Janus kinase 1 Homo sapiens 209-213 22544377-1 2012 On November 16, 2011, the U.S. Food and Drug Administration (FDA) granted full approval to ruxolitinib, (Jakafi; Incyte Corp.), an inhibitor of the Janus kinases 1 and 2, for the treatment of patients with intermediate- or high-risk myelofibrosis, including primary myelofibrosis, postpolycythemia vera myelofibrosis, and postessential thrombocythemia myelofibrosis. ruxolitinib 91-102 Janus kinase 1 Homo sapiens 148-169 22474318-6 2012 Ruxolitinib (Jakafi; Incyte) is a small-molecule inhibitor of JAK1/2 that has proved to be effective at reducing splenomegaly and ameliorating symptoms in myeloproliferative neoplasms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 62-68 22402124-5 2012 IL-2 challenge enhanced tyrosine phosphorylation of Janus-activated kinase (JAK)1-3 and STAT5, and induced JAK1 and JAK2 to associate with STAT5 in IL-2-dependent ATL cells. Tyrosine 24-32 Janus kinase 1 Homo sapiens 76-83 22528658-3 2012 IL-5 binding to IL-5R on target cells induces rapid tyrosine phosphorylation and activation of various cellular proteins, including JAK1/JAK2 and STAT1/STAT5. Tyrosine 52-60 Janus kinase 1 Homo sapiens 132-136 22394507-6 2012 Exposure to quercetin resulted in the reduction of GP130, JAK1 and STAT3 activation by IL-6, as well as a marked decrease of the proliferative and migratory properties of glioblastoma cells induced by IL-6. Quercetin 12-21 Janus kinase 1 Homo sapiens 58-62 22406175-0 2012 STAT6 and JAK1 are essential for IL-4-mediated suppression of prostaglandin production in human follicular dendritic cells: opposing roles of phosphorylated and unphosphorylated STAT6. Prostaglandins 62-75 Janus kinase 1 Homo sapiens 10-14 22406175-7 2012 IL-4 induced tyrosine phosphorylation of STAT1, 3, and 6, but only JAK1-STAT6 pathway was responsible for the prevention of COX-2 augmentation and PG production. Prostaglandins 147-149 Janus kinase 1 Homo sapiens 67-71 22279053-1 2012 On November 16, 2011, the Food and Drug Administration approved ruxolitinib (a JAK1 and JAK2 inhibitor) for use in the treatment of high and intermediate risk myelofibrosis. ruxolitinib 64-75 Janus kinase 1 Homo sapiens 79-83 22375970-2 2012 We evaluated the efficacy and safety of ruxolitinib, a potent and selective Janus kinase (JAK) 1 and 2 inhibitor, as compared with the best available therapy, in patients with myelofibrosis. ruxolitinib 40-51 Janus kinase 1 Homo sapiens 76-102 22375971-1 2012 BACKGROUND: Ruxolitinib, a selective inhibitor of Janus kinase (JAK) 1 and 2, has clinically significant activity in myelofibrosis. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 50-76 22038826-6 2012 Acutely, curcumin inhibited Stat1 binding to the GAS cis-element, prevented Stat1 nuclear translocation, and reduced Jak1 phosphorylation and phosphorylation of Stat1 at Tyr(701). Curcumin 9-17 Janus kinase 1 Homo sapiens 117-121 22252297-9 2012 In HEK293T cells, CP-690,550 less effectively suppressed JAK1-mediated STAT3 phosphorylation compared with JAK3. tofacitinib 18-24 Janus kinase 1 Homo sapiens 57-61 22252297-10 2012 These results suggest that CP-690,550 has a different effects among JAKs and STATs, thereby affecting helper T cell differentiation, and murine autoimmune disease models. tofacitinib 27-33 Janus kinase 1 Homo sapiens 68-72 22333600-9 2012 Furthermore, lentiviral-mediated JAK1-overexpressing cells were more sensitive to enzastaurin than control cells. enzastaurin 82-93 Janus kinase 1 Homo sapiens 33-37 22333600-10 2012 CONCLUSION: Our results suggested that the JAK1 pathway may be used as a single predictive biomarker for enzastaurin treatment. enzastaurin 105-116 Janus kinase 1 Homo sapiens 43-47 23119228-7 2012 Discovery of the JAK2V617F mutation paved the way for drug discovery in MF, and the first JAK1/2 inhibitor, ruxolitinib, has been approved by FDA and Health Canada. ruxolitinib 108-119 Janus kinase 1 Homo sapiens 90-96 23055694-7 2012 Tofacitinib, a JAK1/3 inhibitor, was shown to be efficacious in two Phase III trials, while VX-509, a JAK3 inhibitor, showed promising results in a Phase II trial. tofacitinib 0-11 Janus kinase 1 Homo sapiens 15-21 22830345-4 2012 Ruxolitinib (previously known as INCB018424; Incyte Corporation, Wilmington, Delaware, USA) is a rationally designed potent oral JAK1 and JAK2 inhibitor that has undergone clinical trials in patients with PV, ET, and PMF. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 129-133 22905257-1 2012 We previously showed that oxidative stress inhibits leukemia inhibitory factor (LIF) signaling by targeting JAK1, and the catalytic domains of JAK 1 and 2 have a cysteine-based redox switch. Cysteine 162-170 Janus kinase 1 Homo sapiens 143-154 22661199-4 2012 CONCLUSION: These findings indicate that the STAT6 phosphorylation/activation induced by IL-13 is mediated by an activation of JAK1 in cultured hBSMCs. hbsmcs 144-150 Janus kinase 1 Homo sapiens 127-131 22108298-8 2012 Piceatannol also inhibits JAK-1, which is a key member of the STAT pathway that is crucial in controlling cellular activities in response to extracellular cytokines and is a COX-2-inducible enzyme involved in inflammation and carcinogenesis. 3,3',4,5'-tetrahydroxystilbene 0-11 Janus kinase 1 Homo sapiens 26-31 22149883-9 2012 Among the H-iridoids tested, H-geniposide inhibited constitutive STAT3 activation through inhibiting upstream JAK1 and c-Src. h-geniposide 29-41 Janus kinase 1 Homo sapiens 110-114 23056499-3 2012 Here, we tested the efficacy of a JAK1/2- inhibitor, AZD1480, in the in vitro and in vivo growth of thyroid cancer cell lines expressing oncogenic RET. AZD 1480 53-60 Janus kinase 1 Homo sapiens 34-38 21257798-1 2011 INCB018424 phosphate, a potent inhibitor of JAK enzymes with selectivity for JAK1&2, is in development for the treatment of myelofibrosis (MF). Ruxolitinib phosphate 0-20 Janus kinase 1 Homo sapiens 77-87 22319590-7 2012 Interestingly, treatment of NSCLC cells with the JAK1/2 inhibitor ruxolitinib has no effect on cell proliferation and viability in two-dimensional culture, but inhibits growth in soft agar and xenograft assays. ruxolitinib 66-77 Janus kinase 1 Homo sapiens 49-55 22399854-1 2012 Ruxolitinib is an orally bioavailable, selective Janus kinase (JAK) 1 and 2 inhibitor approved for the treatment of myelofibrosis (MF), a bone marrow disease in which the JAK pathway is dysregulated, leading to impaired hematopoiesis and immune function. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 49-75 22399854-2 2012 By inhibiting JAK1 and JAK2, ruxolitinib modulates cytokine-stimulated intracellular signaling. ruxolitinib 29-40 Janus kinase 1 Homo sapiens 14-18 21880948-5 2011 The kinase JAK1 is enriched in membrane fractions and is activated during human sperm capacitation as suggested by its increase in phosphotyrosine content. Phosphotyrosine 131-146 Janus kinase 1 Homo sapiens 11-15 21325634-7 2011 Second, curcumin suppressed activation of signal transducer and activator of transcription-3 as indicated by decreased phosphorylation at both tyrosine(705) and serine(727) and inhibition of janus kinase-1 phosphorylation. Curcumin 8-16 Janus kinase 1 Homo sapiens 191-205 21788946-4 2011 CYT387 is a novel, orally bioavailable JAK1/2 inhibitor, which has recently been described. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-6 Janus kinase 1 Homo sapiens 39-45 22027691-4 2011 AZD1480 treatment effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. AZD 1480 0-7 Janus kinase 1 Homo sapiens 71-75 21965659-7 2011 Importantly, we identified a cluster of three membrane-proximal betac lysine residues (Lys(457), Lys(461), and Lys(467)) whose presence was required for both JAK1/2 binding to betac and receptor ubiquitination. Lysine 70-76 Janus kinase 1 Homo sapiens 158-162 21965659-7 2011 Importantly, we identified a cluster of three membrane-proximal betac lysine residues (Lys(457), Lys(461), and Lys(467)) whose presence was required for both JAK1/2 binding to betac and receptor ubiquitination. Lysine 87-90 Janus kinase 1 Homo sapiens 158-162 21965659-7 2011 Importantly, we identified a cluster of three membrane-proximal betac lysine residues (Lys(457), Lys(461), and Lys(467)) whose presence was required for both JAK1/2 binding to betac and receptor ubiquitination. Lysine 97-100 Janus kinase 1 Homo sapiens 158-162 21965659-7 2011 Importantly, we identified a cluster of three membrane-proximal betac lysine residues (Lys(457), Lys(461), and Lys(467)) whose presence was required for both JAK1/2 binding to betac and receptor ubiquitination. Lysine 97-100 Janus kinase 1 Homo sapiens 158-162 21691275-1 2011 SB1518 is an innovative pyrimidine-based macrocycle that shows a unique kinase profile with selective inhibition of Janus Kinase-2 (JAK2; IC50=23 and 19 nM for JAK2(WT) and JAK2(V617F), respectively) within the JAK family (IC50=1280, 520 and 50 nM for JAK1, JK3 and TYK2, respectively) and fms-like tyrosine kinase-3 (FLT3; IC50=22 nM). 11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,26-triazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene 0-6 Janus kinase 1 Homo sapiens 252-256 22034658-1 2011 Ruxolitinib (INCB018424) is a JAK1 and JAK2 inhibitor recently evaluated for the treatment of myelofibrosis (MF) in early- and advanced-phase clinical trials. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 30-34 22034658-1 2011 Ruxolitinib (INCB018424) is a JAK1 and JAK2 inhibitor recently evaluated for the treatment of myelofibrosis (MF) in early- and advanced-phase clinical trials. ruxolitinib 13-23 Janus kinase 1 Homo sapiens 30-34 22146225-1 2011 Ruxolitinib is an orally available, ATP-competitive inhibitor, selective for tyrosine-protein kinases JAK1 and JAK2 and is the most advanced JAK1/JAK2 inhibitor in development for the treatment of myeloproliferative neoplasms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 102-106 22146225-1 2011 Ruxolitinib is an orally available, ATP-competitive inhibitor, selective for tyrosine-protein kinases JAK1 and JAK2 and is the most advanced JAK1/JAK2 inhibitor in development for the treatment of myeloproliferative neoplasms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 141-145 22146225-1 2011 Ruxolitinib is an orally available, ATP-competitive inhibitor, selective for tyrosine-protein kinases JAK1 and JAK2 and is the most advanced JAK1/JAK2 inhibitor in development for the treatment of myeloproliferative neoplasms. Adenosine Triphosphate 36-39 Janus kinase 1 Homo sapiens 102-106 22146225-2 2011 The suggested mechanism of action of ruxolitinib is attenuation of cytokine signaling via the inhibition of JAK1 and JAK2 (wild-type or mutated forms), resulting in antiproliferative and proapoptotic effects. ruxolitinib 37-48 Janus kinase 1 Homo sapiens 108-112 21635221-2 2011 In a recently completed Phase I?II study, ruxolitinib, a selective orally available JAK1 and JAK2 inhibitor, has shown efficacy in patients with advanced myelofibrosis. ruxolitinib 42-53 Janus kinase 1 Homo sapiens 84-88 22362131-11 2011 Recently, the positive results of the first in class of the JAK1/JAK2 inhibitors, ruxolitinib (formerly INCB18242), from 2 large phase III studies were presented and are discussed herein. ruxolitinib 82-93 Janus kinase 1 Homo sapiens 60-64 21919691-0 2011 Ruxolitinib: a new JAK1/2 inhibitor that offers promising options for treatment of myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 19-25 21919691-1 2011 Ruxolitinib (INCB018424) is the first potent, selective, oral inhibitor of JAK1 and 2 being developed for clinical use. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 75-85 21919691-1 2011 Ruxolitinib (INCB018424) is the first potent, selective, oral inhibitor of JAK1 and 2 being developed for clinical use. ruxolitinib 13-23 Janus kinase 1 Homo sapiens 75-85 21677670-3 2011 We hypothesized that local inhibition of cytokine signaling using topical administration of INCB018424, a small molecule inhibitor of JAK1 and JAK2, would provide benefit similar to systemic cytokine neutralization. ruxolitinib 92-102 Janus kinase 1 Homo sapiens 134-138 21635221-8 2011 Ruxolitinib, a potent JAK1 and JAK2 inhibitor, known to decrease spleen size and alleviate constitutional symptoms in myelofibrosis, represents a potentially promising agent for the treatment of leukemias by inhibiting the JAK?STAT signaling. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-26 21289371-0 2011 Oral administration of penta-O-galloyl-beta-D-glucose suppresses triple-negative breast cancer xenograft growth and metastasis in strong association with JAK1-STAT3 inhibition. penta-o-galloyl-beta-d-glucose 23-53 Janus kinase 1 Homo sapiens 154-158 21679692-6 2011 Adenovirus-based expression of Jak1 inactive mutant demonstrated that Jak1 mediates ZO-2 tyrosine phosphorylation. Tyrosine 89-97 Janus kinase 1 Homo sapiens 31-35 21679692-6 2011 Adenovirus-based expression of Jak1 inactive mutant demonstrated that Jak1 mediates ZO-2 tyrosine phosphorylation. Tyrosine 89-97 Janus kinase 1 Homo sapiens 70-74 21289371-2 2011 Extending on our recent work, we hypothesize that the herbal compound 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) can inhibit the growth and metastasis of TNBCa xenograft and target Janus-activated kinase (JAK)-signal transducer and activator of transcription (STAT) 3-signaling axis. beta-penta-O-galloyl-glucose 70-110 Janus kinase 1 Homo sapiens 209-212 21289371-2 2011 Extending on our recent work, we hypothesize that the herbal compound 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) can inhibit the growth and metastasis of TNBCa xenograft and target Janus-activated kinase (JAK)-signal transducer and activator of transcription (STAT) 3-signaling axis. beta-penta-O-galloyl-glucose 112-115 Janus kinase 1 Homo sapiens 209-212 21289371-7 2011 In cell culture of MDA-MB-231 cells, PGG decreased pSTAT3 and its downstream target proteins, decreased its upstream kinase pJAK1 and induced the expression of SHP1, a JAK1 upstream tyrosine phosphatase, within as early as 1 h of exposure. beta-penta-O-galloyl-glucose 37-40 Janus kinase 1 Homo sapiens 125-129 21289371-10 2011 Mechanistically, PGG-induced inhibition of JAK1-STAT3 axis may contribute to the observed in vivo efficacy and the effects on the cellular processes. beta-penta-O-galloyl-glucose 17-20 Janus kinase 1 Homo sapiens 43-47 21393331-0 2011 Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors. Adenosine Triphosphate 58-61 Janus kinase 1 Homo sapiens 10-14 21420464-4 2011 Interestingly, CK inhibited phosphorylation of STAT3 and its upstream activators, the Janus activated kinase 1 (JAK1), but not JAK2. ginsenoside M1 15-17 Janus kinase 1 Homo sapiens 86-110 21420464-4 2011 Interestingly, CK inhibited phosphorylation of STAT3 and its upstream activators, the Janus activated kinase 1 (JAK1), but not JAK2. ginsenoside M1 15-17 Janus kinase 1 Homo sapiens 112-116 21420464-8 2011 Overall, our findings demonstrate that JAK1/STAT3 signaling mediates CK-induced apoptosis in U266 cells and also suggest the chemopreventive potential of CK for treatment of multiple myeloma. ginsenoside M1 69-71 Janus kinase 1 Homo sapiens 39-43 21393331-4 2011 We further used this library of JAK1 mutation-positive cell lines to assess their sensitivity to ATP-competitive inhibitors. Adenosine Triphosphate 97-100 Janus kinase 1 Homo sapiens 32-36 21393331-5 2011 RESULTS: While most JAK1 mutants were sensitive to ATP-competitive JAK inhibitors, mutations targeting Phe958 and Pro960 in the hinge region of the kinase domain rendered JAK1 constitutively active but also resistant to all tested JAK inhibitors. Adenosine Triphosphate 51-54 Janus kinase 1 Homo sapiens 20-24 20478313-2 2010 Although the crystal structures of active JAK1 and JAK2 kinase domains have been reported recently with the clinical compound CP-690550, the structures of both TYK2 and JAK3 with CP-690550 have remained outstanding. tofacitinib 126-135 Janus kinase 1 Homo sapiens 42-46 21439476-6 2011 Specific inhibition of the "analog-sensitive" mutant AS-Jak1 but not AS-Jak3 by the ATP-competitive analog 1NM-PP1 abrogated IL-2 signaling, corroborating the data with the selective Jak3 inhibitor. Adenosine Triphosphate 84-87 Janus kinase 1 Homo sapiens 56-60 21439476-6 2011 Specific inhibition of the "analog-sensitive" mutant AS-Jak1 but not AS-Jak3 by the ATP-competitive analog 1NM-PP1 abrogated IL-2 signaling, corroborating the data with the selective Jak3 inhibitor. 1-tert-butyl-3-naphthalen-1-ylmethyl-1H-pyrazolo(3,4-d)pyrimidin-4-ylemine 107-114 Janus kinase 1 Homo sapiens 56-60 21439476-7 2011 Jak1 thus plays a dominant role over Jak3 and these data challenge the notion that selective ATP-competitive Jak3 kinase inhibitors will be effective. Adenosine Triphosphate 93-96 Janus kinase 1 Homo sapiens 0-4 21216930-5 2011 Inhibition of JAK1 with small molecules or RNA interference resulted in loss of STAT3 tyrosine phosphorylation and inhibition of cell growth. Tyrosine 86-94 Janus kinase 1 Homo sapiens 14-18 20878062-11 2010 RNA transcript analyses showed decreased EGF-R and KRas expression in vivo, following indomethacin treatment, which also included KRas, PI3K, JAK1, STAT3 and c-jun, mRNAs in cultured tumor cells. Indomethacin 86-98 Janus kinase 1 Homo sapiens 142-146 20570727-4 2010 IL-13 stimulates intracellular ROS synthesis within 5min via IL-13Ralpha1-JAK1-STAT6- and IL-13Ralpha2-MEK1/2-ERK1/2-dependent activation of nicotinamide adenine dinucleotide phosphate (NADPH) oxidase-1 (NOX-1). Reactive Oxygen Species 31-34 Janus kinase 1 Homo sapiens 74-78 20843246-3 2010 INCB018424 is a potent and selective Janus kinase 1 (JAK1) and JAK2 inhibitor. ruxolitinib 0-10 Janus kinase 1 Homo sapiens 37-51 20843246-3 2010 INCB018424 is a potent and selective Janus kinase 1 (JAK1) and JAK2 inhibitor. ruxolitinib 0-10 Janus kinase 1 Homo sapiens 53-57 21198544-6 2011 gamma-Tocotrienol also inhibited the activation of Src, JAK1 and JAK2 implicated in STAT3 activation. plastochromanol 8 0-17 Janus kinase 1 Homo sapiens 56-60 21277633-0 2011 IL-4 and IL-13 suppress prostaglandins production in human follicular dendritic cells by repressing COX-2 and mPGES-1 expression through JAK1 and STAT6. Prostaglandins 24-38 Janus kinase 1 Homo sapiens 137-141 21277633-8 2011 Although IL-4 induced tyrosine phosphorylation of JAK1 and TYK2, RNA interference experiments revealed that only JAK1 was responsible for the IL-4-stimulated STAT6 phosphorylation. Tyrosine 22-30 Janus kinase 1 Homo sapiens 50-54 21277633-9 2011 Knocking down JAK1 and STAT6 ablated the inhibitory effect of IL-4 on COX-2 expression and significantly reduced production of PGE(2) and prostacyclin. Dinoprostone 127-133 Janus kinase 1 Homo sapiens 14-18 21277633-9 2011 Knocking down JAK1 and STAT6 ablated the inhibitory effect of IL-4 on COX-2 expression and significantly reduced production of PGE(2) and prostacyclin. Epoprostenol 138-150 Janus kinase 1 Homo sapiens 14-18 21277633-13 2011 These results stress the essential roles of JAK1 and STAT6 in the early signaling pathway of IL-4 and IL-13 leading to suppression of COX-2 expression and repression of PG production by HK cells. Prostaglandins 169-171 Janus kinase 1 Homo sapiens 44-48 21079613-4 2011 However, most patients treated with a JAK2 (TG101348) or JAK1/2 (INCB018424) inhibitor experienced substantial improvement in constitutional symptoms and reduction in spleen size; the mechanism of action for INCB018424 includes anti-JAK1-mediated downregulation of proinflammatory cytokines. ruxolitinib 65-75 Janus kinase 1 Homo sapiens 57-63 21079613-4 2011 However, most patients treated with a JAK2 (TG101348) or JAK1/2 (INCB018424) inhibitor experienced substantial improvement in constitutional symptoms and reduction in spleen size; the mechanism of action for INCB018424 includes anti-JAK1-mediated downregulation of proinflammatory cytokines. ruxolitinib 65-75 Janus kinase 1 Homo sapiens 57-61 21079613-4 2011 However, most patients treated with a JAK2 (TG101348) or JAK1/2 (INCB018424) inhibitor experienced substantial improvement in constitutional symptoms and reduction in spleen size; the mechanism of action for INCB018424 includes anti-JAK1-mediated downregulation of proinflammatory cytokines. ruxolitinib 208-218 Janus kinase 1 Homo sapiens 57-63 21079613-4 2011 However, most patients treated with a JAK2 (TG101348) or JAK1/2 (INCB018424) inhibitor experienced substantial improvement in constitutional symptoms and reduction in spleen size; the mechanism of action for INCB018424 includes anti-JAK1-mediated downregulation of proinflammatory cytokines. ruxolitinib 208-218 Janus kinase 1 Homo sapiens 57-61 21625597-2 2011 We report that, in human THP-1 cell line, they inhibit IL-6-elicited tyrosine phosphorylation of STAT3 and its DNA binding activity with EC(50) of 10 microM with concomitant down-regulation of the phosphorylation of the tyrosine Janus kinases JAK1, JAK2 and Tyk2. Tyrosine 69-77 Janus kinase 1 Homo sapiens 243-247 21106455-0 2010 Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. diamino-1,2,4-triazole 0-22 Janus kinase 1 Homo sapiens 72-76 21106455-2 2010 Presented is the design and synthesis of 1,2,4-triazoles, and the evaluation of their inhibitory activity against the Janus associated kinases TYK2 and JAKs 1-3. 1,2,4-triazole 41-56 Janus kinase 1 Homo sapiens 152-156 19937797-3 2010 We found that betulinic acid inhibited constitutive activation of STAT3, Src kinase, JAK1 and JAK2. betulinic acid 14-28 Janus kinase 1 Homo sapiens 85-89 20053498-4 2010 The activation of c-Src, JAK1 and JAK2 implicated in STAT3 activation, were also suppressed by this saponin. Saponins 100-107 Janus kinase 1 Homo sapiens 25-29 20167604-3 2010 Upon IL-7 binding, both chains are driven in cholesterol- and sphingomyelin-rich rafts where associated signaling proteins Jak1, Jak3, STAT1, -3, and -5 are found to be phosphorylated. Cholesterol 58-69 Janus kinase 1 Homo sapiens 136-140 20506062-0 2010 Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 25-29 20506062-1 2010 Ruxolitinib (INCB-018424) is a potent, orally available, selective inhibitor of both JAK1 and JAK2 of the JAK-STAT signaling pathway, being developed by Incyte Corp and Novartis AG. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 85-89 20506062-1 2010 Ruxolitinib (INCB-018424) is a potent, orally available, selective inhibitor of both JAK1 and JAK2 of the JAK-STAT signaling pathway, being developed by Incyte Corp and Novartis AG. ruxolitinib 13-24 Janus kinase 1 Homo sapiens 85-89 20167604-3 2010 Upon IL-7 binding, both chains are driven in cholesterol- and sphingomyelin-rich rafts where associated signaling proteins Jak1, Jak3, STAT1, -3, and -5 are found to be phosphorylated. Sphingomyelins 75-88 Janus kinase 1 Homo sapiens 136-140 20371721-7 2010 These data indicate that the inhibition of STAT3 activity by sorafenib involves both the inhibition of upstream kinases (JAK1 and JAK2) of STAT3 and increased phosphatase activity. Sorafenib 61-70 Janus kinase 1 Homo sapiens 121-125 20442315-9 2010 Western blot analysis of the xenograft tumor tissues showed that HO-3867 inhibited pSTAT3 (Tyr705 and Ser727) and JAK1 and increased apoptotic markers cleaved caspase-3 and poly ADP ribose polymerase. Holmium 65-67 Janus kinase 1 Homo sapiens 114-118 20130243-0 2010 Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. ruxolitinib 63-73 Janus kinase 1 Homo sapiens 46-52 20672017-6 2010 From this screen, we have identified novel signaling molecules, such as JAK1, STAT1, cortactin (CTTN), FER, p130Cas (BCAR1), SRC and FYN as tyrosine phosphorylated in human MM cell lines. Tyrosine 140-148 Janus kinase 1 Homo sapiens 72-76 19710367-4 2009 We provide evidence that AD412 inhibited the JAK1/3-dependent phosphorylations of Akt, STAT5a/b, and ERK1/2 in IL-2-stimulated CTL-L2 cells. 3-(1-(4-chlorobenzyl)indol-3-yl)-N-(pyridin-4-yl)propanamide 25-30 Janus kinase 1 Homo sapiens 45-49 19945455-3 2010 Stimulation of WISH cells with the cyclic peptide showed tyrosine phosphorylation of Jak1 and Tyk2 kinases, tyrosine and serine phosphorylation of STAT1 and STAT3 transcription factors and activation of p38 MAPK pathway, although phosphorylation levels or kinetics were in some conditions different to those obtained under IFN-alpha2b stimulus. Tyrosine 57-65 Janus kinase 1 Homo sapiens 85-89 20072651-0 2010 INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support. INCB 16562 0-9 Janus kinase 1 Homo sapiens 13-19 20072651-2 2010 INCB16562 was developed as a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. INCB 16562 0-9 Janus kinase 1 Homo sapiens 99-103 20072651-9 2010 Taken together, these data suggest that INCB16562 is a potent JAK1/2 inhibitor and that mitigation of JAK/STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. INCB 16562 40-49 Janus kinase 1 Homo sapiens 62-68 20072651-9 2010 Taken together, these data suggest that INCB16562 is a potent JAK1/2 inhibitor and that mitigation of JAK/STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. INCB 16562 40-49 Janus kinase 1 Homo sapiens 62-66 19887489-9 2009 CONCLUSIONS: These data showed that administration of the dual JAK1/2 inhibitor INCB16562 reduces malignant cell burden, normalizes spleen size and architecture, suppresses inflammatory cytokines, improves weight gain, and extends survival in a rodent model of JAK2V617F-driven hematologic malignancy. INCB 16562 80-89 Janus kinase 1 Homo sapiens 63-69 19928918-10 2010 Moreover, phosphorylation of PKC-delta, JAK-1, and JAK-2, which are the upstream event for the activation of STAT1, are also inhibited by EGCG in IFN-gamma-stimulated human oral cancer cells. epigallocatechin gallate 138-142 Janus kinase 1 Homo sapiens 40-45 20006573-7 2010 Concomitantly, TNFalpha induced phosphorylation of STAT1 at Tyr-701 by JAK1 facilitates its nuclear translocation and activation of CD40 through p300 recruitment and core Histone-3 acetylation. Tyrosine 60-63 Janus kinase 1 Homo sapiens 71-75 19706767-6 2009 Addition of DTT or glutathione prevents the JAK cross-linking and blocks the inhibitory effects of HJB on IL-6-induced STAT3 activation, suggesting that HJB may react with cystein residues of JAKs to form covalent bonds that inactivate JAKs. Dithiothreitol 12-15 Janus kinase 1 Homo sapiens 192-196 19762238-0 2009 Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). phenylaminopyrimidines 0-22 Janus kinase 1 Homo sapiens 55-59 19762238-1 2009 A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). phenylaminopyrimidines 12-34 Janus kinase 1 Homo sapiens 87-91 19762238-2 2009 Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 73-79 Janus kinase 1 Homo sapiens 58-62 19762238-2 2009 Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 81-159 Janus kinase 1 Homo sapiens 58-62 19706767-6 2009 Addition of DTT or glutathione prevents the JAK cross-linking and blocks the inhibitory effects of HJB on IL-6-induced STAT3 activation, suggesting that HJB may react with cystein residues of JAKs to form covalent bonds that inactivate JAKs. Glutathione 19-30 Janus kinase 1 Homo sapiens 192-196 19706767-6 2009 Addition of DTT or glutathione prevents the JAK cross-linking and blocks the inhibitory effects of HJB on IL-6-induced STAT3 activation, suggesting that HJB may react with cystein residues of JAKs to form covalent bonds that inactivate JAKs. Dithiothreitol 12-15 Janus kinase 1 Homo sapiens 236-240 19706767-6 2009 Addition of DTT or glutathione prevents the JAK cross-linking and blocks the inhibitory effects of HJB on IL-6-induced STAT3 activation, suggesting that HJB may react with cystein residues of JAKs to form covalent bonds that inactivate JAKs. Glutathione 19-30 Janus kinase 1 Homo sapiens 236-240 19295546-0 2009 CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-6 Janus kinase 1 Homo sapiens 20-24 19706767-6 2009 Addition of DTT or glutathione prevents the JAK cross-linking and blocks the inhibitory effects of HJB on IL-6-induced STAT3 activation, suggesting that HJB may react with cystein residues of JAKs to form covalent bonds that inactivate JAKs. Cysteine 172-179 Janus kinase 1 Homo sapiens 192-196 19295546-6 2009 Overall, our data indicate that the JAK1/JAK2 selective inhibitor CYT387 has potential for efficacious treatment of MPN harboring mutated JAK2 and MPL alleles. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 66-72 Janus kinase 1 Homo sapiens 36-40 19295546-2 2009 CYT387 is an ATP-competitive small molecule that potently inhibits JAK1/JAK2 kinases (IC(50)=11 and 18 nM, respectively), with significantly less activity against other kinases, including JAK3 (IC(50)=155 nM). N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-6 Janus kinase 1 Homo sapiens 67-71 19295546-2 2009 CYT387 is an ATP-competitive small molecule that potently inhibits JAK1/JAK2 kinases (IC(50)=11 and 18 nM, respectively), with significantly less activity against other kinases, including JAK3 (IC(50)=155 nM). Adenosine Triphosphate 13-16 Janus kinase 1 Homo sapiens 67-71 18664717-0 2008 Ceramide accelerates ultraviolet-induced MMP-1 expression through JAK1/STAT-1 pathway in cultured human dermal fibroblasts. Ceramides 0-8 Janus kinase 1 Homo sapiens 66-70 19951532-7 2009 The phosphorylation of JAK1 was enhanced after the NB4 cells treated with As2O3. Arsenic Trioxide 74-79 Janus kinase 1 Homo sapiens 23-27 19951532-9 2009 The effect of As2O3 inhibiting NB4 cells proliferation was weaker in the JAK1 siRNA transfected group. Arsenic Trioxide 14-19 Janus kinase 1 Homo sapiens 73-77 19951532-10 2009 The inhibiting rate of 4 micromol/L As2O3 on NB4 cells proliferation of JAK1 siRNA group was 49.12% being lower than that of the non-specific siRNA group (74.58%) and control group (72.33%). Arsenic Trioxide 36-41 Janus kinase 1 Homo sapiens 72-76 19951532-11 2009 After NB4 cells transfected with JAK1 plasmid, the JAK1 expression level in wild-type and mutant type plasmid groups were significantly higher than those in the empty plasmid group, moreover the effect of As2O3 inhibiting proliferation was stronger in wild-type plasmid group. Arsenic Trioxide 205-210 Janus kinase 1 Homo sapiens 33-37 19951532-11 2009 After NB4 cells transfected with JAK1 plasmid, the JAK1 expression level in wild-type and mutant type plasmid groups were significantly higher than those in the empty plasmid group, moreover the effect of As2O3 inhibiting proliferation was stronger in wild-type plasmid group. Arsenic Trioxide 205-210 Janus kinase 1 Homo sapiens 51-55 19951532-12 2009 The inhibiting rate of 4 micromol/L As2O3 on NB4 cells proliferation of wild-type plasmid group was 69.53% being higher than that of the mutant type JAK1 plasmid group (37.26%) and the empty plasmid group (39.61%). Arsenic Trioxide 36-41 Janus kinase 1 Homo sapiens 149-153 19951532-15 2009 Arsenic trioxide inhibits the proliferation of NB4 cells through activating the JAK1. Arsenic Trioxide 0-16 Janus kinase 1 Homo sapiens 80-84 19951532-16 2009 P21 is up-regulated after arsenic trioxide activated the JAK1 to inhibit the proliferation of NB4 cells. Arsenic Trioxide 26-42 Janus kinase 1 Homo sapiens 57-61 19139102-4 2009 Mutation of the FERM domain of JAK1, which is critical for cytokine receptor association, or of the single tyrosine of IL-9Ralpha involved in STAT recruitment abolished this activity, indicating that JAK1 mutants need to associate with a functional IL-9Ralpha to activate STAT factors. Tyrosine 107-115 Janus kinase 1 Homo sapiens 200-204 18995957-0 2009 Myricetin directly targets JAK1 to inhibit cell transformation. myricetin 0-9 Janus kinase 1 Homo sapiens 27-31 18995957-7 2009 Myricetin inhibited the phosphorylation of JAK1 and increased the autophosphorylation of EGF receptor (EGFR). myricetin 0-9 Janus kinase 1 Homo sapiens 43-47 18995957-9 2009 Affinity data further demonstrated that myricetin had a higher affinity for JAK1 than STAT3. myricetin 40-49 Janus kinase 1 Homo sapiens 76-80 19014879-9 2009 CONCLUSIONS: IFNalpha determines the binding of PEA3 to JAK1 and its tyrosine phosphorylation. Tyrosine 69-77 Janus kinase 1 Homo sapiens 56-60 19635391-4 2009 Exposure of BE(2)-C cells to the heavy metals CdCl(2) and HgCl(2) and to the mitochondrial complex I inhibitor rotenone inhibited interleukin-6, interferon-gamma and ciliary neurotrophic factor-mediated Jak/STAT signaling, reduced Jak1 and Jak2 auto-phosphorylation and induced Jak tyrosine nitration. Rotenone 111-119 Janus kinase 1 Homo sapiens 231-235 19385051-5 2009 EGF also induced the phosphorylation of EGFR, ERK, and STAT-3, and these effects were inhibited by the EGFR inhibitor, AG1478.To investigate the involvement of the STAT-3 pathway on EGF-induced MMP-9 expression, we pretreatedSKBR3 cells with JAK1, JAK2, and JAK3 inhibitors prior to EGF treatment. RTKI cpd 119-125 Janus kinase 1 Homo sapiens 242-246 19231233-6 2009 Expressions of proteins and mRNAs of cytokines were determined by ELISA and RT-PCR, respectively, activities of MAP kinases, PKC, JAK1/2, and STAT1 on tyrosine 701 and serine 727 by immunoblotting, the DNA-binding activity of the transcription factors by electrophoretic mobility shift assay. Tyrosine 151-159 Janus kinase 1 Homo sapiens 130-136 19231233-7 2009 IFNgamma-stimulated mast cells showed increase in expressions of proteins and mRNAs of inflammatory cytokines, phosphorylations of MAP kinases, PKCalpha and betaI, JAK1/2, and STAT1 on tyrosine 701 and serine 727. Tyrosine 185-193 Janus kinase 1 Homo sapiens 164-170 19361440-4 2009 Both inhibitors bound in a similar manner to JAK1, namely buried deep within a constricted ATP-binding site, thereby providing a basis for the potent inhibition of JAK1. Adenosine Triphosphate 91-94 Janus kinase 1 Homo sapiens 45-49 19361440-4 2009 Both inhibitors bound in a similar manner to JAK1, namely buried deep within a constricted ATP-binding site, thereby providing a basis for the potent inhibition of JAK1. Adenosine Triphosphate 91-94 Janus kinase 1 Homo sapiens 164-168 19361440-5 2009 As expected, the mode of inhibitor binding in JAK1 was very similar to that observed in JAK2, highlighting the challenges in developing JAK-specific inhibitors that target the ATP-binding site. Adenosine Triphosphate 176-179 Janus kinase 1 Homo sapiens 46-50 19361440-6 2009 Nevertheless, differences surrounding the JAK1 and JAK2 ATP-binding sites were apparent, thereby providing a platform for the rational design of JAK2- and JAK1-specific inhibitors. Adenosine Triphosphate 56-59 Janus kinase 1 Homo sapiens 155-159 18922133-2 2009 In addition to their role in phosphorylation of receptor tyrosine residues and downstream signalling substrates, JAKs have recently been implicated in controlling expression of cytokine receptors, predominantly by masking critical motifs involved in endocytosis and lysosomal targeting. Tyrosine 57-65 Janus kinase 1 Homo sapiens 113-117 18664717-7 2008 The activation of ceramide pathway by C(2)-ceramide enhanced phosphorylation of signal transducer and activators of transcription-1 (STAT-1), whereas ceramide-induced MMP-1 expression was potently prevented by piceatannol; Janus kinase (JAK1) inhibtor; and WHI-P131, a specific inhibitor of JAK3; but not by AG490, JAK 2 inhbitor, in human dermal fibroblasts. Ceramides 18-26 Janus kinase 1 Homo sapiens 237-241 18664717-8 2008 We also found that UV induced the phosphorylation of STAT-1, and UV-induced MMP-1 expression was significantly decreased by JAK1 inhibitor, piceatannol. 3,3',4,5'-tetrahydroxystilbene 140-151 Janus kinase 1 Homo sapiens 124-128 18664717-9 2008 Overall, we demonstrate that induction of intracellular ceramide by UV may activate MMP-1 gene expression via JAK1/STAT-1 pathway. Ceramides 56-64 Janus kinase 1 Homo sapiens 110-114 18596134-6 2008 Combined results from EMSA and western blot analysis revealed the inhibitory ability of 15d-PGJ(2), but not of synthetic PPARgamma ligands, on IFN-gamma-induced tyrosine phosphorylation of JAK1, JAK2, STAT1 and nuclear STAT1 translocation and DNA binding. 15d-pgj 88-95 Janus kinase 1 Homo sapiens 189-193 18596134-6 2008 Combined results from EMSA and western blot analysis revealed the inhibitory ability of 15d-PGJ(2), but not of synthetic PPARgamma ligands, on IFN-gamma-induced tyrosine phosphorylation of JAK1, JAK2, STAT1 and nuclear STAT1 translocation and DNA binding. Tyrosine 161-169 Janus kinase 1 Homo sapiens 189-193 18682290-6 2008 We also demonstrate, in Jak1, phosphorylation of Y(939), a corresponding tyrosine residue with Y(913), negatively regulated Jak1 signaling pathway. Tyrosine 73-81 Janus kinase 1 Homo sapiens 24-28 18682290-6 2008 We also demonstrate, in Jak1, phosphorylation of Y(939), a corresponding tyrosine residue with Y(913), negatively regulated Jak1 signaling pathway. Tyrosine 73-81 Janus kinase 1 Homo sapiens 124-128 18413761-0 2008 Triterpenoid CDDO-methyl ester inhibits the Janus-activated kinase-1 (JAK1)-->signal transducer and activator of transcription-3 (STAT3) pathway by direct inhibition of JAK1 and STAT3. triterpenoid TP-222 0-12 Janus kinase 1 Homo sapiens 70-74 18413761-3 2008 The present studies show that CDDO-Me blocks interleukin-6 (IL-6)-induced and constitutive activation of the Janus-activated kinase 1 (JAK1) in cells. bardoxolone methyl 30-37 Janus kinase 1 Homo sapiens 109-133 18413761-3 2008 The present studies show that CDDO-Me blocks interleukin-6 (IL-6)-induced and constitutive activation of the Janus-activated kinase 1 (JAK1) in cells. bardoxolone methyl 30-37 Janus kinase 1 Homo sapiens 135-139 18413761-4 2008 In support of a direct mechanism, CDDO-Me forms adducts with JAK1 at Cys(1077) in the kinase domain and inhibits JAK1 activity. bardoxolone methyl 34-41 Janus kinase 1 Homo sapiens 61-65 18413761-4 2008 In support of a direct mechanism, CDDO-Me forms adducts with JAK1 at Cys(1077) in the kinase domain and inhibits JAK1 activity. bardoxolone methyl 34-41 Janus kinase 1 Homo sapiens 113-117 18413761-4 2008 In support of a direct mechanism, CDDO-Me forms adducts with JAK1 at Cys(1077) in the kinase domain and inhibits JAK1 activity. Cysteine 69-72 Janus kinase 1 Homo sapiens 61-65 18413761-7 2008 These findings indicate that CDDO-Me inhibits activation of the JAK1-->STAT3 pathway by forming adducts with both JAK1 and STAT3. bardoxolone methyl 29-36 Janus kinase 1 Homo sapiens 64-68 18413761-7 2008 These findings indicate that CDDO-Me inhibits activation of the JAK1-->STAT3 pathway by forming adducts with both JAK1 and STAT3. bardoxolone methyl 29-36 Janus kinase 1 Homo sapiens 117-121 18381062-2 2008 Here, I showed that coumermycin-induced chemical heterodimerization of Jak1 and Jak3 but not homodimerization of Jak1 or Jak3 induces cell proliferation of an IL-2R-reconstituted cell line. coumermycin 20-31 Janus kinase 1 Homo sapiens 71-75 18346458-7 2008 Superimposition of the interface residues suggested that substitution of Asp 99 (Jak3) into Glu 101 (Jak1) generated steric hindrance and a Tyr 91 to Phe 93 switch altered the shape of catalytic cleft which collectively prohibited the inhibitor binding. Glutamic Acid 92-95 Janus kinase 1 Homo sapiens 101-105 18346458-8 2008 Furthermore, in-silico mutagenesis of these two residues back to Asp and Tyr enabled Jak1 to accommodate WHI-P131. Aspartic Acid 65-68 Janus kinase 1 Homo sapiens 85-89 18346458-8 2008 Furthermore, in-silico mutagenesis of these two residues back to Asp and Tyr enabled Jak1 to accommodate WHI-P131. Tyrosine 73-76 Janus kinase 1 Homo sapiens 85-89 18413761-0 2008 Triterpenoid CDDO-methyl ester inhibits the Janus-activated kinase-1 (JAK1)-->signal transducer and activator of transcription-3 (STAT3) pathway by direct inhibition of JAK1 and STAT3. triterpenoid TP-222 0-12 Janus kinase 1 Homo sapiens 172-176 18413761-0 2008 Triterpenoid CDDO-methyl ester inhibits the Janus-activated kinase-1 (JAK1)-->signal transducer and activator of transcription-3 (STAT3) pathway by direct inhibition of JAK1 and STAT3. bardoxolone methyl 13-30 Janus kinase 1 Homo sapiens 70-74 18413761-0 2008 Triterpenoid CDDO-methyl ester inhibits the Janus-activated kinase-1 (JAK1)-->signal transducer and activator of transcription-3 (STAT3) pathway by direct inhibition of JAK1 and STAT3. bardoxolone methyl 13-30 Janus kinase 1 Homo sapiens 172-176 17592174-13 2007 The inhibition of JAK1, JAK3, STAT5, ERK1/2, and Akt phosphorylation caused by DHA, SA, and PA is associated with an alteration of CD25 expression at the cell surface. sa 84-86 Janus kinase 1 Homo sapiens 18-22 18281483-3 2008 All three cytokines induced tyrosine phosphorylation of Jak1 and Jak3 in CTCL cell lines and native leukemic (Sezary) cells. Tyrosine 28-36 Janus kinase 1 Homo sapiens 56-60 17645497-0 2007 Auranofin blocks interleukin-6 signalling by inhibiting phosphorylation of JAK1 and STAT3. Auranofin 0-9 Janus kinase 1 Homo sapiens 75-79 17645497-10 2007 Thiol-group-reactive proteins may be involved in AF-induced suppression of JAK1/STAT3 phosphorylation. Sulfhydryl Compounds 0-5 Janus kinase 1 Homo sapiens 75-79 17948269-4 2007 Importantly, inhibition of IL-10-induced STAT3 activation and IL-10-suppressive action by a prolonged exposure to cycloheximide (CHX) was observed to occur also in human monocytes and was caused by a defective IL-10-mediated activation of Jak1 and Tyk2 kinases. Cycloheximide 114-127 Janus kinase 1 Homo sapiens 239-243 17948269-4 2007 Importantly, inhibition of IL-10-induced STAT3 activation and IL-10-suppressive action by a prolonged exposure to cycloheximide (CHX) was observed to occur also in human monocytes and was caused by a defective IL-10-mediated activation of Jak1 and Tyk2 kinases. Cycloheximide 129-132 Janus kinase 1 Homo sapiens 239-243 18052729-11 2007 However, GM-CSF-induced downregulation of Tyk2 and Jak1 tyrosine phosphorylation as well as Tyk2 protein levels likely contributed to the reduced Stat1 tyrosine phosphorylation. Tyrosine 56-64 Janus kinase 1 Homo sapiens 51-55 17919239-6 2007 AG490, a JAK inhibitor, blocked JAK1 phosphorylation accompanied by inhibition of PI3K and Akt activation as well as alpha1(I) collagen mRNA expression, indicating a JAK1-dependent mechanism. alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide 0-5 Janus kinase 1 Homo sapiens 32-36 17919239-6 2007 AG490, a JAK inhibitor, blocked JAK1 phosphorylation accompanied by inhibition of PI3K and Akt activation as well as alpha1(I) collagen mRNA expression, indicating a JAK1-dependent mechanism. alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide 0-5 Janus kinase 1 Homo sapiens 166-170 17785825-8 2007 Treatment of cells with kaempferol did not affect activation of Src kinase by IL-4 but did prevent the phosphorylation of JAK1 and JAK3. kaempferol 24-34 Janus kinase 1 Homo sapiens 122-126 17592174-8 2007 PA, SA, DHA, and EPA decreased JAK1, JAK3, STAT5, and Akt phosphorylation induced by IL-2, but OA and LA did not cause any effect. Protactinium 0-2 Janus kinase 1 Homo sapiens 31-35 17592174-8 2007 PA, SA, DHA, and EPA decreased JAK1, JAK3, STAT5, and Akt phosphorylation induced by IL-2, but OA and LA did not cause any effect. sa 4-6 Janus kinase 1 Homo sapiens 31-35 17592174-13 2007 The inhibition of JAK1, JAK3, STAT5, ERK1/2, and Akt phosphorylation caused by DHA, SA, and PA is associated with an alteration of CD25 expression at the cell surface. Protactinium 92-94 Janus kinase 1 Homo sapiens 18-22 17592174-8 2007 PA, SA, DHA, and EPA decreased JAK1, JAK3, STAT5, and Akt phosphorylation induced by IL-2, but OA and LA did not cause any effect. Dihydroalprenolol 8-11 Janus kinase 1 Homo sapiens 31-35 17592174-8 2007 PA, SA, DHA, and EPA decreased JAK1, JAK3, STAT5, and Akt phosphorylation induced by IL-2, but OA and LA did not cause any effect. Eicosapentaenoic Acid 17-20 Janus kinase 1 Homo sapiens 31-35 17385713-0 2007 Evidence that IL-6-type cytokine signaling in cardiomyocytes is inhibited by oxidative stress: parthenolide targets JAK1 activation by generating ROS. parthenolide 95-107 Janus kinase 1 Homo sapiens 116-120 17592174-13 2007 The inhibition of JAK1, JAK3, STAT5, ERK1/2, and Akt phosphorylation caused by DHA, SA, and PA is associated with an alteration of CD25 expression at the cell surface. Dihydroalprenolol 79-82 Janus kinase 1 Homo sapiens 18-22 17550976-2 2007 We now report marked PRL-induced tyrosine phosphorylation of Jak1, in addition to Jak2, in a series of human breast cancer cell lines, including T47D, MCF7, and SKBR3. Tyrosine 33-41 Janus kinase 1 Homo sapiens 61-65 17550976-7 2007 Instead, PRL activated Jak1 through a Jak2-dependent mechanism, based on disruption of PRL activation of Jak1 after Jak2 suppression by 1) lentiviral delivery of Jak2 short hairpin RNA, 2) adenoviral delivery of dominant-negative Jak2, and 3) AG490 pharmacological inhibition. alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide 243-248 Janus kinase 1 Homo sapiens 23-27 17550976-8 2007 Finally, suppression of Jak1 by lentiviral delivery of Jak1 short hairpin RNA blocked PRL activation of ERK and signal transducer and activator of transcription (Stat)3 and suppressed PRL activation of Jak2, Stat5a, Stat5b, and Akt, as well as tyrosine phosphorylation of PRLR. Tyrosine 244-252 Janus kinase 1 Homo sapiens 24-28 17550976-8 2007 Finally, suppression of Jak1 by lentiviral delivery of Jak1 short hairpin RNA blocked PRL activation of ERK and signal transducer and activator of transcription (Stat)3 and suppressed PRL activation of Jak2, Stat5a, Stat5b, and Akt, as well as tyrosine phosphorylation of PRLR. Tyrosine 244-252 Janus kinase 1 Homo sapiens 55-59 17703129-6 2007 Moreover, we hypothesize that hyperactivation of the JAK kinases, particularly JAK2, mismatched STAT3 serine-tyrosine phosphorylation or heightened STAT3 transcriptional activity, and SOCS3 induction may ultimately prove detrimental. Serine 102-108 Janus kinase 1 Homo sapiens 53-56 17703129-6 2007 Moreover, we hypothesize that hyperactivation of the JAK kinases, particularly JAK2, mismatched STAT3 serine-tyrosine phosphorylation or heightened STAT3 transcriptional activity, and SOCS3 induction may ultimately prove detrimental. Tyrosine 109-117 Janus kinase 1 Homo sapiens 53-56 17385713-3 2007 Activation of Janus kinase 1 (JAK1) tyrosine kinase was markedly reduced by parthenolide. parthenolide 76-88 Janus kinase 1 Homo sapiens 14-28 17385713-3 2007 Activation of Janus kinase 1 (JAK1) tyrosine kinase was markedly reduced by parthenolide. parthenolide 76-88 Janus kinase 1 Homo sapiens 30-34 17385713-4 2007 Pretreatment with parthenolide inhibited JAK1-mediated phosphorylation of the LIF receptor subunits LIF receptor (LIFR) alpha and glycoprotein 130 (gp130), and reduced the LIF-induced increase in JAK1 association with both components. parthenolide 18-30 Janus kinase 1 Homo sapiens 41-45 17385713-4 2007 Pretreatment with parthenolide inhibited JAK1-mediated phosphorylation of the LIF receptor subunits LIF receptor (LIFR) alpha and glycoprotein 130 (gp130), and reduced the LIF-induced increase in JAK1 association with both components. parthenolide 18-30 Janus kinase 1 Homo sapiens 196-200 17385713-7 2007 Pretreatment with the antioxidant, N-acetyl-L-cysteine, completely suppressed the effect of parthenolide on JAK1 and STAT3. Acetylcysteine 35-54 Janus kinase 1 Homo sapiens 108-112 17385713-7 2007 Pretreatment with the antioxidant, N-acetyl-L-cysteine, completely suppressed the effect of parthenolide on JAK1 and STAT3. parthenolide 92-104 Janus kinase 1 Homo sapiens 108-112 17385713-8 2007 From these results, we conclude ROS generation in cardiomyocytes blocks STAT3 signaling of the IL-6-type cytokines by targeting JAK1. Reactive Oxygen Species 32-35 Janus kinase 1 Homo sapiens 128-132 17341659-7 2007 Interestingly, JAK1 inhibitor only in combination with silibinin resulted in a complete reduction in Stat3 phosphorylation at Tyr705, activated caspase-9 and caspase-3, and caused strong PARP cleavage and apoptotic death of DU145 cells. Silybin 55-64 Janus kinase 1 Homo sapiens 15-19 17397165-1 2007 Herein, we describe the design and surface-binding characterization of a de novo designed peptide, JAK1, which undergoes surface-induced folding at the hydroxyapatite (HA)-solution interface. Durapatite 152-166 Janus kinase 1 Homo sapiens 99-103 17570252-0 2007 Exenatide blocks JAK1-STAT1 in pancreatic beta cells. Exenatide 0-9 Janus kinase 1 Homo sapiens 17-21 17397165-2 2007 JAK1 is designed to be unstructured in buffered saline solution, yet undergo HA-induced folding that is largely governed by the periodic positioning of gamma-carboxyglutamic acid (Gla) residues within the primary sequence of the peptide. Sodium Chloride 48-54 Janus kinase 1 Homo sapiens 0-4 17397165-2 2007 JAK1 is designed to be unstructured in buffered saline solution, yet undergo HA-induced folding that is largely governed by the periodic positioning of gamma-carboxyglutamic acid (Gla) residues within the primary sequence of the peptide. 1-Carboxyglutamic Acid 152-178 Janus kinase 1 Homo sapiens 0-4 17397165-2 2007 JAK1 is designed to be unstructured in buffered saline solution, yet undergo HA-induced folding that is largely governed by the periodic positioning of gamma-carboxyglutamic acid (Gla) residues within the primary sequence of the peptide. 1-Carboxyglutamic Acid 180-183 Janus kinase 1 Homo sapiens 0-4 17290288-0 2007 Interferons induce tyrosine phosphorylation of the eIF2alpha kinase PKR through activation of Jak1 and Tyk2. Tyrosine 19-27 Janus kinase 1 Homo sapiens 94-98 17290288-5 2007 Moreover, we provide strong evidence that both the induction of eIF2alpha phosphorylation and inhibition of protein synthesis by IFN are impaired in cells lacking Jak1 or Tyk2, which corresponds to a lack of induction of PKR tyrosine phosphorylation. Tyrosine 225-233 Janus kinase 1 Homo sapiens 163-167 16544577-7 2006 Compared with controls, DHA changed the localization of IL-2R, STAT5a and STAT5b in lipid rafts and suppressed the expression of JAK1, JAK3 and tyrosine phosphotyrosine in soluble membrane fractions. dehydroacetic acid 24-27 Janus kinase 1 Homo sapiens 129-133 17121792-3 2007 The signaling pathways employed by cmvIL-10 were investigated, and the classic IL-10R/JAK1/Stat3 pathway was found to be activated in monocytes. cmvil-10 35-43 Janus kinase 1 Homo sapiens 86-90 16920889-6 2007 Inhibition of JAK1/STAT-3 pathways by piceatannol or ERK1/2 by the MAPK/ERK kinase 1/2 inhibitor U0126 blunted the increase in total protein synthesis. 3,3',4,5'-tetrahydroxystilbene 38-49 Janus kinase 1 Homo sapiens 14-18 16920889-6 2007 Inhibition of JAK1/STAT-3 pathways by piceatannol or ERK1/2 by the MAPK/ERK kinase 1/2 inhibitor U0126 blunted the increase in total protein synthesis. U 0126 97-102 Janus kinase 1 Homo sapiens 14-18 17016659-9 2006 In JAK1 and ISGF3gamma-silenced Hep3B cells, the apoptosis induction and caspase-8 activation levels by IFN, even in combination with 5-FU, were abrogated. Fluorouracil 134-138 Janus kinase 1 Homo sapiens 3-7 16595158-5 2006 This was accomplished by preventing the IFN-alpha-induced tyrosine phosphorylation of STAT-1 and STAT-2 through the inactivation of the upstream receptor associated tyrosine kinases, JAK-1 and Tyk-2. Tyrosine 58-66 Janus kinase 1 Homo sapiens 183-188 16448461-5 2006 H2O2 was increased while glutathione was decreased; these changes were prevented by AG490, suggesting a Janus kinases (JAK)-mediated process. Hydrogen Peroxide 0-4 Janus kinase 1 Homo sapiens 119-122 16448461-5 2006 H2O2 was increased while glutathione was decreased; these changes were prevented by AG490, suggesting a Janus kinases (JAK)-mediated process. Glutathione 25-36 Janus kinase 1 Homo sapiens 119-122 16982750-9 2006 PD98059 also increased back the expression of the MAD2 cell cycle checkpoint protein that was down-regulated during "all JAKs inhibitor"-mediated endoreduplication. 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one 0-7 Janus kinase 1 Homo sapiens 121-125 16843830-3 2006 We found that divalent cadmium (CdCl2) inhibited ciliary neurotrophic factor (CNTF)-mediated Jak1 and Jak2 tyrosine kinase signaling in human BE(2)-C neuroblastoma cells. Cadmium 23-30 Janus kinase 1 Homo sapiens 93-97 16843830-3 2006 We found that divalent cadmium (CdCl2) inhibited ciliary neurotrophic factor (CNTF)-mediated Jak1 and Jak2 tyrosine kinase signaling in human BE(2)-C neuroblastoma cells. Cadmium Chloride 32-37 Janus kinase 1 Homo sapiens 93-97 16474838-0 2006 The mutation in the ATP-binding region of JAK1, identified in human uterine leiomyosarcomas, results in defective interferon-gamma inducibility of TAP1 and LMP2. Adenosine Triphosphate 20-23 Janus kinase 1 Homo sapiens 42-46 15978943-5 2005 Treatment of HL-205 and HL-525 cells with DMSO and HL-205 cells with PMA-induced JAK1 phosphorylation, JAK1/STAT1 association, formation of STAT1-STAT2 heterodimers, and the binding of the active IFN stimulating growth factor 3 (ISGF3) to the IFN-stimulated response element (ISRE) fragment isolated from the 2-5A synthetase promoter. Dimethyl Sulfoxide 42-46 Janus kinase 1 Homo sapiens 81-85 16324217-17 2005 When IFN-alpha binds its receptor, two receptor associated tyrosine kinases, Tyk2 and Jak1 become activated by phosphorylation, and phosphorylate Stat1 and Stat2 on conserved tyrosine residues 13. Tyrosine 59-67 Janus kinase 1 Homo sapiens 86-90 16044161-3 2005 Such effects of curcumin appear to result from suppression of the constitutively active STAT3 through inhibition of Janus kinase 1 (JAK1). Curcumin 16-24 Janus kinase 1 Homo sapiens 116-130 16044161-3 2005 Such effects of curcumin appear to result from suppression of the constitutively active STAT3 through inhibition of Janus kinase 1 (JAK1). Curcumin 16-24 Janus kinase 1 Homo sapiens 132-136 16044161-5 2005 Altogether, our findings suggest a novel function for curcumin, acting as a suppressor of JAK-1 and STAT3 activation in PEL cells, leading to inhibition of proliferation and induction of caspase-dependent apoptosis. Curcumin 54-62 Janus kinase 1 Homo sapiens 90-95 15978943-5 2005 Treatment of HL-205 and HL-525 cells with DMSO and HL-205 cells with PMA-induced JAK1 phosphorylation, JAK1/STAT1 association, formation of STAT1-STAT2 heterodimers, and the binding of the active IFN stimulating growth factor 3 (ISGF3) to the IFN-stimulated response element (ISRE) fragment isolated from the 2-5A synthetase promoter. Dimethyl Sulfoxide 42-46 Janus kinase 1 Homo sapiens 103-107 15894543-3 2005 We investigated the functionality of the Jak1 SH2 domain by stably reconstituting Jak1-defective human fibrosarcoma cells U4C with endogenous amounts of Jak1 in which the crucial arginine residue Arg466 within the SH2 domain has been replaced by lysine. Arginine 179-187 Janus kinase 1 Homo sapiens 41-45 15659558-7 2005 We observed induced phosphorylation on several well documented as well as novel tyrosine phosphorylation sites on proteins involved in IFNalpha signal transduction, such as Tyk2, JAK1, and IFNAR subunits. Tyrosine 80-88 Janus kinase 1 Homo sapiens 179-183 15939634-10 2005 These findings suggest that hypoxia induces the expression of JAK1, JAK2, JAK3 and phospho-STAT1 and -STAT3 in PASMC. pasmc 111-116 Janus kinase 1 Homo sapiens 62-66 15582995-9 2005 The Met-Janus kinase 1-STAT3 signaling pathway may be a major signaling pathway for DCP-induced cell proliferation. dcp 84-87 Janus kinase 1 Homo sapiens 8-22 14978237-7 2004 ICAM-1 promoter activities induced by the overexpression of wild-type JAK1- and PLC-gamma2 were blocked by the PLCgamma2 mutant or the dominant-negative PKCalpha (Lys-->Arg), c-Src (Lys-->Met), or STAT1 (Y701M) mutants, but not by dominant-negative STAT3 (DN) mutants. Lysine 163-166 Janus kinase 1 Homo sapiens 70-74 15123634-2 2004 In this study we demonstrated that inhibitors of histone deacetylase (HDAC) activity, butyrate, trichostatin A, and suberoylanilide hydroxamic acid, prevented IFNgamma-induced JAK1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation. Butyrates 86-94 Janus kinase 1 Homo sapiens 176-180 15123634-2 2004 In this study we demonstrated that inhibitors of histone deacetylase (HDAC) activity, butyrate, trichostatin A, and suberoylanilide hydroxamic acid, prevented IFNgamma-induced JAK1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation. trichostatin A 96-110 Janus kinase 1 Homo sapiens 176-180 15123634-2 2004 In this study we demonstrated that inhibitors of histone deacetylase (HDAC) activity, butyrate, trichostatin A, and suberoylanilide hydroxamic acid, prevented IFNgamma-induced JAK1 activation, STAT1 phosphorylation, its nuclear translocation, and STAT1-dependent gene activation. Vorinostat 116-147 Janus kinase 1 Homo sapiens 176-180 14978237-4 2004 Tyrosine phosphorylation of Janus kinases (JAK) 1/2 was induced by IFN-gamma but not by TPA. Tyrosine 0-8 Janus kinase 1 Homo sapiens 28-51 14978237-6 2004 IFN-gamma-induced tyrosine phosphorylation of phospholipase C (PLC)-gamma was inhibited by AG 490 (a JAK inhibitor), and the association between JAK1/2 and PLC-gamma was increased after IFN-gamma treatment, indicating the activation of PLC-gamma via JAK1/2 phosphorylation. Tyrosine 18-26 Janus kinase 1 Homo sapiens 145-151 14978237-7 2004 ICAM-1 promoter activities induced by the overexpression of wild-type JAK1- and PLC-gamma2 were blocked by the PLCgamma2 mutant or the dominant-negative PKCalpha (Lys-->Arg), c-Src (Lys-->Met), or STAT1 (Y701M) mutants, but not by dominant-negative STAT3 (DN) mutants. Arginine 172-175 Janus kinase 1 Homo sapiens 70-74 14978237-6 2004 IFN-gamma-induced tyrosine phosphorylation of phospholipase C (PLC)-gamma was inhibited by AG 490 (a JAK inhibitor), and the association between JAK1/2 and PLC-gamma was increased after IFN-gamma treatment, indicating the activation of PLC-gamma via JAK1/2 phosphorylation. Tyrosine 18-26 Janus kinase 1 Homo sapiens 145-149 14978237-7 2004 ICAM-1 promoter activities induced by the overexpression of wild-type JAK1- and PLC-gamma2 were blocked by the PLCgamma2 mutant or the dominant-negative PKCalpha (Lys-->Arg), c-Src (Lys-->Met), or STAT1 (Y701M) mutants, but not by dominant-negative STAT3 (DN) mutants. Lysine 185-188 Janus kinase 1 Homo sapiens 70-74 14970177-3 2004 Here we show that vIL-6 is N-linked glycosylated at N78 and N89 and demonstrate that N-linked glycosylation at site N89 of vIL-6 markedly enhances binding to gp130, signaling through the JAK1-STAT1/3 pathway and functions in a cytokine-dependent cell proliferation bioassay. vil-6 18-23 Janus kinase 1 Homo sapiens 187-191 14970177-3 2004 Here we show that vIL-6 is N-linked glycosylated at N78 and N89 and demonstrate that N-linked glycosylation at site N89 of vIL-6 markedly enhances binding to gp130, signaling through the JAK1-STAT1/3 pathway and functions in a cytokine-dependent cell proliferation bioassay. vil-6 123-128 Janus kinase 1 Homo sapiens 187-191 14647450-7 2004 However, inhibition of Jak1 expression also decreased IFN-alpha-induced tyrosine phosphorylation of ErbB3. Tyrosine 72-80 Janus kinase 1 Homo sapiens 23-27 12941469-3 2003 Exposure of human neuroblastoma cells, BE(2)-C, first to tyrosine phosphatase inhibitors (either phenylarsine oxide or PTP inhibitor-2) prevented Jak1, STAT1 and STAT3 activation elicited subsequently by either CNTF or interferon-gamma. oxophenylarsine 97-115 Janus kinase 1 Homo sapiens 146-150 14555918-6 2003 STAT activation is strongly associated with tyrosine phosphorylation by tyrosine kinases, namely Jak1, Jak2, Jak3, and Tyk2. Tyrosine 44-52 Janus kinase 1 Homo sapiens 97-101 12771930-4 2003 Signalling cascade studies revealed that IL-10 stimulated tyrosine phosphorylation of JAK1 and TYK2 receptor kinases and tyrosine phosphorylation of IL-10E1. Tyrosine 58-66 Janus kinase 1 Homo sapiens 86-90 12837923-7 2003 JAK1 and JNK1 were two of the genes shown by the arrays to be down-regulated in RU486-treated endometrial explants. Mifepristone 80-85 Janus kinase 1 Homo sapiens 0-4 12802285-2 2003 IL-10E1 signaling involves tyrosine phosphorylation of the IL-10R JAK1 (Janus kinase) and TYK2 (tyrosine kinase) receptor kinases and tyrosine phosphorylation of two tyrosine moieties (Y57 and Y62) of a LIM domain of the IL-10E1 protein. Tyrosine 27-35 Janus kinase 1 Homo sapiens 66-70 12738762-6 2003 The up-regulation of Fer and its dissociation from Jak1 were accompanied by an augmented association of activated Fer with Stat3 and by a concomitant increase in the tyrosine phosphorylation of Stat3. Tyrosine 166-174 Janus kinase 1 Homo sapiens 51-55 12584205-4 2003 We show that 15-deoxy-Delta12,14-prostaglandin J(2) (15d-PGJ(2)) and rosiglitazone reduce the phosphorylation of STAT1 and STAT3 as well as Janus kinase 1 (JAK1) and JAK2 in activated astrocytes and microglia. 14-prostaglandin j 30-48 Janus kinase 1 Homo sapiens 140-154 12584205-4 2003 We show that 15-deoxy-Delta12,14-prostaglandin J(2) (15d-PGJ(2)) and rosiglitazone reduce the phosphorylation of STAT1 and STAT3 as well as Janus kinase 1 (JAK1) and JAK2 in activated astrocytes and microglia. 14-prostaglandin j 30-48 Janus kinase 1 Homo sapiens 156-160 12584205-4 2003 We show that 15-deoxy-Delta12,14-prostaglandin J(2) (15d-PGJ(2)) and rosiglitazone reduce the phosphorylation of STAT1 and STAT3 as well as Janus kinase 1 (JAK1) and JAK2 in activated astrocytes and microglia. 2-(ETHOXYMETHYL)-4-(4-FLUOROPHENYL)-3-[2-(2-HYDROXYPHENOXY)PYRIMIDIN-4-YL]ISOXAZOL-5(2H)-ONE 57-60 Janus kinase 1 Homo sapiens 140-154 12584205-4 2003 We show that 15-deoxy-Delta12,14-prostaglandin J(2) (15d-PGJ(2)) and rosiglitazone reduce the phosphorylation of STAT1 and STAT3 as well as Janus kinase 1 (JAK1) and JAK2 in activated astrocytes and microglia. 2-(ETHOXYMETHYL)-4-(4-FLUOROPHENYL)-3-[2-(2-HYDROXYPHENOXY)PYRIMIDIN-4-YL]ISOXAZOL-5(2H)-ONE 57-60 Janus kinase 1 Homo sapiens 156-160 12584205-4 2003 We show that 15-deoxy-Delta12,14-prostaglandin J(2) (15d-PGJ(2)) and rosiglitazone reduce the phosphorylation of STAT1 and STAT3 as well as Janus kinase 1 (JAK1) and JAK2 in activated astrocytes and microglia. Rosiglitazone 69-82 Janus kinase 1 Homo sapiens 140-154 12584205-4 2003 We show that 15-deoxy-Delta12,14-prostaglandin J(2) (15d-PGJ(2)) and rosiglitazone reduce the phosphorylation of STAT1 and STAT3 as well as Janus kinase 1 (JAK1) and JAK2 in activated astrocytes and microglia. Rosiglitazone 69-82 Janus kinase 1 Homo sapiens 156-160 12551917-7 2003 We provide evidence that JAK1, like JAK2, phosphorylates Tyr-439 and Tyr-494 in SH2-Bbeta and that PDGF receptor phosphorylates SH2-Bbeta on Tyr-439. Tyrosine 69-72 Janus kinase 1 Homo sapiens 25-29 12589807-2 2003 Making use of Jak-1 or STAT-1 deficient cell lines, we demonstrated that the apoptotic process induced by butyrate is independent of the presence of these proteins. Butyrates 106-114 Janus kinase 1 Homo sapiens 14-19 12551917-7 2003 We provide evidence that JAK1, like JAK2, phosphorylates Tyr-439 and Tyr-494 in SH2-Bbeta and that PDGF receptor phosphorylates SH2-Bbeta on Tyr-439. Tyrosine 57-60 Janus kinase 1 Homo sapiens 25-29 12551917-7 2003 We provide evidence that JAK1, like JAK2, phosphorylates Tyr-439 and Tyr-494 in SH2-Bbeta and that PDGF receptor phosphorylates SH2-Bbeta on Tyr-439. Tyrosine 69-72 Janus kinase 1 Homo sapiens 25-29 12559972-2 2003 Since transphosphorylation of the two kinases is presumed to occur after receptor engagement we examined the phosphorylation by recombinant JAK3 of a peptide substrate corresponding to the JAK1 activation loop (KAIETDKEYYTVKD), which has two adjacent tyrosines. Tyrosine 251-260 Janus kinase 1 Homo sapiens 189-193 12559972-5 2003 Kinetic analysis of the reactions of singly phosphorylated JAK1 activation loop peptides showed that phosphorylating the first or second tyrosine decreased the k(cat)/K(m) for the phosphorylation of the other 115- and 26-fold, respectively. Tyrosine 137-145 Janus kinase 1 Homo sapiens 59-63 11960349-3 2002 The reduced IL-6-mediated STAT3 tyrosine phosphorylation after pre-treatment with TGF-beta1 was associated with apoptosis and coincided with the degradation of certain cellular proteins, including JAK1 and -2 and Tyk2, without affecting the ERK expression and phosphorylation. Tyrosine 32-40 Janus kinase 1 Homo sapiens 197-208 12044887-5 2002 Regulation of inducible ICAM-1 expression by taxifolin was at transcriptional level by inhibiting the activation of signal transducers and activators of transcription (STAT)1 and protein tyrosine phosphorylation of Janus kinase (JAK)1 suggesting that the JAK-STAT pathway may be the molecular site of action of taxifolin. taxifolin 45-54 Janus kinase 1 Homo sapiens 229-234 12177620-5 2002 METHODS: The tyrosine phosphorylation (P-tyr) states of the Janus kinases (Jaks) and signal transducers and activators of transcription (STAT) proteins were examined by immunoprecipitation and immunoblot. Tyrosine 13-21 Janus kinase 1 Homo sapiens 75-79 12177620-5 2002 METHODS: The tyrosine phosphorylation (P-tyr) states of the Janus kinases (Jaks) and signal transducers and activators of transcription (STAT) proteins were examined by immunoprecipitation and immunoblot. Tyrosine 13-16 Janus kinase 1 Homo sapiens 75-79 11882386-3 2002 In the human cell line (SH-SY5Y), STAT1 and STAT3 activation by CNTF-like cytokines showed tyrosine phosphorylation peaking at 0.5 h and inactivating within 2 h. Tyrosine phosphorylation of the receptor-associated tyrosine kinases Jak1 and Jak2 showed a similar time course of activation and inactivation in response to CNTF. Tyrosine 162-170 Janus kinase 1 Homo sapiens 231-235 12018856-2 2002 Although STAT1 activation is primarily induced upon tyrosine phosphorylation by Jak1 and Jak2 (the IFN-gamma receptor-associated tyrosine kinases), the full activation of STAT1 is thought to involve serine phosphorylation by unidentified protein kinases. Tyrosine 52-60 Janus kinase 1 Homo sapiens 80-84 11960349-6 2002 It was shown that in AML cells cultured in the presence of Z-VAD-fmk, TGF-beta1 pretreatment resulted in a reduction of JAK1 phosphorylation upon IL-6 stimulation. benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone 59-68 Janus kinase 1 Homo sapiens 120-124 11442760-8 2001 The kinase upstream of signal transducer and activator of transcription 3, Janus kinase 1, was constitutively tyrosine-phosphorylated in WM9 cells and did not respond to interleukin-6 with increased phosphorylation. Tyrosine 110-118 Janus kinase 1 Homo sapiens 75-89 11751854-9 2002 However, SH2-B beta bound to both and was tyrosyl-phosphorylated by JAK1. cyclo(tyrosyl-tyrosyl) 42-49 Janus kinase 1 Homo sapiens 68-72 11751854-11 2002 APS also decreased tyrosyl phosphorylation of JAK1, but did not affect the activity or tyrosyl phosphorylation of JAK3. Adenosine Phosphosulfate 0-3 Janus kinase 1 Homo sapiens 46-50 11751854-11 2002 APS also decreased tyrosyl phosphorylation of JAK1, but did not affect the activity or tyrosyl phosphorylation of JAK3. cyclo(tyrosyl-tyrosyl) 19-26 Janus kinase 1 Homo sapiens 46-50 11751854-12 2002 Overexpressed APS bound to and was tyrosyl-phosphorylated by all three JAKs. Adenosine Phosphosulfate 14-17 Janus kinase 1 Homo sapiens 71-75 11751854-12 2002 Overexpressed APS bound to and was tyrosyl-phosphorylated by all three JAKs. cyclo(tyrosyl-tyrosyl) 35-42 Janus kinase 1 Homo sapiens 71-75 11438544-6 2001 In addition to PI3K and Akt, JAK1, JAK2, and the tyrosine 440 STAT1 docking residue of IFNGR1 are required for STAT1 to be phosphorylated on serine. Serine 141-147 Janus kinase 1 Homo sapiens 29-33 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Tyrosine 183-186 Janus kinase 1 Homo sapiens 226-230 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Tyrosine 183-186 Janus kinase 1 Homo sapiens 299-303 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Tyrosine 250-253 Janus kinase 1 Homo sapiens 226-230 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Tyrosine 250-253 Janus kinase 1 Homo sapiens 299-303 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Tyrosine 250-253 Janus kinase 1 Homo sapiens 226-230 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Tyrosine 250-253 Janus kinase 1 Homo sapiens 299-303 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Serine 308-311 Janus kinase 1 Homo sapiens 226-230 11438544-7 2001 Taken together, these results suggest that the following events lead to the activation of STAT1 upon IFN gamma stimulation: 1) PI3K and Akt are activated by the occupied receptor and Tyr-440 is phosphorylated by the activated JAKs; 2) STAT1 docks to Tyr-440; and 3) Tyr-701 is phosphorylated by the JAKs and Ser-727 is phosphorylated by a kinase downstream of Akt. Serine 308-311 Janus kinase 1 Homo sapiens 299-303 11751854-14 2002 These results suggest that 1) SH2-B beta specifically activates JAK2, 2) APS negatively regulates both JAK2 and JAK1, and 3) both SH2-B beta and APS may serve as adapter proteins for all three JAKs independent of any role they have in JAK activity. Adenosine Phosphosulfate 73-76 Janus kinase 1 Homo sapiens 112-116 11751854-14 2002 These results suggest that 1) SH2-B beta specifically activates JAK2, 2) APS negatively regulates both JAK2 and JAK1, and 3) both SH2-B beta and APS may serve as adapter proteins for all three JAKs independent of any role they have in JAK activity. Adenosine Phosphosulfate 73-76 Janus kinase 1 Homo sapiens 193-197 11751854-14 2002 These results suggest that 1) SH2-B beta specifically activates JAK2, 2) APS negatively regulates both JAK2 and JAK1, and 3) both SH2-B beta and APS may serve as adapter proteins for all three JAKs independent of any role they have in JAK activity. Adenosine Phosphosulfate 73-76 Janus kinase 1 Homo sapiens 64-67 11751854-14 2002 These results suggest that 1) SH2-B beta specifically activates JAK2, 2) APS negatively regulates both JAK2 and JAK1, and 3) both SH2-B beta and APS may serve as adapter proteins for all three JAKs independent of any role they have in JAK activity. Adenosine Phosphosulfate 145-148 Janus kinase 1 Homo sapiens 112-116 11751854-14 2002 These results suggest that 1) SH2-B beta specifically activates JAK2, 2) APS negatively regulates both JAK2 and JAK1, and 3) both SH2-B beta and APS may serve as adapter proteins for all three JAKs independent of any role they have in JAK activity. Adenosine Phosphosulfate 145-148 Janus kinase 1 Homo sapiens 193-197 11751854-14 2002 These results suggest that 1) SH2-B beta specifically activates JAK2, 2) APS negatively regulates both JAK2 and JAK1, and 3) both SH2-B beta and APS may serve as adapter proteins for all three JAKs independent of any role they have in JAK activity. Adenosine Phosphosulfate 145-148 Janus kinase 1 Homo sapiens 64-67 12661403-7 2002 The connections of IL-2R or IL-12R with their ligands recruit receptor-associated cytoplasmic proteins from the JAK family (JAK1/JAK3 or JAK2/TYK2, respectively), which catalyze the phosphorylation of themselves and intrinsic tyrosine residues on the receptor, creating STAT docking sites. Tyrosine 226-234 Janus kinase 1 Homo sapiens 112-115 12661403-7 2002 The connections of IL-2R or IL-12R with their ligands recruit receptor-associated cytoplasmic proteins from the JAK family (JAK1/JAK3 or JAK2/TYK2, respectively), which catalyze the phosphorylation of themselves and intrinsic tyrosine residues on the receptor, creating STAT docking sites. Tyrosine 226-234 Janus kinase 1 Homo sapiens 124-128 11468294-4 2001 Substitution of Tyr(107) to alanine, a residue conserved among Jaks and involved in hydrophobic core interactions of the proposed beta-grasp domain, abrogated binding of full-length Jak1 to gp130 in COS-7 transfectants. carbonyl sulfide 199-202 Janus kinase 1 Homo sapiens 182-186 11369622-3 2001 This study reports that SDF-1alpha can stimulate the tyrosine phosphorylation of Janus kinase 2 (JAK2) and other members of the JAK/signal transduction and activation of transcription (STAT) family, including JAK1, tyrosine kinase 2, STAT2, and STAT4 in the human progenitor cell line, CTS. Tyrosine 53-61 Janus kinase 1 Homo sapiens 209-213 11294841-7 2001 The results obtained showed an activation of Janus kinases (JAK1, JAK2, and TYK2) leading to a tyrosine phosphorylation of the gp130 and LIFR. Tyrosine 95-103 Janus kinase 1 Homo sapiens 60-64 11160325-6 2001 Fes appears to be a downstream kinase from Jak1/Jak3 in this process. Iron 0-3 Janus kinase 1 Homo sapiens 43-47 11162588-1 2001 We have previously shown that interferon-alpha (IFN alpha)-dependent tyrosine phosphorylation of insulin receptor substrate-1 (IRS-1) is impaired by serine phosphorylation of IRS-1 due to the reduced ability of serine phosphorylated IRS-1 to serve as a substrate for Janus kinase 1 (JAK1). Serine 211-217 Janus kinase 1 Homo sapiens 267-281 11162588-1 2001 We have previously shown that interferon-alpha (IFN alpha)-dependent tyrosine phosphorylation of insulin receptor substrate-1 (IRS-1) is impaired by serine phosphorylation of IRS-1 due to the reduced ability of serine phosphorylated IRS-1 to serve as a substrate for Janus kinase 1 (JAK1). Serine 211-217 Janus kinase 1 Homo sapiens 283-287 11162588-1 2001 We have previously shown that interferon-alpha (IFN alpha)-dependent tyrosine phosphorylation of insulin receptor substrate-1 (IRS-1) is impaired by serine phosphorylation of IRS-1 due to the reduced ability of serine phosphorylated IRS-1 to serve as a substrate for Janus kinase 1 (JAK1). Tyrosine 69-77 Janus kinase 1 Homo sapiens 267-281 11162588-1 2001 We have previously shown that interferon-alpha (IFN alpha)-dependent tyrosine phosphorylation of insulin receptor substrate-1 (IRS-1) is impaired by serine phosphorylation of IRS-1 due to the reduced ability of serine phosphorylated IRS-1 to serve as a substrate for Janus kinase 1 (JAK1). Tyrosine 69-77 Janus kinase 1 Homo sapiens 283-287 11162588-4 2001 Importantly, only FRAP-dependent IRS-1(511-772) serine phosphorylation inhibited by 50% subsequent JAK1-dependent tyrosine phosphorylation of IRS-1. Serine 48-54 Janus kinase 1 Homo sapiens 99-103 11162588-1 2001 We have previously shown that interferon-alpha (IFN alpha)-dependent tyrosine phosphorylation of insulin receptor substrate-1 (IRS-1) is impaired by serine phosphorylation of IRS-1 due to the reduced ability of serine phosphorylated IRS-1 to serve as a substrate for Janus kinase 1 (JAK1). Serine 149-155 Janus kinase 1 Homo sapiens 267-281 11162588-4 2001 Importantly, only FRAP-dependent IRS-1(511-772) serine phosphorylation inhibited by 50% subsequent JAK1-dependent tyrosine phosphorylation of IRS-1. Tyrosine 114-122 Janus kinase 1 Homo sapiens 99-103 11162588-1 2001 We have previously shown that interferon-alpha (IFN alpha)-dependent tyrosine phosphorylation of insulin receptor substrate-1 (IRS-1) is impaired by serine phosphorylation of IRS-1 due to the reduced ability of serine phosphorylated IRS-1 to serve as a substrate for Janus kinase 1 (JAK1). Serine 149-155 Janus kinase 1 Homo sapiens 283-287 11162588-6 2001 Taken together, these data indicate that FRAP, but not p70(s6k), is a likely physiologic IRS-1 serine kinase that negatively regulates JAK1-dependent IRS-1 tyrosine phosphorylation and suggests that FRAP may modulate IRS-dependent cytokine signaling. Tyrosine 156-164 Janus kinase 1 Homo sapiens 135-139 10993906-6 2000 STAM2 is downstream of the Jak family of kinases since coexpression of STAM2 with Jak1 or Jak2 but not an unrelated Tec family kinase, Etk, resulted in its tyrosine phosphorylation. Tyrosine 156-164 Janus kinase 1 Homo sapiens 27-30 11133764-4 2001 In cotransfection experiments, JAB/SOCS1/SSI-1 associates with both Jak1 and Jak3; however, JAB/SOCS1/SSI-1 had a greater effect on Jak1 tyrosine phosphorylation and kinase activity. Tyrosine 137-145 Janus kinase 1 Homo sapiens 132-136 11163041-5 2001 The induction of protein tyrosine phosphorylation of proteins including PTKs, janus kinase (JAK)1, and JAK2, was examined by Western blotting and immunoprecipitation. Tyrosine 25-33 Janus kinase 1 Homo sapiens 78-97 11163041-7 2001 RESULTS: IFN 1 (Interferon) induced tyrosine phosphorylation of multiple substrates, particularly that of 75,000; 90,000; 130,000; and 160,000 molecular weight proteins including JAK1 and JAK2 in cultured HCE cells. Tyrosine 36-44 Janus kinase 1 Homo sapiens 179-183 11163041-11 2001 CONCLUSIONS: Tyrosine phosphorylation of proteins including JAK1 and JAK2 is essential for IFN-gamma-induction of MHC class II expression, but not critical for that of ICAM-1 expression in cultured HCE cells. Tyrosine 13-21 Janus kinase 1 Homo sapiens 60-64 10993906-6 2000 STAM2 is downstream of the Jak family of kinases since coexpression of STAM2 with Jak1 or Jak2 but not an unrelated Tec family kinase, Etk, resulted in its tyrosine phosphorylation. Tyrosine 156-164 Janus kinase 1 Homo sapiens 82-86 11046056-8 2000 Jak1 was inhibited at the level of tyrosine phosphorylation, indicating that inhibition occurred at least in part upstream of Stats in the Jak-Stat pathway. Tyrosine 35-43 Janus kinase 1 Homo sapiens 0-4 10875931-4 2000 Tyrosine kinases, Jak1 and Jak3, involved in IL-4 signaling can associate with SHIP, yet only Jak1 can tyrosine-phosphorylate SHIP when co-expressed. Tyrosine 103-111 Janus kinase 1 Homo sapiens 18-22 10982844-5 2000 Nuclear presence of tyrosine-phosphorylated STAT1 could be restored in Jak1-deficient cells by leptomycin B, an inhibitor of nuclear export. Tyrosine 20-28 Janus kinase 1 Homo sapiens 71-75 10982844-5 2000 Nuclear presence of tyrosine-phosphorylated STAT1 could be restored in Jak1-deficient cells by leptomycin B, an inhibitor of nuclear export. leptomycin B 95-107 Janus kinase 1 Homo sapiens 71-75 10982844-8 2000 Impaired binding of the transcriptional coactivator CBP to tyrosine-phosphorylated STAT1 derived from Jak1-deficient cells offers a model for the intermolecular regulation of the nuclear export sequence. Tyrosine 59-67 Janus kinase 1 Homo sapiens 102-106 11096454-5 2000 The receptor blockade by mAb 51.44 and 234.28 resulted in the inhibition of IFN-alpha2a and IFN-beta-induced tyrosine phosphorylation of Jak1, Tyk2, Stat1/2/3, and IFNAR-1/2 and inhibition of IFN-stimulated gene factor 3 (ISGF3) formation. Tyrosine 109-117 Janus kinase 1 Homo sapiens 137-141 10875931-4 2000 Tyrosine kinases, Jak1 and Jak3, involved in IL-4 signaling can associate with SHIP, yet only Jak1 can tyrosine-phosphorylate SHIP when co-expressed. Tyrosine 103-111 Janus kinase 1 Homo sapiens 94-98 10747872-5 2000 Moreover, tyrosine phosphorylation of STAT3, JAK1, and JAK2 was increased upon IGF-I stimulation of endogenous IGF-IR in 293T cells transfected with the respective STAT or JAK expression vector. Tyrosine 10-18 Janus kinase 1 Homo sapiens 45-49 10918594-3 2000 Analysis of the early signals triggered by IFN-alpha and IFN-beta demonstrated that the two IFNs were similarly effective in inducing tyrosine phosphorylation of the Jak-1 and Tyk-2 kinases and the transcription factors Stat-1 and Stat-2. Tyrosine 134-142 Janus kinase 1 Homo sapiens 166-171 10747872-7 2000 Dominant-negative JAK1 or JAK2 was able to block the IGF-IR-mediated tyrosine phosphorylation of STAT3 in 293T cells. Tyrosine 69-77 Janus kinase 1 Homo sapiens 18-22 10586107-5 1999 Type I IFN induces the phosphorylation of STAT1 and STAT2 proteins by tyrosine phosphorylation involving the type I IFN receptor-associated tyrosine kinases TYK2 and JAK1. Tyrosine 70-78 Janus kinase 1 Homo sapiens 166-170 10660600-1 2000 Degenerate polymerase chain reaction against conserved kinase catalytic subdomains identified 15 tyrosine and serine-threonine kinases expressed in surgically removed prostatic carcinoma tissues, including six receptor kinases (PDGFBR, IGF1-R, VEGFR2, MET, RYK, and EPH-A1), six non-receptor kinases (ABL, JAK1, JAK2, TYK2, PLK-1, and EMK), and three novel kinases. Tyrosine 97-105 Janus kinase 1 Homo sapiens 306-310 10666284-4 2000 Moreover, tyrosine phosphorylation of Jak1 in response to IFN-alpha was unaffected at the early phase of infection, suggesting that oligomerization of the receptor subunits proceeded normally. Tyrosine 10-18 Janus kinase 1 Homo sapiens 38-42 10488146-0 1999 JAK1-dependent phosphorylation of insulin receptor substrate-1 (IRS-1) is inhibited by IRS-1 serine phosphorylation. Serine 93-99 Janus kinase 1 Homo sapiens 0-4 10488146-3 1999 In addition, we demonstrate that serine phosphorylation of IRS-1 renders it a poorer substrate for JAK1 (Janus kinase-1). Serine 33-39 Janus kinase 1 Homo sapiens 99-103 10488146-8 1999 Taken together, these data indicate that serine phosphorylation of IRS-1 prevents its subsequent tyrosine phosphorylation by JAK1 and suggest that IRS-1 serine phosphorylation may play a counter-regulatory role in pathways outside the insulin signaling system. Tyrosine 97-105 Janus kinase 1 Homo sapiens 125-129 10488146-3 1999 In addition, we demonstrate that serine phosphorylation of IRS-1 renders it a poorer substrate for JAK1 (Janus kinase-1). Serine 33-39 Janus kinase 1 Homo sapiens 105-119 10488146-8 1999 Taken together, these data indicate that serine phosphorylation of IRS-1 prevents its subsequent tyrosine phosphorylation by JAK1 and suggest that IRS-1 serine phosphorylation may play a counter-regulatory role in pathways outside the insulin signaling system. Serine 153-159 Janus kinase 1 Homo sapiens 125-129 10488146-8 1999 Taken together, these data indicate that serine phosphorylation of IRS-1 prevents its subsequent tyrosine phosphorylation by JAK1 and suggest that IRS-1 serine phosphorylation may play a counter-regulatory role in pathways outside the insulin signaling system. Serine 41-47 Janus kinase 1 Homo sapiens 125-129 10404396-5 1999 It is clear that PRL activates the tyrosine phosphorylation of several proteins, including members of a novel family of protein tyrosine kinases, the Janus Kinases (JAKs). Tyrosine 35-43 Janus kinase 1 Homo sapiens 165-169 10433356-6 1999 STAT3 binds to these sites via its SH2 (Src homology 2) domain, and is, in turn, tyrosine-phosphorylated by the receptor-associated JAKs. Tyrosine 81-89 Janus kinase 1 Homo sapiens 132-136 10409622-9 1999 A glutathione S-transferase fusion protein of the cytoplasmic domain of IL-13Ralpha was phosphorylated on tyrosine in vitro by JAK1, JAK3, and Tyk2, although the tyrosine phosphorylation events mediated by Tyk2 and JAK3 were not detectable using anti-phosphotyrosine antibodies. Tyrosine 106-114 Janus kinase 1 Homo sapiens 127-131 10373548-5 1999 Tyrosine phosphorylation of SOCS-3 was observed upon coexpression with Jak1 and Jak2 but only weakly with Jak3. Tyrosine 0-8 Janus kinase 1 Homo sapiens 71-75 10373548-7 1999 Moreover, following IL-2 stimulation of T cells, SOCS-3 was able to interact with the IL-2 receptor complex, and in particular tyrosine phosphorylated Jak1 and IL-2Rbeta. Tyrosine 127-135 Janus kinase 1 Homo sapiens 151-155 10502458-2 1999 In addition, growth hormone (GH) stimulates tyrosine phosphorylation of Jak1 and Jak3 in certain cell lines, while the effect on Tyk2 has not been analysed. Tyrosine 44-52 Janus kinase 1 Homo sapiens 72-76 10037026-2 1999 Wild type Jak3 was able to tyrosine phosphorylate a kinase-dead Jak1 (Jak1E908). Tyrosine 27-35 Janus kinase 1 Homo sapiens 64-68 10080544-1 1999 Binding of interferon-gamma (IFN-gamma) to its heterodimeric receptor induces activation of the tyrosine kinases JAK1 and JAK2 followed by tyrosine phosphorylation of STAT1alpha. Tyrosine 96-104 Janus kinase 1 Homo sapiens 113-117 10224470-7 1999 RESULTS: We show that binding of IFN-gamma to human eosinophils initiated a series of events that resulted in the rapid tyrosine phosphorylation of not only the IFN-gammaRalpha chain but also Jak1, Jak2, and Stat1alpha. Tyrosine 120-128 Janus kinase 1 Homo sapiens 192-196 9935235-9 1999 Furthermore, stimulation of IMC-2 cells with rG-CSF induced rapid activation of tyrosine-phosphorylated JAK1, suggesting that the G-CSF signal may be transduced into the cells through G-CSFR. Tyrosine 80-88 Janus kinase 1 Homo sapiens 104-108 10229853-4 1999 We demonstrate that HCMV inhibits IFN-alpha-stimulated MHC class I, IFN regulatory factor-1, MxA and 2",5-oligoadenylate synthetase gene expression, transcription factor activation, and signaling in infected fibroblasts and endothelial cells by decreasing the expression of Janus kinase 1 and p48, two essential components of the IFN-alpha signal transduction pathway. hcmv 20-24 Janus kinase 1 Homo sapiens 274-288 10408379-3 1999 JAK1 but not JAK2 was tyrosine phosphorylated in response to sublytic C5b-9. Tyrosine 22-30 Janus kinase 1 Homo sapiens 0-4 10233717-6 1999 In vitro analyses using synthetic peptides of this region showed that the tyrosine kinase Janus kinase 1 (JAK1), as well as IRS-1 and IRS-2 bind to the I4R motif irrespective of the polymorphism or a tyrosine phosphorylation. Tyrosine 74-82 Janus kinase 1 Homo sapiens 90-104 10233717-6 1999 In vitro analyses using synthetic peptides of this region showed that the tyrosine kinase Janus kinase 1 (JAK1), as well as IRS-1 and IRS-2 bind to the I4R motif irrespective of the polymorphism or a tyrosine phosphorylation. Tyrosine 74-82 Janus kinase 1 Homo sapiens 106-110 10037026-2 1999 Wild type Jak3 was able to tyrosine phosphorylate a kinase-dead Jak1 (Jak1E908). Tyrosine 27-35 Janus kinase 1 Homo sapiens 70-78 10037026-6 1999 By comparison only IL2Rbeta was recognized and tyrosine phosphorylated by wild-type Jak1. Tyrosine 47-55 Janus kinase 1 Homo sapiens 84-88 9278334-8 1997 Furthermore, the tyrosine phosphorylation of STAT1 and the tyrosine kinases JAK1 and JAK2 was enhanced significantly in RGD-adherent monocytes compared with control cells. Tyrosine 17-25 Janus kinase 1 Homo sapiens 76-80 9849880-0 1998 Constitutive association of JAK1 and STAT5 in pro-B cells is dissolved by interleukin-4-induced tyrosine phosphorylation of both proteins. Tyrosine 96-104 Janus kinase 1 Homo sapiens 28-32 9794795-7 1998 It is concluded that Jak1 is required for the tyrosine phosphorylation of SHP2. Tyrosine 46-54 Janus kinase 1 Homo sapiens 21-25 9774657-6 1998 We also found that Jak1 interacts with p85 in the absence of IL-2Rbeta and that IL-2Rbeta and Jak1 cooperate for the efficient recruitment and tyrosine phosphorylation of p85. Tyrosine 143-151 Janus kinase 1 Homo sapiens 94-98 9788278-6 1998 In this study, we report that PDGF- and CNTF-induced OL progenitors responded with a rapid tyrosine phosphorylation of JAK1, JAK2, STAT1alpha/beta, and STAT3. Tyrosine 91-99 Janus kinase 1 Homo sapiens 119-123 9520455-1 1998 Interleukin 2 (IL-2) rapidly induces tyrosine phosphorylation of intracellular substrates, including the IL-2 receptor beta chain (IL-2Rbeta), Janus kinase 1 (Jak1), Jak3, signal transducer/activator of transcription proteins, and Shc, but the mechanism underlying dephosphorylation of these proteins is not known. Tyrosine 37-45 Janus kinase 1 Homo sapiens 143-157 9520455-1 1998 Interleukin 2 (IL-2) rapidly induces tyrosine phosphorylation of intracellular substrates, including the IL-2 receptor beta chain (IL-2Rbeta), Janus kinase 1 (Jak1), Jak3, signal transducer/activator of transcription proteins, and Shc, but the mechanism underlying dephosphorylation of these proteins is not known. Tyrosine 37-45 Janus kinase 1 Homo sapiens 159-163 9520455-3 1998 We have found that IL-2 induces association of SHP-1 with the IL-2 receptor complex, and that once SHP-1 is recruited to the activated receptor it is able to decrease tyrosine phosphorylation of IL-2Rbeta and the associated tyrosine kinases Jak1 and Jak3. Tyrosine 167-175 Janus kinase 1 Homo sapiens 241-245 9452436-4 1998 G-CSF-dependent tyrosyl phosphorylation of Jak1 and Jak2 occurred in all three cell lines. cyclo(tyrosyl-tyrosyl) 16-23 Janus kinase 1 Homo sapiens 43-47 9637709-1 1998 PDGF stimulates tyrosine phosphorylation of Janus kinase 1 (JAK1) and the signal transducer and activator of transcription 1 (STAT1alpha). Tyrosine 16-24 Janus kinase 1 Homo sapiens 44-58 9637709-1 1998 PDGF stimulates tyrosine phosphorylation of Janus kinase 1 (JAK1) and the signal transducer and activator of transcription 1 (STAT1alpha). Tyrosine 16-24 Janus kinase 1 Homo sapiens 60-64 9610741-6 1998 Upon stimulation with IL-6/sIL-6R, the gp130, cytoplasmic Janus kinases JAK1 and JAK2 were tyrosine phosphorylated. Tyrosine 91-99 Janus kinase 1 Homo sapiens 72-76 9516124-7 1998 IL-5 stimulation resulted in tyrosine phosphorylation of JAK2, JAK1, betac, and STAT5. Tyrosine 29-37 Janus kinase 1 Homo sapiens 63-67 9516124-9 1998 Furthermore, tyrosine phosphorylation of JAK1 was dependent on the activation of JAK2. Tyrosine 13-21 Janus kinase 1 Homo sapiens 41-45 9452495-6 1998 MK stimulates tyrosine phosphorylation of JAK1, JAK2, and STAT1alpha. Tyrosine 14-22 Janus kinase 1 Homo sapiens 42-46 9382798-0 1997 Janus kinases in interleukin-2-mediated signaling: JAK1 and JAK3 are differentially regulated by tyrosine phosphorylation. Tyrosine 97-105 Janus kinase 1 Homo sapiens 51-55 9382798-2 1997 Many cytokines activate receptor-associated Janus kinases (JAKs) that promote tyrosine phosphorylation of signal transducers and activators of transcription (STAT) factors. Tyrosine 78-86 Janus kinase 1 Homo sapiens 59-63 9382798-3 1997 Although JAK activation has been correlated with phosphorylation, the role of this tyrosine phosphorylation in the regulation of JAK1 and JAK3 remains unclear. Tyrosine 83-91 Janus kinase 1 Homo sapiens 129-133 9382798-5 1997 RESULTS: We targeted two conserved tyrosine residues within the activation loop of the JAK1 and JAK3 kinase domains for substitution with phenylalanines. Tyrosine 35-43 Janus kinase 1 Homo sapiens 87-91 9382798-5 1997 RESULTS: We targeted two conserved tyrosine residues within the activation loop of the JAK1 and JAK3 kinase domains for substitution with phenylalanines. Phenylalanine 138-152 Janus kinase 1 Homo sapiens 87-91 9382798-6 1997 In an overexpression system, the catalytic function of JAK1 strictly required the presence of the first of these tyrosines, Y1033. Tyrosine 113-122 Janus kinase 1 Homo sapiens 55-59 9382798-6 1997 In an overexpression system, the catalytic function of JAK1 strictly required the presence of the first of these tyrosines, Y1033. y1033 124-129 Janus kinase 1 Homo sapiens 55-59 9382798-11 1997 CONCLUSIONS: JAK1 and JAK3 are differentially regulated by specific tyrosines within their respective activation loops. Tyrosine 68-77 Janus kinase 1 Homo sapiens 13-17 9199317-2 1997 The Janus family of tyrosine kinases (Jak1, Jak2, Jak3, and Tyk2) is required for cytokine-induced tyrosine phosphorylation and dimerization of the Stat proteins. Tyrosine 20-28 Janus kinase 1 Homo sapiens 38-42 9202126-6 1997 Interaction of JAB with Jak1, Jak2 or Jak3 markedly reduces their tyrosine-kinase activity and suppresses the tyrosine-phosphorylation and activation of STATs. Tyrosine 66-74 Janus kinase 1 Homo sapiens 24-28 9212064-1 1997 Several different Janus kinases (JAKs) and signal transducers and activation of transcription (STATs) have been implicated in mediating the biological responses induced by PRL, based on their ligand-dependent tyrosine phosphorylation and activation. Tyrosine 209-217 Janus kinase 1 Homo sapiens 33-37 9159166-7 1997 Disruption of the Jak1-binding proline-rich Box1 region of IL-4Ralpha abolished signaling by this chimeric receptor. Proline 31-38 Janus kinase 1 Homo sapiens 18-22 9199189-6 1997 In contrast, IL-4 stimulated tyrosine phosphorylation of JAK1, JAK2 and tyk2 in this cell line. Tyrosine 29-37 Janus kinase 1 Homo sapiens 57-61 9135582-2 1997 We have identified that hPL rapidly stimulated the tyrosine phosphorylation of at least 7 proteins including Janus Kinases (JAK1 and JAK2) and a signal transducer and activator of transcription protein (Stat3). Tyrosine 51-59 Janus kinase 1 Homo sapiens 124-128 9162019-4 1997 This sustained STAT5 activation can be blocked by protein kinase inhibitors, which is consistent with the ability of the proteasome inhibitor to stabilize IL-2-induced tyrosine phosphorylation of Jak1 and Jak3. Tyrosine 168-176 Janus kinase 1 Homo sapiens 196-200 9178903-5 1997 Furthermore, Jak1 but not Jak2 induces tyrosine phosphorylation of Btk, but not Tec. Tyrosine 39-47 Janus kinase 1 Homo sapiens 13-17 9178903-6 1997 These observations suggest that upon cytokine stimulation JAKs activate Tec/Btk or induce their dimerization resulting in endogenous tyrosine phosphorylation. Tyrosine 133-141 Janus kinase 1 Homo sapiens 58-62 9209327-7 1997 JAK1 and STAT5 were constitutively tyrosine-phosphorylated but the DNA binding activity of STAT5 was not induced. Tyrosine 35-43 Janus kinase 1 Homo sapiens 0-4 9045682-0 1997 Jak1 expression is required for mediating interleukin-4-induced tyrosine phosphorylation of insulin receptor substrate and Stat6 signaling molecules. Tyrosine 64-72 Janus kinase 1 Homo sapiens 0-4 9209410-4 1997 Furthermore, we revealed that two proline residues in the box1 region, which is conserved in the IL-2 receptor beta chain and the alpha chains of the cytokine receptors, are essentially involved in association with Jak1. Proline 34-41 Janus kinase 1 Homo sapiens 215-219 9045682-1 1997 The Jak1, Jak2, Jak3, and Fes tyrosine kinases have been demonstrated to undergo tyrosine phosphorylation in response to interleukin (IL)-4 stimulation in different cell systems. Tyrosine 30-38 Janus kinase 1 Homo sapiens 4-8 9045682-7 1997 Reconstitution of Jak1 expression in E1C3 cells restored the ability of IL-4 to induce IRS and Stat6 tyrosine phosphorylation. Tyrosine 101-109 Janus kinase 1 Homo sapiens 18-22 9045682-8 1997 These results provide evidence that Jak1 expression is required for mediating tyrosine phosphorylation and activation of crucial molecules involved in IL-4 signal transduction. Tyrosine 78-86 Janus kinase 1 Homo sapiens 36-40 9036989-6 1997 Treatment of cells with wortmannin also inhibited the phosphorylation of the p85 subunit of PI 3"-kinase and the type I IFN-regulated activation of the Map kinase, but had no inhibitory effect on the IFN-alpha-induced activation of Tyk-2 and Jak-1 kinases nor on the activation of Stat-1, Stat-2, and Stat-3. Wortmannin 24-34 Janus kinase 1 Homo sapiens 242-247 9013940-0 1997 The IL-4-induced tyrosine phosphorylation of the insulin receptor substrate is dependent on JAK1 expression in human fibrosarcoma cells. Tyrosine 17-25 Janus kinase 1 Homo sapiens 92-96 9047382-3 1997 In signaling from gp130, a common signal transducer for the IL-6 family cytokines, STAT3, a transcription factor that contains an SH2 domain, is recruited by phosphotyrosines on gp130 and is subsequently phosphorylated by gp130-associated JAKs. Phosphotyrosine 158-174 Janus kinase 1 Homo sapiens 239-243 9013940-1 1997 It has been shown that IL-4 induces the tyrosine phosphorylation of JAK1 and JAK3 in the majority of hemopoietic cell types, and JAK2 and TYK2 in several other types. Tyrosine 40-48 Janus kinase 1 Homo sapiens 68-72 9013940-3 1997 To determine whether JAKs play a role in activating a signal transduction pathway different from the classical JAK/STAT pathway, we analyzed the ability of huIL-4 to stimulate the tyrosine phosphorylation of one of its major cellular substrates, the insulin receptor substrate (IRS). Tyrosine 180-188 Janus kinase 1 Homo sapiens 21-25 9013940-4 1997 Using human fibrosarcoma cell lines with mutations in JAK1, JAK2, and TYK2, we found that expression of functional JAK1, but not TYK2 or JAK2, is essential for IL-4-induced tyrosine phosphorylation of IRS. Tyrosine 173-181 Janus kinase 1 Homo sapiens 115-119 8759739-3 1996 We have previously demonstrated that IFN-gamma-induced class II expression in glial cells involves activation of both tyrosine kinase and protein kinase C. IFN-gamma induces tyrosine phosphorylation of the tyrosine kinases Jak1 and Jak2 and of Stat1 alpha. Tyrosine 118-126 Janus kinase 1 Homo sapiens 223-227 8940193-4 1996 There was low level tyrosine phosphorylation of JAKs 1, 2, and 3 in Bcr/Abl-transformed cells, but no detectable complex formation with Bcr/Abl, and activation of STAT5 by P210 was not blocked by two different dominant-negative JAK mutants. Tyrosine 20-28 Janus kinase 1 Homo sapiens 48-64 8887543-5 1996 The activated Eyk kinases specifically stimulate tyrosine phosphorylation of STAT1, STAT3 and JAK1. Tyrosine 49-57 Janus kinase 1 Homo sapiens 94-98 8892755-6 1996 Our results demonstrate that c-JH1 and c-JH2 associate with each other and c-JH2 can be tyrosine-phosphorylated by c-JAK1 and by c-JH(1 + 2). Tyrosine 88-96 Janus kinase 1 Homo sapiens 117-121 8628273-1 1996 Binding of alpha interferon (IFNalpha) to its receptors induces rapid tyrosine phosphorylation of the receptor subunits IFNaR1 and IFNaR2, the TYK2 and JAK1 tyrosine kinases, and the Stat1 and Stat2 transcription factors. Tyrosine 70-78 Janus kinase 1 Homo sapiens 152-156 8700538-1 1996 Interferon-alpha induces the rapid tyrosine phosphorylation of a number of molecules, including the cognate receptors, JAK-family kinases (Jak1 and tyk2), and latent transcription factors (STATs 1 and 2). Tyrosine 35-43 Janus kinase 1 Homo sapiens 139-143 8647212-5 1996 Using MOLT-4 transfectants with the mutant beta chains, we found that two conserved proline residues within the box 1 region are essentially involved in association with Jak1. Proline 84-91 Janus kinase 1 Homo sapiens 170-174 8864852-6 1996 Interleukin 4, but not insulin, stimulated the tyrosine phosphorylation of JAK1 and, to a lesser extent, JAK2. Tyrosine 47-55 Janus kinase 1 Homo sapiens 75-79 8683106-10 1996 Finally, IL-2 induced tyrosine phosphorylation of JAK1 and JAK3, while IL-12 induced phosphorylation of JAK2 and TYK2 in both preactivated primary NK and NK3.3 cells. Tyrosine 22-30 Janus kinase 1 Homo sapiens 50-54 8780896-1 1996 Janus kinase (JAK) family protein tyrosine kinases are constituents of a signaling path leading to tyrosine phosphorylation and activation of signal transducer and activator of transcription (STAT) family transcription factors. Tyrosine 34-42 Janus kinase 1 Homo sapiens 14-17 8621573-3 1996 One of these signaling events involves the tyrosine phosphorylation of STATs (signal transducers and activators of transcription), a process believed to require the activation of a tyrosine kinase of the JAK family. Tyrosine 43-51 Janus kinase 1 Homo sapiens 204-207 8625884-4 1996 The JAKs, a family of intracellular kinases, and the STATs, a family of transcription factors, have both previously been shown to be tyrosine phosphorylated and activated in response to various cytokines, interferons, and growth factors in cells of non-skeletal origin. Tyrosine 133-141 Janus kinase 1 Homo sapiens 4-8 8605323-7 1996 IL-2 stimulation of the transduced cell line resulted in appropriate tyrosine phosphorylation of both Jak1 and Jak3. Tyrosine 69-77 Janus kinase 1 Homo sapiens 102-106 8550631-6 1996 In addition, Pro-267 is required for JAK-1 binding. Proline 13-16 Janus kinase 1 Homo sapiens 37-42 8657115-5 1996 IFNalpha-stimulated tyrosine phosphorylation of Jak1 and the alpha subunit of the IFN-alpha receptor were unaffected by phorbol 12-myristate 13-acetate (PMA). Tyrosine 20-28 Janus kinase 1 Homo sapiens 48-52 8608222-2 1996 G-CSF induces tyrosine phosphorylation of Jak1, Jak2, STAT1, and STAT3. Tyrosine 14-22 Janus kinase 1 Homo sapiens 42-46 8671609-4 1996 Mutational analysis revealed that one of the proline residues, particularly Pro352 and Pro355, in the membrane-proximal proline-rich sequence (Pro352-Pro353-X-Pro355) of the cytoplasmic domain of IL-5R alpha is required for cell proliferation, and for both JAK1 and JAK2 activation. Proline 45-52 Janus kinase 1 Homo sapiens 257-261 8671609-4 1996 Mutational analysis revealed that one of the proline residues, particularly Pro352 and Pro355, in the membrane-proximal proline-rich sequence (Pro352-Pro353-X-Pro355) of the cytoplasmic domain of IL-5R alpha is required for cell proliferation, and for both JAK1 and JAK2 activation. Proline 120-127 Janus kinase 1 Homo sapiens 257-261 8671609-5 1996 In addition, transfectants expressing chimeric receptors which consist of the extracellular domain of IL-5R alpha and the cytoplasmic domain of beta c responded to IL-5 for proliferation and tyrosine phosphorylation of JAK1. Tyrosine 191-199 Janus kinase 1 Homo sapiens 219-223 8671609-7 1996 These results indicate that activation of JAK1, JAK2 and STAT5 is critical to coupling IL-5-induced tyrosine phosphorylation and ultimately mitogenesis, and that Pro352 and Pro355 in the proline-rich sequence appear to play more essential roles in cell growth and in both JAK1/STAT5 and JAK2/STAT5 activation than Pro353 does. Tyrosine 100-108 Janus kinase 1 Homo sapiens 42-46 8550573-1 1996 Binding of interferon alpha (IFN alpha) to its receptor induces activation of the Tyk-2 and Jak-1 tyrosine kinases and tyrosine phosphorylation of multiple downstream signaling elements, including the Stat components of the interferon-stimulated gene factor 3 (ISGF-3). Tyrosine 98-106 Janus kinase 1 Homo sapiens 92-97 8770944-0 1996 PDGF stimulates tyrosine phosphorylation of JAK 1 protein tyrosine kinase in human mesangial cells. Tyrosine 16-24 Janus kinase 1 Homo sapiens 44-49 8770944-12 1996 Antiphosphotyrosine immunoblotting of JAK 1 immunoprecipitates from PDGF-stimulated mesangial cell lysate showed increased tyrosine phosphorylation of this tyrosine kinase. Tyrosine 11-19 Janus kinase 1 Homo sapiens 38-43 8770944-15 1996 The data also provide the first evidence that PDGF stimulates tyrosine phosphorylation of JAK 1, the cytoplasmic tyrosine kinase stimulated by many other cytokines to activate transcription via STATs. Tyrosine 62-70 Janus kinase 1 Homo sapiens 90-95 7594533-7 1995 In addition, IL-4 and IL-7 induced the rapid tyrosine phosphorylation of JAK3 and JAK1, and IL-4 activated both JAK3 and JAK1 phosphotransferase activity. Tyrosine 45-53 Janus kinase 1 Homo sapiens 82-86 8536716-6 1995 Finally, insulin appears to induce the tyrosine phosphorylation of JAK1, but does not modify the tyrosine phosphorylation state of JAK2. Tyrosine 39-47 Janus kinase 1 Homo sapiens 67-71 7591091-2 1995 The changes in gene expression brought about by gamma interferon are thought to involve transient increases in the activities of cellular protein tyrosine kinases, including the Janus kinases Jak1 and Jak2, leading to tyrosine phosphorylation of the transcription factor Stat1. Tyrosine 146-154 Janus kinase 1 Homo sapiens 192-196 7579336-1 1995 The protein tyrosine kinases JAK1 and JAK2 are phosphorylated tyrosine after the interaction of granulocyte colony-stimulating factor (G-CSF) with its transmembrane receptor. Tyrosine 12-20 Janus kinase 1 Homo sapiens 29-33 7591091-3 1995 To investigate the mechanisms accounting for the impaired responses to gamma interferon, a model system for examining overall changes in protein tyrosine phosphorylation, activation of Jak1 and Jak2 and phosphorylation of Stat1 was developed in phorbol 12-myristate 13-acetate-differentiated U-937 cells. Tetradecanoylphorbol Acetate 245-276 Janus kinase 1 Homo sapiens 185-189 7657660-3 1995 Co-expression of Stat1 with Tyk2, Jak1, or Jak2 resulted in the specific tyrosine phosphorylation of Stat1 at Tyr701, the residue phosphorylated in mammalian cells stimulated with interferon gamma. Tyrosine 73-81 Janus kinase 1 Homo sapiens 34-38 7591091-5 1995 Increased labeling of these proteins occurred to similar extents in control cells and in cells that had been infected with L. donovani for 16 h. Jak1, Jak2, and Stat1 were immunoprecipitated from control and interferon-treated cells, and tyrosine phosphorylation of these proteins, detected by antiphosphotyrosine immunoblotting was used to measured their activation. Tyrosine 238-246 Janus kinase 1 Homo sapiens 145-149 7591091-6 1995 Tyrosine phosphorylation of Jak1, Jak2, and Stat1 increased markedly, in a dose-dependent manner, in U-937 cells incubated with gamma interferon. Tyrosine 0-8 Janus kinase 1 Homo sapiens 28-32 7591091-7 1995 In contrast, in cells infected with L. donovani, tyrosine phosphorylation of Jak1, Jak2, and Stat1 was markedly impaired. Tyrosine 49-57 Janus kinase 1 Homo sapiens 77-81 7579387-4 1995 In fibroblasts, the activation of the STAT proteins is accompanied by tyrosine phosphorylation of Tyk2 and JAK1. Tyrosine 70-78 Janus kinase 1 Homo sapiens 107-111 7569929-2 1995 In murine pre-B lymphocytes transformed with A-MuLV, the Janus kinases (Jaks) Jak1 and Jak3 exhibited constitutive tyrosine kinase activity, and the STAT proteins (signal transducers and activators of transcription) normally activated by interleukin-4 and interleukin-7 were tyrosine-phosphorylated in the absence of these cytokines. Tyrosine 115-123 Janus kinase 1 Homo sapiens 72-76 7569929-2 1995 In murine pre-B lymphocytes transformed with A-MuLV, the Janus kinases (Jaks) Jak1 and Jak3 exhibited constitutive tyrosine kinase activity, and the STAT proteins (signal transducers and activators of transcription) normally activated by interleukin-4 and interleukin-7 were tyrosine-phosphorylated in the absence of these cytokines. Tyrosine 115-123 Janus kinase 1 Homo sapiens 78-82 7568001-6 1995 JAK1 and JAK3 were tyrosine-phosphorylated in response to IL-2 and IL-15. Tyrosine 19-27 Janus kinase 1 Homo sapiens 0-4 7543512-0 1995 IL-10 induces the tyrosine phosphorylation of tyk2 and Jak1 and the differential assembly of STAT1 alpha and STAT3 complexes in human T cells and monocytes. Tyrosine 18-26 Janus kinase 1 Homo sapiens 55-59 7544000-4 1995 In this report we demonstrate that both IL-4 and IL-13 induced the tyrosine phosphorylation of 4PS and JAK1. Tyrosine 67-75 Janus kinase 1 Homo sapiens 103-107 7543512-4 1995 IL-10 treatment of both T cells and monocytes results in the ligand-induced tyrosine phosphorylation of tyk2 and Jak1, but not Jak2 or Jak3. Tyrosine 76-84 Janus kinase 1 Homo sapiens 113-117 7756643-4 1995 In this report we show that IL-9 induces tyrosine phosphorylation and activation of the JAK family tyrosine kinases including JAK1, JAK3, and Tyk2. Tyrosine 41-49 Janus kinase 1 Homo sapiens 126-130 7615558-9 1995 IFN gamma clusters at least two receptor units which results in the tyrosine phosphorylation of Jak1 and Jak2, the activation of Jak2 kinase activity, and the recruitment of STAT1 alpha resulting in its activation by tyrosine phosphorylation. Tyrosine 68-76 Janus kinase 1 Homo sapiens 96-100 7615558-9 1995 IFN gamma clusters at least two receptor units which results in the tyrosine phosphorylation of Jak1 and Jak2, the activation of Jak2 kinase activity, and the recruitment of STAT1 alpha resulting in its activation by tyrosine phosphorylation. Tyrosine 217-225 Janus kinase 1 Homo sapiens 96-100 7608217-5 1995 Stimulation of the cells by these factors led to rapid phosphorylation of Jak1, but not Jak2 or Jak3, on tyrosine residues. Tyrosine 105-113 Janus kinase 1 Homo sapiens 74-78 7713924-8 1995 We also demonstrate that only mouse cells expressing the human alpha subunit are able to tyrosine-phosphorylate p135tyk2 and JAK-1 and to form the ISGF3 complex in response to human IFN alpha 8. Tyrosine 89-97 Janus kinase 1 Homo sapiens 125-130 7721895-1 1995 The tyrosine kinases JAK1 and JAK3 have been shown to undergo tyrosine phosphorylation in response to interleukin-2 (IL), IL4, IL7, and IL9, cytokines which share the common IL2 receptor gamma-chain (IL2R gamma), and evidence has been found for a preferential coupling of JAK3 to IL2R gamma and JAK1 to IL2R beta. Tyrosine 4-12 Janus kinase 1 Homo sapiens 21-25 7721895-1 1995 The tyrosine kinases JAK1 and JAK3 have been shown to undergo tyrosine phosphorylation in response to interleukin-2 (IL), IL4, IL7, and IL9, cytokines which share the common IL2 receptor gamma-chain (IL2R gamma), and evidence has been found for a preferential coupling of JAK3 to IL2R gamma and JAK1 to IL2R beta. Tyrosine 4-12 Janus kinase 1 Homo sapiens 295-299 7532278-4 1995 Binding of IFNs to their receptors triggers tyrosine phosphorylation and activation of the receptors, JAK family kinases, STAT1, and STAT2. Tyrosine 44-52 Janus kinase 1 Homo sapiens 102-105 7528775-4 1995 In this report we show that IL-12 and IL-2 induce tyrosine phosphorylation of distinct members of the Janus (JAK) family of protein tyrosine kinases in human T lymphocytes. Tyrosine 50-58 Janus kinase 1 Homo sapiens 109-112 7988557-4 1994 IFN alpha induced the tyrosine phosphorylation of JAK1 and Tyk2, but not JAK2 or JAK3. Tyrosine 22-30 Janus kinase 1 Homo sapiens 50-54 7995951-8 1995 Pretreatment with IC resulted in the inhibition of the tyrosine phosphorylation of the tyrosine kinases, Jak1 and Jak2, both of which are involved in IFN-gamma signal transduction. Tyrosine 55-63 Janus kinase 1 Homo sapiens 105-109 7973658-4 1994 IL-2, IL-4, IL-7 (whose receptors are known to contain gamma c), and IL-9 (whose receptor is shown here to contain gamma c) induced the tyrosine phosphorylation and activation of the Janus family tyrosine kinases Jak1 and Jak3. Tyrosine 136-144 Janus kinase 1 Homo sapiens 213-217 7526154-1 1994 Binding of type I interferons (IFNs) to their receptors induces rapid tyrosine phosphorylation of multiple proteins, including the alpha and beta subunits of the receptor, the polypeptides that form the transcriptional activator ISGF3 alpha (Stat113, Stat84, and Stat91), and the p135tyk2 and Jak-1 tyrosine kinases. Tyrosine 70-78 Janus kinase 1 Homo sapiens 293-298 7525556-0 1994 Differential tyrosine phosphorylation of JAK1, JAK2, and STAT1 by growth hormone and interferon-gamma in IM-9 cells. Tyrosine 13-21 Janus kinase 1 Homo sapiens 41-45 7525556-3 1994 We demonstrate that, in the human IM-9 lymphocyte, both JAK1 and JAK2 are tyrosine-phosphorylated in response to IFN gamma, whereas only JAK2 is tyrosine-phosphorylated in response to GH. Tyrosine 74-82 Janus kinase 1 Homo sapiens 56-60 7973659-2 1994 Stimulation with IL-2 induces the tyrosine phosphorylation and activation of the Janus kinases Jak1 and Jak3. Tyrosine 34-42 Janus kinase 1 Homo sapiens 95-99 7973659-3 1994 Jak1 and Jak3 were found to be selectively associated with the "serine-rich" region of IL-2R beta and the carboxyl-terminal region of IL-2R gamma, respectively. Serine 64-70 Janus kinase 1 Homo sapiens 0-4 7957877-3 1994 The results have shown that out of 4 members of JAK family tyrosine kinases (JAK1, JAK2, JAK3 and Tyk2), only JAK3 was tyrosine-phosphorylated and activated in cells of a T cell clone by stimulation with IL-7. Tyrosine 59-67 Janus kinase 1 Homo sapiens 48-51 7929391-7 1994 The overlapping and distinct protein tyrosine phosphorylation and activation of the same JAK1 kinase in T lymphocytes strongly suggests that IL-4 and IL-9 share the common signal transduction pathways and that the specificity for each cytokine could be achieved through the unique tyrosine-phosphorylated proteins triggered by individual cytokines. Tyrosine 37-45 Janus kinase 1 Homo sapiens 89-93 7929391-7 1994 The overlapping and distinct protein tyrosine phosphorylation and activation of the same JAK1 kinase in T lymphocytes strongly suggests that IL-4 and IL-9 share the common signal transduction pathways and that the specificity for each cytokine could be achieved through the unique tyrosine-phosphorylated proteins triggered by individual cytokines. Tyrosine 281-289 Janus kinase 1 Homo sapiens 89-93 7957877-3 1994 The results have shown that out of 4 members of JAK family tyrosine kinases (JAK1, JAK2, JAK3 and Tyk2), only JAK3 was tyrosine-phosphorylated and activated in cells of a T cell clone by stimulation with IL-7. Tyrosine 59-67 Janus kinase 1 Homo sapiens 77-81 7935373-6 1994 In contrast, stimulation with IL-2 or the related cytokine IL-4 resulted in the rapid, dose-dependent tyrosine phosphorylation of JAK1 and an additional 116-kDa protein. Tyrosine 102-110 Janus kinase 1 Homo sapiens 130-134 7929242-4 1994 In addition, cells from the G1/S phase exhibited increased tyrosine phosphorylation of JAK-1 and Tyk-2 kinases and p91 by IFN-alpha as compared with asynchronized cells. Tyrosine 59-67 Janus kinase 1 Homo sapiens 87-92 7929242-6 1994 These findings demonstrate that the levels of constitutive and inducible expression of IFN-alpha-inducible genes, activation of p91, and tyrosine phosphorylation of JAK-1 and Tyk-2 kinases are differentially influenced by the state of the cell cycle. Tyrosine 137-145 Janus kinase 1 Homo sapiens 165-170 8022486-3 1994 Recent studies have shown that one or more of the Janus kinase family members (Jaks) associate with cytokine receptors and are tyrosine phosphorylated and activated following ligand binding. Tyrosine 127-135 Janus kinase 1 Homo sapiens 79-83 8041779-3 1994 Tyrosine phosphorylation of JAK1 and JAK2 was induced upon IL-2 stimulation, and IL-2 activated the JAK2 kinase. Tyrosine 0-8 Janus kinase 1 Homo sapiens 28-32 8022486-4 1994 Here we describe a new Jak family kinase, Jak-3, and demonstrate that Jak-3, and to a lesser extent Jak-1, are tyrosine phosphorylated and Jak-3 is activated in the responses to interleukin-2 and interleukin-4 in T cells and myeloid cells. Tyrosine 111-119 Janus kinase 1 Homo sapiens 23-26 8022486-4 1994 Here we describe a new Jak family kinase, Jak-3, and demonstrate that Jak-3, and to a lesser extent Jak-1, are tyrosine phosphorylated and Jak-3 is activated in the responses to interleukin-2 and interleukin-4 in T cells and myeloid cells. Tyrosine 111-119 Janus kinase 1 Homo sapiens 100-105 7514165-3 1994 H2O2/vanadate treatment of cells for 15 min resulted in only the tyrosine phosphorylation of Jak1 and IFN-gamma R. Only after 60 min of this treatment did we observe tyrosine phosphorylation of Jak2 and p91 and assembly of the transcription factor complex FcRF gamma that binds to the promoter of the fcgr1 gene. Hydrogen Peroxide 0-4 Janus kinase 1 Homo sapiens 93-97 7517047-3 1994 Recent studies have shown that members of the Janus kinase (JAK) family of protein tyrosine kinases associate with the membrane proximal region, are rapidly tyrosine phosphorylated following ligand binding and their in vitro kinase activity is activated. Tyrosine 83-91 Janus kinase 1 Homo sapiens 60-63 7514165-3 1994 H2O2/vanadate treatment of cells for 15 min resulted in only the tyrosine phosphorylation of Jak1 and IFN-gamma R. Only after 60 min of this treatment did we observe tyrosine phosphorylation of Jak2 and p91 and assembly of the transcription factor complex FcRF gamma that binds to the promoter of the fcgr1 gene. Vanadates 5-13 Janus kinase 1 Homo sapiens 93-97 7514165-3 1994 H2O2/vanadate treatment of cells for 15 min resulted in only the tyrosine phosphorylation of Jak1 and IFN-gamma R. Only after 60 min of this treatment did we observe tyrosine phosphorylation of Jak2 and p91 and assembly of the transcription factor complex FcRF gamma that binds to the promoter of the fcgr1 gene. Tyrosine 65-73 Janus kinase 1 Homo sapiens 93-97 33237566-1 2020 Filgotinib (Jyseleca ) is an oral, ATP-competitive, reversible JAK1 preferential inhibitor that is being developed by Galapagos NV and Gilead Sciences for the treatment of inflammatory autoimmune diseases, including inflammatory arthritis and inflammatory bowel disease. GLPG0634 0-10 Janus kinase 1 Homo sapiens 63-67 7504784-11 1993 We find that Jak1 also becomes phosphorylated on tyrosine after cells are treated with these same three ligands, although each ligand is shown to activate at least one other different kinase. Tyrosine 49-57 Janus kinase 1 Homo sapiens 13-17 7504784-12 1993 Jak1 may therefore be the enzyme that phosphorylates Tyr 701 in Stat91. Tyrosine 53-56 Janus kinase 1 Homo sapiens 0-4 33826132-1 2021 BACKGROUND: Baricitinib, a selective Janus kinase 1/Janus kinase 2 inhibitor, is indicated in the European Union and Japan for the treatment of moderate-to-severe atopic dermatitis (AD) in adults who are candidates for systemic therapy. baricitinib 12-23 Janus kinase 1 Homo sapiens 37-51 33797200-9 2021 The mechanism of MPTP inhibition was via gp130 signalling and the downstream JAK/STAT pathway. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 17-21 Janus kinase 1 Homo sapiens 77-80 33792844-11 2021 Collectively, TFA exhibited a potential protective effect against CDDP-induced testicular injury by inhibiting oxidative stress as well as TLR4/IRF3/INF-gamma, P38-MAPK/NF-kappaB-p65/TNF-alpha, and JAK1/STAT-3/ERK1/2 inflammatory signaling pathways with enhancing its in vitro cytotoxic activity. ferulic acid 14-17 Janus kinase 1 Homo sapiens 198-202 7512720-0 1994 Tyrosine kinase JAK1 is associated with the granulocyte-colony-stimulating factor receptor and both become tyrosine-phosphorylated after receptor activation. Tyrosine 107-115 Janus kinase 1 Homo sapiens 16-20 7512720-3 1994 We detected tyrosine phosphorylation of both the G-CSF receptor and the protein tyrosine kinase JAK1 following G-CSF binding to the human G-CSF receptor. Tyrosine 12-20 Janus kinase 1 Homo sapiens 96-100 33971281-6 2021 Sustained treatment of MYB-TYK2-rearranged ALL cells with cerdulatinib led to enhanced and persistent JAK/STAT signaling, co-occurring with JAK1 overexpression. 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide 58-70 Janus kinase 1 Homo sapiens 140-144 33971281-7 2021 Hyperactivation of JAK/STAT signaling and JAK1 overexpression was reversible as cerdulatinib withdrawal resulted in re-sensitization to the drug. 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide 80-92 Janus kinase 1 Homo sapiens 42-46 33970999-6 2021 Notably, we also find that established tumors may no longer require high levels of IL-7R expression upon secondary transplantation and can progress in the absence of IL-7, but remain sensitive to inhibitors of IL-7R-mediated signaling Ruxolitinib (Jak1), AZD1208 (Pim), Dactolisib (PI3K/mTOR), Palbociclib (Cdk4/6), and Venetoclax (Bcl-2). ruxolitinib 235-246 Janus kinase 1 Homo sapiens 248-252 33970999-6 2021 Notably, we also find that established tumors may no longer require high levels of IL-7R expression upon secondary transplantation and can progress in the absence of IL-7, but remain sensitive to inhibitors of IL-7R-mediated signaling Ruxolitinib (Jak1), AZD1208 (Pim), Dactolisib (PI3K/mTOR), Palbociclib (Cdk4/6), and Venetoclax (Bcl-2). AZD1208 255-262 Janus kinase 1 Homo sapiens 248-252 33970999-6 2021 Notably, we also find that established tumors may no longer require high levels of IL-7R expression upon secondary transplantation and can progress in the absence of IL-7, but remain sensitive to inhibitors of IL-7R-mediated signaling Ruxolitinib (Jak1), AZD1208 (Pim), Dactolisib (PI3K/mTOR), Palbociclib (Cdk4/6), and Venetoclax (Bcl-2). dactolisib 270-280 Janus kinase 1 Homo sapiens 248-252 33782031-1 2021 PURPOSE: The JAK1/2 inhibitor ruxolitinib has demonstrated significant benefits for patients with Myeloproliferative Neoplasms (MPNs). ruxolitinib 30-41 Janus kinase 1 Homo sapiens 13-19 33237566-1 2020 Filgotinib (Jyseleca ) is an oral, ATP-competitive, reversible JAK1 preferential inhibitor that is being developed by Galapagos NV and Gilead Sciences for the treatment of inflammatory autoimmune diseases, including inflammatory arthritis and inflammatory bowel disease. Adenosine Triphosphate 35-38 Janus kinase 1 Homo sapiens 63-67 33237566-2 2020 The JAK-STAT signalling pathway has been implicated in the pathogenesis of inflammatory and autoimmune diseases, and filgotinib modulates this pathway by preventing the phosphorylation and activation of STATs. GLPG0634 117-127 Janus kinase 1 Homo sapiens 4-7 30384869-12 2018 The phosphorylation of JAK1/2 and STAT1 declined by GL. Glycyrrhizic Acid 52-54 Janus kinase 1 Homo sapiens 23-29 29024542-1 2018 Momelotinib is a potent and selective small-molecule inhibitor of JAK1/2 that is under investigation for the treatment of myeloproliferative neoplasms. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 66-72 34480250-6 2022 Western blot and qRT-PCR analysis suggested that treatment with methotrexate (MTx) dampened CoV-2-SRBD-mediated increase in JAK1/STAT3 phosphorylation, gp130, IL6, and folate-binding protein (FBP) expressions. Methotrexate 64-76 Janus kinase 1 Homo sapiens 124-128 25682576-1 2015 BACKGROUND: In the COMFORT (COntrolled MyeloFibrosis Study with ORal JAK Inhibitor Therapy)-I study, the Janus kinase (JAK)1/JAK2 inhibitor ruxolitinib provided significant reductions in splenomegaly, improvements in myelofibrosis (MF)-related symptoms, and a survival advantage relative to placebo in patients with intermediate-2 or high-risk MF. ruxolitinib 140-151 Janus kinase 1 Homo sapiens 105-124 34740884-1 2022 OBJECTIVE: To characterise safety of the Janus kinase-1 preferential inhibitor filgotinib in patients with moderately to severely active rheumatoid arthritis. GLPG0634 79-89 Janus kinase 1 Homo sapiens 41-55 29224367-2 2018 Ruxolitinib, a potent Janus kinase 1 (JAK1)/JAK2 inhibitor, led to substantial improvements in splenomegaly, MF-associated symptoms, and QoL in the phase 3 COMFORT studies, proving superior to placebo and best available therapy. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 22-36 29224367-2 2018 Ruxolitinib, a potent Janus kinase 1 (JAK1)/JAK2 inhibitor, led to substantial improvements in splenomegaly, MF-associated symptoms, and QoL in the phase 3 COMFORT studies, proving superior to placebo and best available therapy. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-42 26380150-3 2015 Ruxolitinib, a potent inhibitor of Janus kinase (JAK) 1 and JAK2, was associated with an overall survival benefit and improvements in splenomegaly and patient-reported outcomes in patients with myelofibrosis in the two phase 3 COMFORT studies. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 35-55 34480250-6 2022 Western blot and qRT-PCR analysis suggested that treatment with methotrexate (MTx) dampened CoV-2-SRBD-mediated increase in JAK1/STAT3 phosphorylation, gp130, IL6, and folate-binding protein (FBP) expressions. Methotrexate 78-81 Janus kinase 1 Homo sapiens 124-128 34694880-2 2022 The Janus kinase (JAK1/2) inhibitor ruxolitinib could potentially disrupt the parasite-induced dysfunctional immune response when administered with anti-malarial therapy. ruxolitinib 36-47 Janus kinase 1 Homo sapiens 18-24 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Histidine 302-305 Janus kinase 1 Homo sapiens 118-122 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Histidine 302-305 Janus kinase 1 Homo sapiens 209-213 34774741-0 2022 Synthesis and Structure-activity Relationship Studies of 1,5-Isomers of Triazole-pyrrolopyrimidine as Selective Janus Kinase 1 (JAK1) Inhibitors. triazole-pyrrolopyrimidine 72-98 Janus kinase 1 Homo sapiens 112-126 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Histidine 302-305 Janus kinase 1 Homo sapiens 313-318 34774741-0 2022 Synthesis and Structure-activity Relationship Studies of 1,5-Isomers of Triazole-pyrrolopyrimidine as Selective Janus Kinase 1 (JAK1) Inhibitors. triazole-pyrrolopyrimidine 72-98 Janus kinase 1 Homo sapiens 128-132 34074166-2 2022 Ruxolitinib, an oral selective JAK1/2 inhibitor, has recently shown efficacy and safety in the treatment of secondary HLH, which may be an alternative to intensive chemotherapy. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 31-37 34774741-4 2022 In this study, novel 4-(1,5- or 2,5-triazole)-pyrrolopyrimidine derivatives with aromatic moieties were synthesized as JAK1 inhibitors, and an in vitro enzyme assay was used to evaluate the JAK inhibitory effects. 4-(1,5- or 2,5-triazole)-pyrrolopyrimidine 21-63 Janus kinase 1 Homo sapiens 119-123 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Iodine 270-276 Janus kinase 1 Homo sapiens 12-16 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Iodine 270-276 Janus kinase 1 Homo sapiens 118-122 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Iodine 270-276 Janus kinase 1 Homo sapiens 209-213 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Iodine 270-276 Janus kinase 1 Homo sapiens 313-318 34774741-5 2022 Among these JAK1 inhibitors, the compound 23a showed an IC50 level of 72 nM, as well as being selective against other JAKs by 12 times or more: the results of molecular docking studies suggested that the high JAK1 selectivity resulted from a key interaction between the iodine atom of compound 23a and His-885 of hJAK1. Histidine 302-305 Janus kinase 1 Homo sapiens 12-16 34846636-1 2022 INTRODUCTION: Baricitinib, an oral Janus kinase (JAK)1/JAK2 inhibitor, is indicated in the European Union and Japan for treatment of moderate-to-severe atopic dermatitis (AD) in adults who are candidates for systemic therapy. baricitinib 14-25 Janus kinase 1 Homo sapiens 35-54 34871917-0 2022 Quantification of the janus kinase 1 inhibitor upadacitinib in human plasma by LC-MS/MS. upadacitinib 47-59 Janus kinase 1 Homo sapiens 22-36 34871917-1 2022 Upadacitinib is a selective janus-kinase-1 inhibitor effective in the treatment of autoimmune related diseases like rheumatoid arthritis or psoriatic arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 34807428-1 2021 Abrocitinib (Cibinqo ) is an oral small-molecule inhibitor of Janus kinase 1 (JAK1) being developed by Pfizer for the treatment of moderate-to-severe atopic dermatitis (AD). Abrocitinib 13-20 Janus kinase 1 Homo sapiens 62-76 34627950-5 2021 JAK1 inhibitor, Itacitinib adipate, dramatically inhibited high Rab1A NSCLC metastasis, in both cell line and patient derived xenograft models. Itacitinib adipate 16-34 Janus kinase 1 Homo sapiens 0-4 34911805-2 2022 Subsequently, the use of the Janus kinase ( JAK) 1/2 inhibitor baricitinib resulted in considerable improvement in the patient"s symptoms and skin appearance. baricitinib 63-74 Janus kinase 1 Homo sapiens 29-52 34521299-0 2022 Adherence to ruxolitinib, an oral JAK1/2 inhibitor, in patients with myelofibrosis: interim analysis from an Italian, prospective cohort study (ROMEI). ruxolitinib 13-24 Janus kinase 1 Homo sapiens 34-40 34521299-1 2022 ROMEI, a prospective, observational study in patients with myelofibrosis receiving the oral JAK1/2 inhibitor ruxolitinib in real-world practice, assesses treatment adherence based on the 8-item Morisky Medication Adherence Scale (MMAS-8). ruxolitinib 109-120 Janus kinase 1 Homo sapiens 92-98 34592416-5 2021 The PMA-treated S1P2knockout THP-1 Mphis showed decreases in IL-4/IL-13-induced phosphorylation of Janus-activated kinase (JAK) 1, JAK2, and STAT6 as well as mRNA expression of the M2 marker ARG1 compared with wild-type THP-1 Mphis. Tetradecanoylphorbol Acetate 4-7 Janus kinase 1 Homo sapiens 99-129 34807428-1 2021 Abrocitinib (Cibinqo ) is an oral small-molecule inhibitor of Janus kinase 1 (JAK1) being developed by Pfizer for the treatment of moderate-to-severe atopic dermatitis (AD). Abrocitinib 13-20 Janus kinase 1 Homo sapiens 78-82 34894197-0 2021 Besserung eines oralen und osophagealen Lichen ruber mucosae unter dem JAK1-Inhibitor Upadacitinib. upadacitinib 86-98 Janus kinase 1 Homo sapiens 71-75 34169526-1 2021 Ruxolitinib is an FDA-approved orally administered Janus kinase (JAK 1/2) inhibitor that reduces cytokine-induced inflammation. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 65-72 34402699-3 2021 The number of JAKi has been growing and to date, filgotinib is the latest JAKi to be approved for use in RA.Areas coveredThis review focuses on the pharmacodynamics, pharmacokinetics, efficacy and safety of filgotinib in patients with RA.Expert opinionFilgotinib is an oral targeted synthetic disease-modifying antirheumatic drug (DMARD) that specifically inhibits JAK1. GLPG0634 49-59 Janus kinase 1 Homo sapiens 365-369 34402699-3 2021 The number of JAKi has been growing and to date, filgotinib is the latest JAKi to be approved for use in RA.Areas coveredThis review focuses on the pharmacodynamics, pharmacokinetics, efficacy and safety of filgotinib in patients with RA.Expert opinionFilgotinib is an oral targeted synthetic disease-modifying antirheumatic drug (DMARD) that specifically inhibits JAK1. GLPG0634 207-217 Janus kinase 1 Homo sapiens 365-369 34402699-3 2021 The number of JAKi has been growing and to date, filgotinib is the latest JAKi to be approved for use in RA.Areas coveredThis review focuses on the pharmacodynamics, pharmacokinetics, efficacy and safety of filgotinib in patients with RA.Expert opinionFilgotinib is an oral targeted synthetic disease-modifying antirheumatic drug (DMARD) that specifically inhibits JAK1. opinionfilgotinib 245-262 Janus kinase 1 Homo sapiens 365-369 34645316-1 2021 Upadacitinib, a selective JAK 1 inhibitor, has been evaluated for efficacy and safety in the treatment of psoriatic arthritis (PsA). upadacitinib 0-12 Janus kinase 1 Homo sapiens 26-31 34761860-0 2021 Alleviation of erosive oral and esophageal lichen planus by the JAK1 inhibitor upadacitinib. upadacitinib 79-91 Janus kinase 1 Homo sapiens 64-68 34626199-3 2021 Dysregulation of JAK/STAT pathways and JAK2 copy number gains were observed in the four paclitaxel-resistant PDX tumors. Paclitaxel 88-98 Janus kinase 1 Homo sapiens 17-20 34626199-5 2021 However, JAK1/2 inhibitor treatment resulted in restoration of paclitaxel sensitivity in two out of four paclitaxel-resistant PDX models and JAK1/2 inhibitor alone significantly suppressed the tumor growth in one out of the two remaining PDX models. Paclitaxel 63-73 Janus kinase 1 Homo sapiens 9-15 34880598-3 2021 Ruxolitinib is a selective Janus kinases 1/2 inhibitor which has been shown to control acute (a) and chronic (c) GVHD while maintaining graft-versus-tumor effects. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 27-44 34097102-1 2021 A patient with rheumatoid arthritis (RA) was presented, who developed an infection with the hepatitis E virus (HEV) under treatment with the Janus kinase (JAK) 1 and 2 inhibitor baricitinib. baricitinib 178-189 Janus kinase 1 Homo sapiens 141-167 34946023-7 2021 Our results showed that insulin-mediated reduction of UPEC infection in a high-glucose environment was not only due to the downregulation of JAK1/2 and phosphorylated STAT-1/3, but also because of the decreased expression of TLR-4 proteins and pro-inflammatory IL-6. Glucose 79-86 Janus kinase 1 Homo sapiens 141-147 34873553-1 2021 Introduction Baricitinib is an oral synthetic Janus Kinase inhibitor that inhibits JAK1 and JAK2, and the new kid on the block in the treatment of rheumatoid arthritis (RA). baricitinib 13-24 Janus kinase 1 Homo sapiens 83-87 34845259-0 2021 Computer aided designing of novel pyrrolopyridine derivatives as JAK1 inhibitors. 4-azaindole 34-49 Janus kinase 1 Homo sapiens 65-69 34845259-4 2021 Although JAK1 inhibitors such as Tofacitinib have been approved for medical use, the low potency and off-target effects of these inhibitors have limited their use and calls for the development of novel JAK1 inhibitors. tofacitinib 33-44 Janus kinase 1 Homo sapiens 9-13 34845259-5 2021 In this study, we used computational methods on a series of pyrrolopyridine derivatives to design new JAK1 inhibitors. 4-azaindole 60-75 Janus kinase 1 Homo sapiens 102-106 34845259-9 2021 Of the designed compounds, seventeen of the compounds showed a higher binding energy value than the most active compound in the dataset and at least six of the compounds showed higher binding energy value than the pan JAK inhibitor Tofacitinib. tofacitinib 232-243 Janus kinase 1 Homo sapiens 218-221 34828623-2 2021 Objectives: To evaluate the efficacy and safety of baricitinib, the first JAK 1 and 2 inhibitor approved in Europe for the treatment of adult patients with moderate-to-severe AD. baricitinib 51-62 Janus kinase 1 Homo sapiens 74-85 34867980-4 2021 Several JAK inhibitors have entered clinical trials, including ruxolitinib, the first JAK1/2 inhibitor to become commercially available for the treatment of myelofibrosis and polycythemia vera. ruxolitinib 63-74 Janus kinase 1 Homo sapiens 86-92 34741776-7 2022 JAK1/2 and STAT1 inhibitors could reverse the reduction of SLC7A11, GPx4 and GSH expression induced by IFN-gamma, indicating IFN-gamma induces ARPE-19 cell ferroptosis via activation of the JAK1-2/STAT1/SLC7A11 signaling pathway. Glutathione 77-80 Janus kinase 1 Homo sapiens 0-6 34767869-3 2021 OBJECTIVE: Investigate changes in IL-23/Th17- and type I interferon-pathway biomarkers and gene responses, and measures of selectivity for TYK2 over Janus kinases (JAKs) 1-3, in patients with moderate to severe psoriasis receiving deucravacitinib. Deucravacitinib 231-246 Janus kinase 1 Homo sapiens 164-168 34741617-0 2021 Effects of JAK1-Preferential Inhibitor Filgotinib on Circulating Biomarkers and Whole Blood Genes/Pathways of Patients With Moderately to Severely Active Crohn"s Disease. GLPG0634 39-49 Janus kinase 1 Homo sapiens 11-15 34741617-2 2021 We profiled circulating biomarkers and whole blood transcriptional pathway activity to identify those associated with CD using data from the phase 2 FITZROY study with filgotinib, an oral preferential janus kinase-1 inhibitor. GLPG0634 168-178 Janus kinase 1 Homo sapiens 201-215 34741776-7 2022 JAK1/2 and STAT1 inhibitors could reverse the reduction of SLC7A11, GPx4 and GSH expression induced by IFN-gamma, indicating IFN-gamma induces ARPE-19 cell ferroptosis via activation of the JAK1-2/STAT1/SLC7A11 signaling pathway. Glutathione 77-80 Janus kinase 1 Homo sapiens 190-196 34826840-6 2021 Treatment with Baricitinib - a JAK 1/2 inhibitor - may also be beneficial for patients without or on low oxygen supplementation. baricitinib 15-26 Janus kinase 1 Homo sapiens 31-38 34769307-8 2021 Our results suggest that JAK1 inhibition can ameliorate BRB dysfunction in T2D, and JAK1 inhibitors such as tofacitinib citrate may be re-purposed for the management of diabetic macular oedema. tofacitinib 108-127 Janus kinase 1 Homo sapiens 84-88 34374027-2 2021 SHR0302 is an oral, highly selective, Janus kinase 1 inhibitor under investigation for inflammatory skin diseases. ivarmacitinib 0-7 Janus kinase 1 Homo sapiens 38-52 34435525-0 2021 MiR-146b-5p targets IFI35 to inhibit inflammatory response and apoptosis via JAK1/STAT1 signalling in lipopolysaccharide-induced glomerular cells. mir-146b-5p 0-11 Janus kinase 1 Homo sapiens 77-81 34435525-12 2021 Meanwhile, miR-146b-5p targeted IFI35 to suppress inflammatory response and cell inflammatory response and apoptosis via inactivating the JAK1/STAT1 pathway. mir-146b-5p 11-22 Janus kinase 1 Homo sapiens 138-142 34435525-13 2021 MiR-146b-5p suppressed inflammatory response and cell apoptosis by IFI35 mediated-JAK1/STAT1 signalling in HK-2 cells, which provided a new mechanism for understanding the pathogenesis of LN. mir-146b-5p 0-11 Janus kinase 1 Homo sapiens 82-86 34844720-0 2021 The anti-neoplastic activities of aloperine in HeLa cervical cancer cells are associated with inhibition of the IL-6-JAK1-STAT3 feedback loop. aloperine 34-43 Janus kinase 1 Homo sapiens 117-121 34844720-12 2021 For molecular mechanisms, the expression and activation of the IL-6-JAK1-STAT3 feedback loop were markedly suppressed by ALO treatment. aloperine 121-124 Janus kinase 1 Homo sapiens 68-72 34665696-1 2021 OBJECTIVES: To investigate the ex vivo effect of the JAK1/2 inhibitor baricitinib on expression of pro-inflammatory mediators in rheumatoid arthritis (RA) fibroblast like synoviocytes (FLS) stimulated with TNFalpha, IL-1beta and oncostatin M (OSM), and in RA synovial membrane cells (SMCs). baricitinib 70-81 Janus kinase 1 Homo sapiens 53-59 34514729-6 2021 Crocetin suppressed the activity of upstream kinases such as Src, JAK1, and JAK2. crocetin 0-8 Janus kinase 1 Homo sapiens 66-70 34655610-5 2022 The JAK1/2 inhibitor ruxolitinib strongly inhibited such effects on epidermal cells. ruxolitinib 21-32 Janus kinase 1 Homo sapiens 4-10 34520107-4 2021 Ruxolitinib is a JAK-1/JAK-2 inhibitor and has showed its efficacy in suppressing IE and the immune system. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 17-22 34771643-4 2021 Tris DBA decreased cell viability, increased apoptosis, and inhibited IL-6 induced/constitutive activation of STAT3, JAK1, JAK2, and Src in HCC and MM cells. Tromethamine 0-4 Janus kinase 1 Homo sapiens 117-121 34745769-6 2021 Mechanistically, metformin induced activation of the JAK1/2/3/STAT5 and AKT/mTOR pathways in a p38 MAPK-dependent manner rather than an AMPK-dependent manner. Metformin 17-26 Janus kinase 1 Homo sapiens 53-61 34642693-9 2021 Treatment of SARS-CoV-2 infected RMs with baricitinib (Olumiant ), a novel JAK1/2 inhibitor that recently received Emergency Use Authorization for the treatment of hospitalized COVID-19 patients, was remarkably effective in eliminating the influx of infiltrating, non-alveolar macrophages in the alveolar space, with a concomitant reduction of inflammatory cytokines. baricitinib 42-53 Janus kinase 1 Homo sapiens 77-83 34721386-12 2021 In particular, we identified filgotinub and fedratinib, targeting gene JAK1, as potential drugs for AD. Fedratinib 44-54 Janus kinase 1 Homo sapiens 71-75 34627340-5 2021 Baricitinib, an oral selective Janus kinase (JAK)1 and 2 inhibitor, may impact key cytokines implicated in the pathogenesis of JIA-uveitis or ANA-positive uveitis, representing a potential novel treatment option for disease management. baricitinib 0-11 Janus kinase 1 Homo sapiens 31-56 34642693-9 2021 Treatment of SARS-CoV-2 infected RMs with baricitinib (Olumiant ), a novel JAK1/2 inhibitor that recently received Emergency Use Authorization for the treatment of hospitalized COVID-19 patients, was remarkably effective in eliminating the influx of infiltrating, non-alveolar macrophages in the alveolar space, with a concomitant reduction of inflammatory cytokines. baricitinib 55-63 Janus kinase 1 Homo sapiens 77-83 34629864-1 2021 Background: Upadacitinib, a novel selective Janus kinase 1 (JAK1) inhibitor, has been recently approved by the US FDA for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA). upadacitinib 12-24 Janus kinase 1 Homo sapiens 44-58 34629864-1 2021 Background: Upadacitinib, a novel selective Janus kinase 1 (JAK1) inhibitor, has been recently approved by the US FDA for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA). upadacitinib 12-24 Janus kinase 1 Homo sapiens 60-64 34272171-1 2021 Over the last decade, the Janus kinase (JAK) 1/2 inhibitor ruxolitinib has become widely established as the cornerstone of pharmacologic therapy for most patients with myelofibrosis (MF), providing dramatic and durable benefits in terms of splenomegaly and symptoms, and prolonging survival. ruxolitinib 59-70 Janus kinase 1 Homo sapiens 26-48 34659493-4 2021 Upadacitinib, a JAK 1 selective molecule developed in this context has been evaluated in the SELECT phase-III study program and demonstrated a high and rapid efficacy in monotherapy as well as in combination with csDMARDs both in csDMARD-naive RA patients and in patients refractory to csDMARD and bDMARD treatments. upadacitinib 0-12 Janus kinase 1 Homo sapiens 16-21 34471993-6 2021 Concentrations providing half-maximal inhibition (IC50) in these assays were determined for deucravacitinib and the JAK 1/2/3 inhibitors tofacitinib, upadacitinib, and baricitinib. tofacitinib 137-148 Janus kinase 1 Homo sapiens 116-125 34471993-6 2021 Concentrations providing half-maximal inhibition (IC50) in these assays were determined for deucravacitinib and the JAK 1/2/3 inhibitors tofacitinib, upadacitinib, and baricitinib. upadacitinib 150-162 Janus kinase 1 Homo sapiens 116-125 34471993-6 2021 Concentrations providing half-maximal inhibition (IC50) in these assays were determined for deucravacitinib and the JAK 1/2/3 inhibitors tofacitinib, upadacitinib, and baricitinib. baricitinib 168-179 Janus kinase 1 Homo sapiens 116-125 34471993-11 2021 Simulations indicated that tofacitinib, upadacitinib, and baricitinib at steady state exhibited varying degrees of JAK 1/3 (daily average inhibition, 70-94%) and JAK 2/2 (23%-67%) inhibition at therapeutic concentrations, with Cmax values 17- to 33-fold lower than their TYK2 IC50 levels. tofacitinib 27-38 Janus kinase 1 Homo sapiens 115-122 34471993-11 2021 Simulations indicated that tofacitinib, upadacitinib, and baricitinib at steady state exhibited varying degrees of JAK 1/3 (daily average inhibition, 70-94%) and JAK 2/2 (23%-67%) inhibition at therapeutic concentrations, with Cmax values 17- to 33-fold lower than their TYK2 IC50 levels. upadacitinib 40-52 Janus kinase 1 Homo sapiens 115-122 34471993-11 2021 Simulations indicated that tofacitinib, upadacitinib, and baricitinib at steady state exhibited varying degrees of JAK 1/3 (daily average inhibition, 70-94%) and JAK 2/2 (23%-67%) inhibition at therapeutic concentrations, with Cmax values 17- to 33-fold lower than their TYK2 IC50 levels. baricitinib 58-69 Janus kinase 1 Homo sapiens 115-122 34471993-13 2021 Tofacitinib, upadacitinib, and baricitinib variably inhibit JAK 1/2/3 but not TYK2. tofacitinib 0-11 Janus kinase 1 Homo sapiens 60-69 34471993-13 2021 Tofacitinib, upadacitinib, and baricitinib variably inhibit JAK 1/2/3 but not TYK2. upadacitinib 13-25 Janus kinase 1 Homo sapiens 60-69 34471993-13 2021 Tofacitinib, upadacitinib, and baricitinib variably inhibit JAK 1/2/3 but not TYK2. baricitinib 31-42 Janus kinase 1 Homo sapiens 60-69 34499329-5 2021 RECENT FINDINGS: Momelotonib is a JAK1/2 and ACVR1 inhibitor that has demonstrated not only improvements in splenomegaly and symptoms, but also amelioration of anemia on the SIMPLIFY 1 and 2 clinical trial program. momelotonib 17-28 Janus kinase 1 Homo sapiens 34-40 34157510-3 2021 Ruxolitinib, a JAK1/2 inhibitor, has recently been approved for the treatment of acute GvHD. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 34165774-1 2021 Ruxolitinib (RUX), a JAK1/2-inhibitor, is effective for myeloproliferative neoplasm (MPN) with both JAK2V617 F and calreticulin (CALR) mutations. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 21-25 34165774-1 2021 Ruxolitinib (RUX), a JAK1/2-inhibitor, is effective for myeloproliferative neoplasm (MPN) with both JAK2V617 F and calreticulin (CALR) mutations. ruxolitinib 13-16 Janus kinase 1 Homo sapiens 21-25 34536415-10 2022 Moreover, an overview of the clinical course of the disease, including therapies, provides evidence for the therapeutic efficacy of the Janus kinase (JAK) 1/2 inhibitor ruxolitinib in inflammatory lung disease. ruxolitinib 169-180 Janus kinase 1 Homo sapiens 136-158 34630428-6 2021 We investigated the impact of short-term treatment of BCL2 (venetoclax) or JAK1/2 (ruxolitinib) inhibition on recipient natural killer and T cell immunity and the subsequent effect on donor engraftment. ruxolitinib 83-94 Janus kinase 1 Homo sapiens 75-81 34660145-3 2021 Tofacitinib is an effective JAK1 and JAK3 inhibitor that can block several cytokines such as IL-2, IL-7, and IL-6. tofacitinib 0-11 Janus kinase 1 Homo sapiens 28-32 34498807-1 2022 Filgotinib, a preferential Janus Kinase-1 inhibitor, is approved in Europe and Japan for treatment of rheumatoid arthritis and is being developed for treatment of other chronic inflammatory diseases. GLPG0634 0-10 Janus kinase 1 Homo sapiens 27-41 34660133-3 2021 We present a 78-year-old female with a known diagnosis of primary myelofibrosis (PMF), on ruxolitinib, a Janus kinase (JAK) 1 and 2 inhibitor, presenting with altered mental status. ruxolitinib 90-101 Janus kinase 1 Homo sapiens 105-131 34498056-1 2021 OBJECTIVES: To explore the safety and efficacy of filgotinib (FIL), a Janus kinase 1 inhibitor, and lanraplenib (LANRA), a spleen kinase inhibitor in cutaneous lupus erythematosus (CLE). GLPG0634 50-60 Janus kinase 1 Homo sapiens 70-84 34498056-1 2021 OBJECTIVES: To explore the safety and efficacy of filgotinib (FIL), a Janus kinase 1 inhibitor, and lanraplenib (LANRA), a spleen kinase inhibitor in cutaneous lupus erythematosus (CLE). GLPG0634 62-65 Janus kinase 1 Homo sapiens 70-84 34552486-3 2021 The JAK1/2 inhibitor, ruxolitinib, is now considered a novel therapy in inflammatory disease, and hypercytokinemia is an important feature of CAEBV. ruxolitinib 22-33 Janus kinase 1 Homo sapiens 4-10 34322995-0 2021 Inhibition of Janus Kinase 1 synergizes docetaxel sensitivity in prostate cancer cells. Docetaxel 40-49 Janus kinase 1 Homo sapiens 14-28 34552976-7 2021 Furthermore, in favipiravir-treated cells, the expression of JAK1 and STAT1 was downregulated, whereas that of p-STAT1 was significantly upregulated. favipiravir 16-27 Janus kinase 1 Homo sapiens 61-65 34586102-4 2021 Filgotinib, a selective JAK1 inhibitor, has been approved by the European Medicines Agency (EMA) for treatment of RA. GLPG0634 0-10 Janus kinase 1 Homo sapiens 24-28 34623777-3 2021 Ruxolitinib, a JAK-1 and JAK-2 inhibitor, is documented to have potent anti-inflammatory activity by targeting several cytokines and growth factors with proposed efficacy in the cytokine storm observed in severe COVID-19 patients; therefore, this study examines the efficacy and tolerability of ruxolitinib for adult COVID-19 patients. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-20 34322995-8 2021 Furthermore, inhibition of JAK1/2 by baricitinib and ruxolitinib synergizes docetaxel sensitivity in both androgen receptor (AR)-negative DU145 and PC3 cells, but not in the AR-positive LNCaP cells. baricitinib 37-48 Janus kinase 1 Homo sapiens 27-33 34322995-7 2021 We demonstrated that depletion of endogenous JAK1 enhanced docetaxel-induced apoptosis in PCa cells. Docetaxel 59-68 Janus kinase 1 Homo sapiens 45-49 34322995-8 2021 Furthermore, inhibition of JAK1/2 by baricitinib and ruxolitinib synergizes docetaxel sensitivity in both androgen receptor (AR)-negative DU145 and PC3 cells, but not in the AR-positive LNCaP cells. ruxolitinib 53-64 Janus kinase 1 Homo sapiens 27-33 34171557-3 2021 Herein, we identified that interferon-gamma (IFN-gamma), one of the most important cytokines in the immune and inflammatory response, up-regulated CD47 expression in cancer cells and this effect could be inhibited by the JAK1/2 inhibitor ruxolitinib, as well as siRNA-mediated silencing of JAK1, STAT1, and IRF1. ruxolitinib 238-249 Janus kinase 1 Homo sapiens 221-227 34322995-8 2021 Furthermore, inhibition of JAK1/2 by baricitinib and ruxolitinib synergizes docetaxel sensitivity in both androgen receptor (AR)-negative DU145 and PC3 cells, but not in the AR-positive LNCaP cells. Docetaxel 76-85 Janus kinase 1 Homo sapiens 27-33 34324169-0 2021 Selective Inhibition of JAK1 Primes STAT5-Driven Human Leukemia Cells for ATRA-Induced Differentiation. Tretinoin 74-78 Janus kinase 1 Homo sapiens 24-28 34324169-3 2021 Dysregulated JAK/STAT signaling is known to drive several hematologic malignancies, and targeting JAK1 and JAK2 with the JAK1/JAK2 inhibitor ruxolitinib has led to improvement in survival in primary myelofibrosis and alleviation of vasomotor symptoms and splenomegaly in polycythemia vera and myelofibrosis. ruxolitinib 141-152 Janus kinase 1 Homo sapiens 13-16 34324169-3 2021 Dysregulated JAK/STAT signaling is known to drive several hematologic malignancies, and targeting JAK1 and JAK2 with the JAK1/JAK2 inhibitor ruxolitinib has led to improvement in survival in primary myelofibrosis and alleviation of vasomotor symptoms and splenomegaly in polycythemia vera and myelofibrosis. ruxolitinib 141-152 Janus kinase 1 Homo sapiens 98-102 34226674-5 2021 Restoring CD25 expression using the JAK1/3-inhibitor tofacitinib controlled TCR-induced IFNgamma secretion in vitro. tofacitinib 53-64 Janus kinase 1 Homo sapiens 36-42 34324169-3 2021 Dysregulated JAK/STAT signaling is known to drive several hematologic malignancies, and targeting JAK1 and JAK2 with the JAK1/JAK2 inhibitor ruxolitinib has led to improvement in survival in primary myelofibrosis and alleviation of vasomotor symptoms and splenomegaly in polycythemia vera and myelofibrosis. ruxolitinib 141-152 Janus kinase 1 Homo sapiens 121-125 34324169-5 2021 The objective of this study is to employ JAK1 inhibition (JAK1i) in the presence of ATRA as a potential therapy in non-M3 acute myeloid leukemia (AML). Tretinoin 84-88 Janus kinase 1 Homo sapiens 41-45 34531866-8 2021 In vitro treatment of HIV-infected CD4+ T cells with physiological concentrations of JAK1/2 inhibitors, ruxolitinib and baricitinib, used in clinical settings to target inflammation, reduced latent and productive infection events when added 24 hr after infection and blocked HIV reactivation from latent cells. ruxolitinib 104-115 Janus kinase 1 Homo sapiens 85-91 34531866-8 2021 In vitro treatment of HIV-infected CD4+ T cells with physiological concentrations of JAK1/2 inhibitors, ruxolitinib and baricitinib, used in clinical settings to target inflammation, reduced latent and productive infection events when added 24 hr after infection and blocked HIV reactivation from latent cells. baricitinib 120-131 Janus kinase 1 Homo sapiens 85-91 34514265-4 2021 In this work, GraphGMVAE was validated by rapidly hopping the scaffold from FDA-approved upadacitinib, which is an inhibitor of human Janus kinase 1 (JAK1), to generate more potent molecules with novel chemical scaffolds. graphgmvae 14-24 Janus kinase 1 Homo sapiens 134-148 34532638-4 2021 The JAK1/2 selective JAK inhibitor baricitinib was the first substance from this class of drugs approved by the EMA for the systemic oral treatment of AD. baricitinib 35-46 Janus kinase 1 Homo sapiens 4-10 34532638-5 2021 The clinical development program of the JAK1 selective inhibitors upadacitinib and abrocitinib is finalized with positive results for AD. upadacitinib 66-78 Janus kinase 1 Homo sapiens 40-44 34514265-4 2021 In this work, GraphGMVAE was validated by rapidly hopping the scaffold from FDA-approved upadacitinib, which is an inhibitor of human Janus kinase 1 (JAK1), to generate more potent molecules with novel chemical scaffolds. graphgmvae 14-24 Janus kinase 1 Homo sapiens 150-154 34514265-4 2021 In this work, GraphGMVAE was validated by rapidly hopping the scaffold from FDA-approved upadacitinib, which is an inhibitor of human Janus kinase 1 (JAK1), to generate more potent molecules with novel chemical scaffolds. upadacitinib 89-101 Janus kinase 1 Homo sapiens 134-148 34514265-4 2021 In this work, GraphGMVAE was validated by rapidly hopping the scaffold from FDA-approved upadacitinib, which is an inhibitor of human Janus kinase 1 (JAK1), to generate more potent molecules with novel chemical scaffolds. upadacitinib 89-101 Janus kinase 1 Homo sapiens 150-154 34514265-6 2021 The most potent molecule has 5.0 nM activity against JAK1 kinase, which shows that the GraphGMVAE model can design molecules like how a human expert does but with high efficiency and accuracy. graphgmvae 87-97 Janus kinase 1 Homo sapiens 53-57 34379541-5 2021 Baricitinib shows high selectivity for JAK1 and JAK2, making it appealing for the treatment of this condition. baricitinib 0-11 Janus kinase 1 Homo sapiens 39-43 34169393-2 2021 Ruxolitinib is an FDA approved inhibitor of JAK1 and JAK2. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 44-48 34423448-2 2022 Ruxolitinib, a selective inhibitor of JAK 1 and 2, significantly reduces constitutional symptoms and spleen size compared with placebo, and has significant clinical benefits in patients with myelofibrosis. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-49 34910188-1 2022 OBJECTIVES: Evaluate the efficacy and safety of the Janus kinase-1 inhibitor filgotinib in Japanese patients with rheumatoid arthritis (RA) and inadequate response to methotrexate (MTX). GLPG0634 77-87 Janus kinase 1 Homo sapiens 52-66 34445192-3 2021 Here, we present our work to repurpose a Janus kinase 1 inhibitor, ruxolitinib as a DCLK1 inhibitor, showing micromolar binding affinity and inhibitory activity. ruxolitinib 67-78 Janus kinase 1 Homo sapiens 41-55 34352069-1 2022 OBJECTIVE: To assess the effect of filgotinib, which preferentially inhibits Janus kinase 1 (JAK1), on magnetic resonance imaging (MRI) measures of structural change in the sacroiliac (SI) joint in patients with active ankylosing spondylitis (AS) in the TORTUGA trial. GLPG0634 35-45 Janus kinase 1 Homo sapiens 77-91 34352069-1 2022 OBJECTIVE: To assess the effect of filgotinib, which preferentially inhibits Janus kinase 1 (JAK1), on magnetic resonance imaging (MRI) measures of structural change in the sacroiliac (SI) joint in patients with active ankylosing spondylitis (AS) in the TORTUGA trial. GLPG0634 35-45 Janus kinase 1 Homo sapiens 93-97 34352069-10 2022 CONCLUSION: The significant changes in MRI structural lesions induced by filgotinib in the SI joint by week 12 demonstrate that tissue repair can be observed very soon after starting treatment with a JAK1 preferential inhibitor. GLPG0634 73-83 Janus kinase 1 Homo sapiens 200-204 34184542-2 2021 Material & methods: We tested ruxolitinib (a selective JAK1/2 inhibitor) efficacy in three different preclinical models of GvHD. ruxolitinib 30-41 Janus kinase 1 Homo sapiens 55-61 34391330-9 2021 We present a patient treated with tofacitinib, 5mg twice daily, an oral JAK1/3 inhibitor, who demonstrated clinical improvement of DH and control of new lesion development. tofacitinib 34-45 Janus kinase 1 Homo sapiens 72-78 34397713-1 2021 ABSTRACT: Baricitinib is a Janus kinase (JAK) inhibitor that selectively blocks against JAK1 and JAK2 signaling. baricitinib 10-21 Janus kinase 1 Homo sapiens 88-92 34314383-0 2021 Curcumol may alleviate psoriasis-like inflammation by inhibiting keratinocyte proliferation and inflammatory gene expression via JAK1/STAT3 signaling. curcumol 0-8 Janus kinase 1 Homo sapiens 129-133 34314383-5 2021 Curcumol inhibits activity of JAK1, resulting in the inhibition of STAT3, downregulation of cyclin D2, and cell cycle arrest in stimulated NHEK cells. curcumol 0-8 Janus kinase 1 Homo sapiens 30-34 34314383-6 2021 Together, our data show that curcumol reduces proliferation and inflammatory gene expression in stimulated keratinocytes by inhibiting the JAK1/STAT3 signaling, suggesting that it might serve as a potential therapeutic option for the treatment of psoriasis. curcumol 29-37 Janus kinase 1 Homo sapiens 139-143 34359628-8 2021 Finally, JAK1/2-STAT6 pathway inhibition by ruxolitinib, an FDA approved drug, in cell line models and in one T-LBL primary sample led to cell proliferation reduction and increased apoptosis. ruxolitinib 44-55 Janus kinase 1 Homo sapiens 9-15 34321087-12 2021 Moreover, RSV significantly attenuated the level of IL-6 secretion, which was accompanied by less phosphorylation of the transcription factors Janus kinase 1 (JAK1) and signal transducer and activator of transcription 3 (STAT3). Resveratrol 10-13 Janus kinase 1 Homo sapiens 143-157 34321087-12 2021 Moreover, RSV significantly attenuated the level of IL-6 secretion, which was accompanied by less phosphorylation of the transcription factors Janus kinase 1 (JAK1) and signal transducer and activator of transcription 3 (STAT3). Resveratrol 10-13 Janus kinase 1 Homo sapiens 159-163 34118090-0 2021 Systemic Jak1 activation causes extrarenal calcitriol production and skeletal alterations provoking stunted growth. Calcitriol 43-53 Janus kinase 1 Homo sapiens 9-13 34371735-6 2021 Ruxolitinib was designed as a molecule with low nanomolar potency selective for JAK1 and 2 enzymes, but without significant inhibition of non-JAK kinases, as well as physicochemical properties for both topical and oral administration. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 80-90 34371735-8 2021 Ruxolitinib cream represents a novel, JAK1/2 selective therapy that can be delivered directly to the skin to treat a number of cytokine-driven, inflammatory dermatoses. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 38-44 34260836-3 2021 In retrospective surveys, ruxolitinib, a Janus kinase (JAK1-JAK2) inhibitor, showed potential efficacy in patients with glucocorticoid-refractory or -dependent chronic GVHD. ruxolitinib 26-37 Janus kinase 1 Homo sapiens 55-59 34276662-2 2021 The effect of the JAK1/2 kinase inhibitor ruxolitinib on treating steroid-refractory acute GVHD has been verified by the REACH1/2 study; however, its safety and efficacy in patients with steroid-refractory chronic GVHD (SR-cGVHD) remain unclear. ruxolitinib 42-53 Janus kinase 1 Homo sapiens 18-24 34275303-12 2021 Furthermore, targeted synthetic drugs are used in the treatment of PsA, namely the phosphodiesterase-4 inhibitor apremilast, whose efficacy is lower, and the newly introduced JAK1/3 inhibitor tofacitinib. tofacitinib 192-203 Janus kinase 1 Homo sapiens 175-181 34167562-7 2021 RESULTS: All NOTCH1-signaling-dependent T-ALL cell lines were sensitive to MRK-560 and its combination with ruxolitinib or imatinib in JAK1- or ABL1-dependent cell lines synergistically inhibited leukemia proliferation. Imatinib Mesylate 123-131 Janus kinase 1 Homo sapiens 135-139 34068690-7 2021 The constitutive activation of the tyrosine kinase JAK2 is targeted by ruxolitinib, a JAK1/JAK2 tyrosine kinase inhibitor for PV patients who are resistant or intolerant to cytoreductive treatment with hydroxyurea. ruxolitinib 71-82 Janus kinase 1 Homo sapiens 86-90 34206393-4 2021 However, IL-6 and the JAK1/2 inhibitor Ruxolitinib significantly increased angiogenic factors-endothelial nitric oxide synthase (eNOS), VEGF, and hypoxia-inducible factor-1 alpha (HIF-1alpha)-in patients with polycythemia vera (PV). ruxolitinib 39-50 Janus kinase 1 Homo sapiens 22-28 34090625-2 2021 We assessed the efficacy and safety of filgotinib, a once-daily, oral Janus kinase 1 preferential inhibitor, for treatment of ulcerative colitis. GLPG0634 39-49 Janus kinase 1 Homo sapiens 70-84 34097138-10 2021 Most recently, ruxolitinib, a JAK1/2 inhibitor targeting JAK-STAT signaling downstream from CSF3R, has emerged as a potentially promising new candidate for the treatment of CNL. ruxolitinib 15-26 Janus kinase 1 Homo sapiens 30-36 34073410-4 2021 Numerous JAK inhibitors (JAKinibs) have entered clinical trials, including the JAK1/2 inhibitor Ruxolitinib approved for the treatment of MPN. ruxolitinib 96-107 Janus kinase 1 Homo sapiens 79-85 34097573-4 2022 Flow cytometry, microscopy and other assays found that potent JAK1/2 inhibitors baricitinib and ruxolitinib reduced platelet adhesion to collagen, as well as platelet aggregation, secretion and integrin alphaIIbbeta3 activation in response to the glycoprotein VI (GPVI) agonist collagen-related peptide (CRP-XL). baricitinib 80-91 Janus kinase 1 Homo sapiens 62-68 34097573-4 2022 Flow cytometry, microscopy and other assays found that potent JAK1/2 inhibitors baricitinib and ruxolitinib reduced platelet adhesion to collagen, as well as platelet aggregation, secretion and integrin alphaIIbbeta3 activation in response to the glycoprotein VI (GPVI) agonist collagen-related peptide (CRP-XL). ruxolitinib 96-107 Janus kinase 1 Homo sapiens 62-68 35072287-1 2022 AIMS: Filgotinib is a potent, oral, JAK1-preferential inhibitor for the treatment of rheumatoid arthritis (RA). GLPG0634 6-16 Janus kinase 1 Homo sapiens 36-40 34910214-0 2021 Filgotinib, a novel JAK1-preferential inhibitor for the treatment of rheumatoid arthritis: An overview from clinical trials. GLPG0634 0-10 Janus kinase 1 Homo sapiens 20-24 34910214-3 2021 Filgotinib has demonstrated preferential inhibition of JAK1-dependent cytokine signaling in in vitro assays. GLPG0634 0-10 Janus kinase 1 Homo sapiens 55-59 34349069-6 2021 Based on these findings, an investigator-initiated clinical research of a JAK1/2 inhibitor ruxolitinib for CAEBV infection was initiated in January 2019. ruxolitinib 91-102 Janus kinase 1 Homo sapiens 74-80 35609978-1 2022 OBJECTIVES: To elucidate the mechanism of action of baricitinib, a Janus kinase (JAK) 1/2 inhibitor, and describe immunological pathways related to disease activity in adults with systemic lupus erythematosus (SLE) receiving standard background therapy in a phase II trial. baricitinib 52-63 Janus kinase 1 Homo sapiens 67-89 35604239-0 2022 Ruxolitinib, a JAK1/2 Inhibitor as Treatment for Paraneoplastic Pemphigus: A Case Report. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 15-21 35363892-2 2022 Ruxolitinib (RUX) is the JAK1/2 inhibitor most used for treatment of MF-related splenomegaly and symptoms. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 25-31 35363892-2 2022 Ruxolitinib (RUX) is the JAK1/2 inhibitor most used for treatment of MF-related splenomegaly and symptoms. ruxolitinib 13-16 Janus kinase 1 Homo sapiens 25-31 35603634-4 2022 Momelotinib is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of hepcidin expression and increased availability of iron for erythropoiesis. N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide 0-11 Janus kinase 1 Homo sapiens 17-21 35603634-4 2022 Momelotinib is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of hepcidin expression and increased availability of iron for erythropoiesis. Iron 145-149 Janus kinase 1 Homo sapiens 17-21 35635540-1 2022 Ruxolitinib (RUX), a small molecule inhibitor of JAK1/JAK2, has been identified as the possible novel targeted agent for the treatment of hemophagocytic lymphohistiocytosis (HLH). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 49-53 35635540-1 2022 Ruxolitinib (RUX), a small molecule inhibitor of JAK1/JAK2, has been identified as the possible novel targeted agent for the treatment of hemophagocytic lymphohistiocytosis (HLH). ruxolitinib 13-16 Janus kinase 1 Homo sapiens 49-53 35614292-1 2022 INTRODUCTION: The phase 2 MANTA and MANTA-RAy studies were developed in consultation with global regulatory authorities to investigate potential impacts of filgotinib, a Janus kinase 1 preferential inhibitor, on semen parameters in men with active inflammatory diseases. GLPG0634 156-166 Janus kinase 1 Homo sapiens 170-184 35597252-1 2022 BACKGROUND: The phase 3b, randomised, open-label RESPONSE-2 study in patients with inadequately controlled polycythaemia vera without splenomegaly showed superiority of the Janus kinase (JAK) 1 and JAK2 inhibitor ruxolitinib versus best available therapy for the primary endpoint of haematocrit control at week 28. ruxolitinib 213-224 Janus kinase 1 Homo sapiens 173-193 35595725-9 2022 Imaging analysis detected phosphotyrosine STAT3 in MF patients" BM fibrocytes, and transfection of fibrocytes with STAT3-siRNA or treatment with a JAK1/2 inhibitor ruxolitinib reduced GLI1 and MMP2/9 levels. ruxolitinib 164-175 Janus kinase 1 Homo sapiens 147-153 35599279-8 2022 RESULTS: In ARPE-19 cells exposed to high-glucose conditions, the mRNA and secretory protein levels of VEGF, p-JAK1, p-JAK2, p-STAT3, and p-STAT5 levels were significantly increased. Glucose 42-49 Janus kinase 1 Homo sapiens 111-115 35529449-3 2022 Initially, the ligand-based pharmacophore models were generated using a set of 52 JAK1 inhibitors named C-2 methyl/hydroxyethyl imidazopyrrolopyridines derivatives. c-2 methyl/hydroxyethyl imidazopyrrolopyridines 104-151 Janus kinase 1 Homo sapiens 82-86 35578304-2 2022 Baricitinib is a Janus kinase (JAK)1 and 2 inhibitor that was shown to have therapeutic benefit in patients with SLE in a phase II clinical trial. baricitinib 0-11 Janus kinase 1 Homo sapiens 17-42 34978076-0 2022 Janus kinase 1 inhibitor INCB054707 for patients with moderate-to-severe hidradenitis suppurativa: results from two phase 2 studies. incb054707 25-35 Janus kinase 1 Homo sapiens 0-14 34978076-2 2022 OBJECTIVES: To describe safety and efficacy results from two multicenter phase 2 trials of the JAK1 inhibitor INCB054707 in patients with moderate-to-severe HS. incb054707 110-120 Janus kinase 1 Homo sapiens 95-99 35157370-2 2022 This phase 1, randomized, placebo-controlled trial assessed the pharmacokinetics and safety of single and multiple ascending doses up to 15 mg twice daily for 14 days of a JAK1 inhibitor, GDC-0214, in healthy volunteers (HVs; n=66). gdc-0214 188-196 Janus kinase 1 Homo sapiens 172-176 35437207-10 2022 Dexamethasone (a corticosteroid) significantly inhibited, while ABT494 (a JAK1 inhibitor) partially inhibited, EKH"s induction of cytokines in fibroblasts. upadacitinib 64-70 Janus kinase 1 Homo sapiens 74-78 35437207-10 2022 Dexamethasone (a corticosteroid) significantly inhibited, while ABT494 (a JAK1 inhibitor) partially inhibited, EKH"s induction of cytokines in fibroblasts. 5-Chlorotubercidin 111-114 Janus kinase 1 Homo sapiens 74-78 35368384-2 2022 The Janus kinase (JAK)1/JAK2 inhibitor ruxolitinib reduces inflammatory cytokine concentrations in disorders characterised by cytokine dysregulation, including graft-versus-host disease, myelofibrosis, and secondary hemophagocytic lymphohistiocytosis. ruxolitinib 39-50 Janus kinase 1 Homo sapiens 4-23 35368384-3 2022 We assessed whether treatment with the JAK1/JAK2 inhibitor ruxolitinib would be beneficial in patients with COVID-19 admitted to hospital. ruxolitinib 59-70 Janus kinase 1 Homo sapiens 39-43 35484697-1 2022 BACKGROUND: Baricitinib, an oral selective Janus Kinase (JAK) 1 and JAK 2 inhibitor, was shown to improve the signs and symptoms of moderate-to-severe atopic dermatitis (AD). baricitinib 12-23 Janus kinase 1 Homo sapiens 43-63 35481616-0 2022 Esophageal lichen planus successfully treated with the JAK1/3 inhibitor tofacitinib. tofacitinib 72-83 Janus kinase 1 Homo sapiens 55-61 35451191-0 2022 Arachidonic acid, a clinically adverse mediator in the ovarian cancer microenvironment, impairs JAK-STAT signaling in macrophages by perturbing lipid raft structures. Arachidonic Acid 0-16 Janus kinase 1 Homo sapiens 96-99 35507130-8 2022 Ex vivo treatment with the JAK1/2-inhibitor ruxolitinib reduced cytokine responsiveness and normalized STAT1 phosphorylation in DN STAT3 and STAT1 GOF patient" cells. ruxolitinib 44-55 Janus kinase 1 Homo sapiens 27-31 35368221-1 2022 BACKGROUND: Ruxolitinib cream is a topical formulation of ruxolitinib, an inhibitor of Janus kinase 1 and Janus kinase 2. ruxolitinib 12-23 Janus kinase 1 Homo sapiens 87-101 35368221-1 2022 BACKGROUND: Ruxolitinib cream is a topical formulation of ruxolitinib, an inhibitor of Janus kinase 1 and Janus kinase 2. ruxolitinib 58-69 Janus kinase 1 Homo sapiens 87-101 35503162-1 2022 Baricitinib (Olumiant ) is an oral small molecule inhibitor of Janus kinase (JAK)1 and JAK2, which have been implicated in the pathogenesis of atopic dermatitis (AD). baricitinib 0-11 Janus kinase 1 Homo sapiens 63-82 35503162-1 2022 Baricitinib (Olumiant ) is an oral small molecule inhibitor of Janus kinase (JAK)1 and JAK2, which have been implicated in the pathogenesis of atopic dermatitis (AD). baricitinib 13-21 Janus kinase 1 Homo sapiens 63-82 35266648-3 2022 Inhibition of IFNG pathway by the JAK1/2 inhibitor ruxolitinib or knocking out Stat1 gene abrogated the IFNG-induced melanogenesis. ruxolitinib 51-62 Janus kinase 1 Homo sapiens 34-40 35382859-5 2022 The effects of Ruxolitinib (JAK1/2 inhibitor) on liver fibrosis were studied in LX-2 cells and two progressive and reversible fibrosis animal models (carbon tetrachloride (CCl4), Thioacetamide (TAA)). ruxolitinib 15-26 Janus kinase 1 Homo sapiens 28-34 35443042-6 2022 Ruxolitinib, an oral selective JAK1/2 inhibitor, received FDA approval for the treatment of steroid-refractory acute GVHD in 2019 and remains the only agent approved for acute GVHD. ruxolitinib 0-11 Janus kinase 1 Homo sapiens 31-37 35437311-1 2022 Outside of clinical trials and before commercial availability for acute and chronic graft-versus-host disease (GVHD), the Janus kinase (JAK) 1/JAK2 inhibitor ruxolitinib was available to US patients with steroid-refractory GVHD through an open-label, multicenter expanded access program (EAP) sponsored by Incyte Corporation. ruxolitinib 158-169 Janus kinase 1 Homo sapiens 122-142 35267240-0 2022 Response of rheumatoid arthritis-associated pyoderma gangrenous to the JAK1 inhibitor upadacitinib. upadacitinib 86-98 Janus kinase 1 Homo sapiens 71-75 35346999-10 2022 Furthermore, CJ14939 also promoted oxaliplatin-induced cell death, up-regulated expression of cleaved caspase-3, and down-regulated expression of phospho-JAK1 and phospho-STAT3. Oxaliplatin 35-46 Janus kinase 1 Homo sapiens 154-158 35100463-6 2022 The molecular mechanism of cytotoxicity observed around Fr7 against ATL cells was the degradation of JAK1 to 3 and the dephosphorylation of STAT3/5, which occurs by proteasome-dependent proteolysis, confirming that PAC directly binds to HSP90. proanthocyanidin 215-218 Janus kinase 1 Homo sapiens 101-105 35446502-0 2022 Ansprechen eines mit rheumatoider Arthritis assoziierten Pyoderma gangraenosum auf den JAK1-Inhibitor Upadacitinib. upadacitinib 102-114 Janus kinase 1 Homo sapiens 87-91 35365828-1 2022 OBJECTIVE: Characterize safety of the Janus kinase-1 preferential inhibitor filgotinib in Japanese patients with moderately to severely active rheumatoid arthritis. GLPG0634 76-86 Janus kinase 1 Homo sapiens 38-52 35346999-9 2022 RESULTS: CJ14939 induced cell death, and inhibited phosphorylation of JAK1 and STAT3 in colorectal cancer cells. cj14939 9-16 Janus kinase 1 Homo sapiens 70-74 35346999-10 2022 Furthermore, CJ14939 also promoted oxaliplatin-induced cell death, up-regulated expression of cleaved caspase-3, and down-regulated expression of phospho-JAK1 and phospho-STAT3. cj14939 13-20 Janus kinase 1 Homo sapiens 154-158 35041155-1 2022 INTRODUCTION: Baricitinib is an oral Janus kinase (JAK)1/JAK2 inhibitor approved to treat rheumatoid arthritis (RA). baricitinib 14-25 Janus kinase 1 Homo sapiens 37-56 35354957-0 2022 Itaconate modifies JAK1. itaconic acid 0-9 Janus kinase 1 Homo sapiens 19-23 35235776-0 2022 Itaconate and itaconate derivatives target JAK1 to suppress alternative activation of macrophages. itaconic acid 0-9 Janus kinase 1 Homo sapiens 43-47 35371054-4 2022 Interferon (IFN)-gamma induces IDO1 expression through the Jak/STAT1 pathway and mediates Kyn production concomitantly with Trp consumption in CLL-conditioned media, while INCB018424 (ruxolitinib), a JAK1/2 inhibitor, impaired both effects. ruxolitinib 172-182 Janus kinase 1 Homo sapiens 59-62 35371054-4 2022 Interferon (IFN)-gamma induces IDO1 expression through the Jak/STAT1 pathway and mediates Kyn production concomitantly with Trp consumption in CLL-conditioned media, while INCB018424 (ruxolitinib), a JAK1/2 inhibitor, impaired both effects. ruxolitinib 184-195 Janus kinase 1 Homo sapiens 59-62 35371054-4 2022 Interferon (IFN)-gamma induces IDO1 expression through the Jak/STAT1 pathway and mediates Kyn production concomitantly with Trp consumption in CLL-conditioned media, while INCB018424 (ruxolitinib), a JAK1/2 inhibitor, impaired both effects. ruxolitinib 184-195 Janus kinase 1 Homo sapiens 200-206 35184688-9 2022 CircPIP5K1A was available to competitively combine with miR-552-3p, while whose direct target was JAK1. mir-552-3p 56-66 Janus kinase 1 Homo sapiens 98-102 35364216-2 2022 CTP-543, a deuterated compound that selectively inhibits JAK1 and JAK2, is being developed as an oral treatment for AA. Deuruxolitinib 0-7 Janus kinase 1 Homo sapiens 57-61 35319396-7 2022 Baricitinib, the Janus kinase (JAK) 1/2 inhibitor, is also an attractive candidate due to its properties as a potent anti-inflammatory agent and its hypothesized off-target antiviral effects against SARS-CoV-2. baricitinib 0-11 Janus kinase 1 Homo sapiens 17-39 35337171-5 2022 Recently, the FDA approved the use of ruxolitinib, a JAK1/2 inhibitor, in the treatment of acute steroid-refractory GVHD (SR-aGVHD), highlighting the role of JAK inhibition in this immune deregulation. ruxolitinib 38-49 Janus kinase 1 Homo sapiens 53-59 35235776-0 2022 Itaconate and itaconate derivatives target JAK1 to suppress alternative activation of macrophages. itaconic acid 14-23 Janus kinase 1 Homo sapiens 43-47 35235776-5 2022 Examination of IL-4 signaling revealed inhibition of JAK1 and STAT6 phosphorylation by both itaconate and OI. itaconic acid 92-101 Janus kinase 1 Homo sapiens 53-57 35235776-7 2022 Importantly, JAK1 was directly modified by itaconate derivatives at multiple residues, including cysteines 715, 816, 943, and 1130. itaconic acid 43-52 Janus kinase 1 Homo sapiens 13-17 35235776-7 2022 Importantly, JAK1 was directly modified by itaconate derivatives at multiple residues, including cysteines 715, 816, 943, and 1130. Cysteine 97-106 Janus kinase 1 Homo sapiens 13-17 35235776-10 2022 We therefore identify itaconate and OI as JAK1 inhibitors, suggesting a new strategy to inhibit JAK1 in M2 macrophage-driven diseases. itaconic acid 22-31 Janus kinase 1 Homo sapiens 42-46 35235776-10 2022 We therefore identify itaconate and OI as JAK1 inhibitors, suggesting a new strategy to inhibit JAK1 in M2 macrophage-driven diseases. itaconic acid 22-31 Janus kinase 1 Homo sapiens 96-100 35213752-9 2022 Conversely, inhibition of IL-22-induced JAK1 signalling with ABT-317 strongly attenuated morphological features of the disease but had no effect on NFkappaB-dependent cytokine production, suggesting distinct mechanisms of action by the cytokines driving psoriasis. abt-317 61-68 Janus kinase 1 Homo sapiens 40-44 35131544-5 2022 Furthermore, propionate-induced IFIT expression is dependent on IFN type I and/or type III-mediated signalling since pre-treatment of A549 cells with Ruxolitinib, a specific JAK1/2 tyrosine kinase inhibitor, prior to stimulation with propionate, inhibited the upregulation of IFIT1 expression. Propionates 13-23 Janus kinase 1 Homo sapiens 174-180 35131544-5 2022 Furthermore, propionate-induced IFIT expression is dependent on IFN type I and/or type III-mediated signalling since pre-treatment of A549 cells with Ruxolitinib, a specific JAK1/2 tyrosine kinase inhibitor, prior to stimulation with propionate, inhibited the upregulation of IFIT1 expression. ruxolitinib 150-161 Janus kinase 1 Homo sapiens 174-180 35288468-1 2022 BACKGROUND: This phase I multicenter study was designed to evaluate the safety, tolerability, efficacy, and translational effects on the tumor microenvironment of itacitinib (Janus-associated kinase 1 (JAK1) inhibitor) in combination with epacadostat (indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor) or parsaclisib (phosphatidylinositol 3-kinase delta (PI3Kdelta) inhibitor). INCB039110 163-173 Janus kinase 1 Homo sapiens 175-200 35288468-1 2022 BACKGROUND: This phase I multicenter study was designed to evaluate the safety, tolerability, efficacy, and translational effects on the tumor microenvironment of itacitinib (Janus-associated kinase 1 (JAK1) inhibitor) in combination with epacadostat (indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor) or parsaclisib (phosphatidylinositol 3-kinase delta (PI3Kdelta) inhibitor). INCB039110 163-173 Janus kinase 1 Homo sapiens 202-206 35235887-0 2022 Piceatannol, a metabolite of resveratrol, attenuates atopic dermatitis by targeting Janus kinase 1. 3,3',4,5'-tetrahydroxystilbene 0-11 Janus kinase 1 Homo sapiens 84-98 35113547-0 2022 Identification of a Novel 2,8-Diazaspiro(4.5)decan-1-one Derivative as a Potent and Selective Dual TYK2/JAK1 Inhibitor for the Treatment of Inflammatory Bowel Disease. 2,8-diazaspiro[4.5]decan-1-one 26-56 Janus kinase 1 Homo sapiens 104-108 35113547-1 2022 In this study, we described a series of 2,8-diazaspiro(4.5)decan-1-one derivatives as selective TYK2/JAK1 inhibitors. 2,8-diazaspiro[4.5]decan-1-one 40-70 Janus kinase 1 Homo sapiens 101-105 35235887-0 2022 Piceatannol, a metabolite of resveratrol, attenuates atopic dermatitis by targeting Janus kinase 1. Resveratrol 29-40 Janus kinase 1 Homo sapiens 84-98 35235887-10 2022 Piceatannol decreased phosphorylation of JAK-STAT protein in the TNFalpha/IFNgamma-induced HaCaT cell line. 3,3',4,5'-tetrahydroxystilbene 0-11 Janus kinase 1 Homo sapiens 41-44 35235887-11 2022 A molecular docking study showed that piceatannol strongly interacts with JAK1, suggesting a possible mode of action. 3,3',4,5'-tetrahydroxystilbene 38-49 Janus kinase 1 Homo sapiens 74-78 35186752-5 2022 RNA sequencing identified 126 genes that were regulated by both FUS-DDIT3 expression and JAK1/2 inhibition using ruxolitinib. ruxolitinib 113-124 Janus kinase 1 Homo sapiens 89-95 35096866-1 2021 Baricitinib is a Janus kinase (JAK) inhibitor used to treat refractory rheumatoid arthritis and blocks the subtypes JAK1 and JAK2. baricitinib 0-11 Janus kinase 1 Homo sapiens 116-120 35590143-4 2022 Treatment with the JAK1 inhibitor itacitinib resulted in a rapid resolution of aplastic anemia and a sustained recovery of hematopoiesis. INCB039110 34-44 Janus kinase 1 Homo sapiens 19-23 34738874-0 2022 AZD3759 enhances radiation effects in non-small-cell lung cancer by a synergistic blockade of epidermal growth factor receptor and Janus kinase-1. AZD3759 0-7 Janus kinase 1 Homo sapiens 131-145 34971577-2 2022 We aimed to evaluate the Janus kinase 1 inhibitor itacitinib versus placebo, both in combination with corticosteroids, for initial treatment of acute GVHD. INCB039110 50-60 Janus kinase 1 Homo sapiens 25-39 35224383-6 2022 In the current study, we investigated the mechanism of binding of baricitinib, filgotinib, itacitinib, and upadacitinib to JAK1 using a combined method of molecular docking, molecular dynamics simulation, and binding free energy calculation via the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) scheme. baricitinib 66-77 Janus kinase 1 Homo sapiens 123-127 35224383-6 2022 In the current study, we investigated the mechanism of binding of baricitinib, filgotinib, itacitinib, and upadacitinib to JAK1 using a combined method of molecular docking, molecular dynamics simulation, and binding free energy calculation via the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) scheme. GLPG0634 79-89 Janus kinase 1 Homo sapiens 123-127 35224383-6 2022 In the current study, we investigated the mechanism of binding of baricitinib, filgotinib, itacitinib, and upadacitinib to JAK1 using a combined method of molecular docking, molecular dynamics simulation, and binding free energy calculation via the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) scheme. INCB039110 91-101 Janus kinase 1 Homo sapiens 123-127 35224383-6 2022 In the current study, we investigated the mechanism of binding of baricitinib, filgotinib, itacitinib, and upadacitinib to JAK1 using a combined method of molecular docking, molecular dynamics simulation, and binding free energy calculation via the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) scheme. upadacitinib 107-119 Janus kinase 1 Homo sapiens 123-127 35224383-8 2022 Due to the increased favorable intermolecular electrostatic contribution, upadacitinib is more selective to JAK1 compared to the other three inhibitors. upadacitinib 74-86 Janus kinase 1 Homo sapiens 108-112 35224383-10 2022 Furthermore, our studies indicated that the hydrophobic residues and hydrogen bonds from the hinge region (Glu957 and Leu959) of JAK1 played an essential role in stabilizing the inhibitors. Hydrogen 69-77 Janus kinase 1 Homo sapiens 129-133 35224383-11 2022 Protein structural network analysis reveals that the total number of links and hubs in JAK1/baricitinib (354, 48) is more significant than those in apo (328, 40) and the other three complexes. baricitinib 92-103 Janus kinase 1 Homo sapiens 87-91 35224383-12 2022 The JAK1/baricitinib complex shows the highest probability of the highest-ranked community, indicating a compact network of the JAK1/baricitinib complex, consistent with its higher stability than the rest of the four systems. baricitinib 9-20 Janus kinase 1 Homo sapiens 4-8 35224383-12 2022 The JAK1/baricitinib complex shows the highest probability of the highest-ranked community, indicating a compact network of the JAK1/baricitinib complex, consistent with its higher stability than the rest of the four systems. baricitinib 9-20 Janus kinase 1 Homo sapiens 128-132 35224383-12 2022 The JAK1/baricitinib complex shows the highest probability of the highest-ranked community, indicating a compact network of the JAK1/baricitinib complex, consistent with its higher stability than the rest of the four systems. baricitinib 133-144 Janus kinase 1 Homo sapiens 4-8 35224383-12 2022 The JAK1/baricitinib complex shows the highest probability of the highest-ranked community, indicating a compact network of the JAK1/baricitinib complex, consistent with its higher stability than the rest of the four systems. baricitinib 133-144 Janus kinase 1 Homo sapiens 128-132 35131254-1 2022 Ruxolitinib is a Janus kinase 1/2 inhibitor (JAK1/2) that blocks signal transduction of interferon-gamma, a critical cytokine involved in the pathogenesis of cutaneous lichen planus (LP). ruxolitinib 0-11 Janus kinase 1 Homo sapiens 45-51 35014922-4 2022 AREAS COVERED: This paper explores the use of upadacitinib (a selective JAK1 inhibitor) for the treatment of psoriatic arthritis. upadacitinib 46-58 Janus kinase 1 Homo sapiens 72-76 35159191-4 2022 MB cells subjected to co-culture with microglia exhibited increased expression of phosphorylated JAK1 and STAT3, which was correlated with enhanced resistance to vincristine. Vincristine 162-173 Janus kinase 1 Homo sapiens 97-101 35260349-0 2022 A Phase 1/2 Study of the Oral Janus Kinase 1 Inhibitors INCB052793 and Itacitinib Alone or in Combination With Standard Therapies for Advanced Hematologic Malignancies. incb052793 56-66 Janus kinase 1 Homo sapiens 30-44 35260349-0 2022 A Phase 1/2 Study of the Oral Janus Kinase 1 Inhibitors INCB052793 and Itacitinib Alone or in Combination With Standard Therapies for Advanced Hematologic Malignancies. INCB039110 71-81 Janus kinase 1 Homo sapiens 30-44 35260349-3 2022 PATIENTS AND METHODS: This phase 1/2 study evaluated 2 oral, novel JAK1 inhibitors (INCB052793 and itacitinib) in advanced hematologic malignancies. incb052793 84-94 Janus kinase 1 Homo sapiens 67-71 35260349-3 2022 PATIENTS AND METHODS: This phase 1/2 study evaluated 2 oral, novel JAK1 inhibitors (INCB052793 and itacitinib) in advanced hematologic malignancies. INCB039110 99-109 Janus kinase 1 Homo sapiens 67-71 34738874-7 2022 Mechanistically, the receptor tyrosine kinase signaling antibody array revealed that Janus kinase-1 (JAK1) was specifically inhibited by AZD3759, but not by osimertinib. AZD3759 137-144 Janus kinase 1 Homo sapiens 85-99 34738874-8 2022 The effects of AZD3759 on RA efficacy in PC-9 cells and in a brain metastasis animal model were significantly abolished by the overexpression of JAK1. AZD3759 15-22 Janus kinase 1 Homo sapiens 145-149 34738874-9 2022 Collectively, our results suggested that AZD3759 promoted RA antitumor effects in NSCLC by synergistic blockade of EGFR and JAK1. AZD3759 41-48 Janus kinase 1 Homo sapiens 124-128 35505771-3 2022 Tofacitinib was the first pan-Janus kinase (Jak) inhibitor approved for the treatment of IBD, targeting the 4 isoforms of cytokine-associated Jaks (Jak1, Jak2, Jak3, and tyrosine-protein kinase 2). tofacitinib 0-11 Janus kinase 1 Homo sapiens 148-152