PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 26845171-0 2016 TGF-beta Type I Receptor Kinase Inhibitor EW-7197 Suppresses Cholestatic Liver Fibrosis by Inhibiting HIF1alpha-Induced Epithelial Mesenchymal Transition. vactosertib 42-49 hypoxia inducible factor 1 subunit alpha Homo sapiens 102-111 28732811-10 2017 EW7197, an inhibitor for activin receptor-like kinase 5/TGF-beta receptor I (TGFbetaR1) suppressed KA-mediated phosphorylation of Smad2. vactosertib 0-6 SMAD family member 2 Mus musculus 130-135 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 transforming growth factor beta 1 Homo sapiens 45-53 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 centromere protein W Homo sapiens 76-80 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 AKT serine/threonine kinase 1 Homo sapiens 112-115 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 mitogen-activated protein kinase 1 Homo sapiens 117-120 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 mitogen-activated protein kinase 8 Homo sapiens 122-125 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 transforming growth factor beta 1 Homo sapiens 155-163 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 SMAD family member 2 Homo sapiens 214-221 27974707-7 2017 Treatment with EW-7197, a novel inhibitor of TGF-beta signaling, diminished CUG2-mediated EMT and inhibition of Akt, ERK, JNK, and p38 MAPK, non-canonical TGF-beta signaling molecules, also decreased expression of Smad2/3, Snail and Twist, leading to inhibition of EMT. vactosertib 15-22 snail family transcriptional repressor 1 Homo sapiens 223-228 26845171-8 2016 In addition, EW-7197 inhibited HIF1alpha-derived HSC activation and expression of EMT markers in LX-2 cells in vitro. vactosertib 13-20 hypoxia inducible factor 1 subunit alpha Homo sapiens 31-40 26549110-2 2015 This study was undertaken to gain the proof of concept of a small-molecule inhibitor of TGF-beta type I receptor kinase, EW-7197 as a potent anti-cancer therapy for HCC. vactosertib 121-128 transforming growth factor beta 1 Homo sapiens 88-96 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 transforming growth factor beta receptor 1 Homo sapiens 70-74 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 CD44 molecule (Indian blood group) Homo sapiens 236-240 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 CD24 molecule Homo sapiens 242-246 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 POU class 5 homeobox 1 Homo sapiens 284-288 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 Nanog homeobox Homo sapiens 290-295 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 Kruppel like factor 4 Homo sapiens 297-301 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 MYC proto-oncogene, bHLH transcription factor Homo sapiens 303-306 26462028-4 2015 Blocking TGF-beta signaling with the TGF-beta type I receptor kinase (ALK5) inhibitor, EW-7197, suppresses paclitaxel-induced EMT and CSC properties such as mammosphere-forming efficiency (MSFE), aldehyde dehydrogenase (ALDH) activity, CD44+/CD24- ratio, and pluripotency regulators (Oct4, Nanog, Klf4, Myc, and Sox2). vactosertib 87-94 SRY-box transcription factor 2 Homo sapiens 312-316 26549110-6 2015 In addition, EW-7197 inhibited TGF-beta-stimulated TIMP-1 secretion by HSCs as well as the TIMP-1-induced proliferation, motility, and survival of HCC cells. vactosertib 13-20 TIMP metallopeptidase inhibitor 1 Homo sapiens 91-97 26549110-6 2015 In addition, EW-7197 inhibited TGF-beta-stimulated TIMP-1 secretion by HSCs as well as the TIMP-1-induced proliferation, motility, and survival of HCC cells. vactosertib 13-20 transforming growth factor beta 1 Homo sapiens 31-39 26549110-6 2015 In addition, EW-7197 inhibited TGF-beta-stimulated TIMP-1 secretion by HSCs as well as the TIMP-1-induced proliferation, motility, and survival of HCC cells. vactosertib 13-20 TIMP metallopeptidase inhibitor 1 Homo sapiens 51-57 34478262-3 2021 To surmount the pathological obstacle, we developed a size switchable nanosystem based on PEG-PLGA nanospheres encapsulated within liposomes for the combined delivery of vactosertib (VAC), a TGF-beta1 receptor kinase inhibitor, and the cytotoxic drug paclitaxel (TAX). vactosertib 170-181 transforming growth factor beta 1 Homo sapiens 191-200 25487606-0 2015 EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-beta/Smad and ROS signaling. vactosertib 0-7 transforming growth factor beta 1 Homo sapiens 68-76 25487606-4 2015 Western blot, immunofluorescence, siRNA, and ChIP analysis were carried out to characterize EW-7197 as a TGF-beta/Smad signaling inhibitor in LX-2, Hepa1c1c7, NRK52E, and MRC5 cells. vactosertib 92-99 transforming growth factor beta 1 Homo sapiens 105-113 24127404-4 2013 Oral treatment with a novel ALK5 inhibitor, EW-7197 (2.5 mg/kg daily) or a representative ALK5 inhibitor, LY-2157299 (75 mg/kg bid) suppressed the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. vactosertib 44-51 transforming growth factor, beta receptor I Mus musculus 28-32 24786585-0 2014 Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-beta type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. vactosertib 123-130 transforming growth factor beta receptor 1 Homo sapiens 198-222 35390248-2 2022 Here we evaluated the anti-metastatic therapeutic potential of vactosertib, an orally bioavailable TGF-beta type I receptor (activin receptor-like kinase 5, ALK5) inhibitor, via suppression of radiation-induced EMT and CSC properties, oxidative stress generation, and breast to lung metastasis in a breast cancer mouse model and breast cancer cell lines. vactosertib 63-74 transforming growth factor, beta receptor I Mus musculus 157-161 34445093-10 2021 Pretreatment with EW-7197 prevented the effects of HMGB1. vactosertib 18-25 high mobility group box 1 Homo sapiens 51-56 35390248-8 2022 CONCLUSIONS: These results indicate that inhibition of TGF-beta signaling with vactosertib in breast cancer patients undergoing radiotherapy would be an attractive strategy for the prevention of cancer metastasis and recurrence. vactosertib 79-90 transforming growth factor alpha Homo sapiens 55-63 35024955-8 2022 Knockdown of FOXO3 prevented the growth of cilia-like structures induced by EW-7197 or AG-1478 and induced cell migration under treatment with EW-7197. vactosertib 76-83 forkhead box O3 Mus musculus 13-18 35024955-8 2022 Knockdown of FOXO3 prevented the growth of cilia-like structures induced by EW-7197 or AG-1478 and induced cell migration under treatment with EW-7197. vactosertib 143-150 forkhead box O3 Mus musculus 13-18 33890869-8 2021 Treatment with follistatin, a potent inhibitor of activin, or vactosertib, which inhibits both TGFbetaR1 and the activin type I receptor ALK4, induced a profound inhibition of pSMAD in BrafV600E-PTCs. vactosertib 62-73 activin A receptor, type 1B Mus musculus 137-141 35255604-3 2022 We aimed to examine the effects of EW-7197, an inhibitor of TGF-beta type 1 receptor kinase (ALK5), in retarding the progression of DN, both in vivo, using a diabetic mouse model (db/db mice), and in vitro, in podocytes and mesangial cells. vactosertib 35-42 transforming growth factor, beta receptor I Mus musculus 93-97 35255604-11 2022 Treatment with EW-7197 significantly inhibited TGF-beta signaling, inflammation, apoptosis, reactive oxygen species, and endoplasmic reticulum stress in diabetic mice and renal cells. vactosertib 15-22 transforming growth factor alpha Mus musculus 47-55 35255604-13 2022 EW-7197 alleviates renal fibrosis and inflammation in diabetes by inhibiting downstream TGF-beta signaling, thereby retarding the progression of DN. vactosertib 0-7 transforming growth factor alpha Mus musculus 88-96 32076068-4 2020 Compared to nal-IRI/5-FU/LV treatment, combining nal-IRI/5-FU/LV with vactosertib, a TGF-beta signalling inhibitor, significantly improved long-term survival rates and effectively suppressed invasion to surrounding tissues. vactosertib 70-81 transforming growth factor alpha Mus musculus 85-93 32857676-5 2020 Pretreatment with EW-7197 prevented the changes of all tight junction molecules induced by HMGB1. vactosertib 18-25 high mobility group box 1 Homo sapiens 91-96 32857676-6 2020 In 2.5D Matrigel culture, treatment with HMGB1 induced permeability of FITC-dextran (FD-4) into the lumen, whereas pretreatment with EW-7197 prevented the hyperpermeability of FD-4 into the lumen caused by HMGB1. vactosertib 133-140 high mobility group box 1 Homo sapiens 206-211 32857676-8 2020 In the 2D culture of HLE cells with HMGB1, knockdown of p63 increased the level of angulin-1/LSR and CLDN-4, while pretreatment with EW-7197 enhanced the increase of CLDN-4 induced by knockdown of p63. vactosertib 133-140 claudin 4 Homo sapiens 166-172 32857676-8 2020 In the 2D culture of HLE cells with HMGB1, knockdown of p63 increased the level of angulin-1/LSR and CLDN-4, while pretreatment with EW-7197 enhanced the increase of CLDN-4 induced by knockdown of p63. vactosertib 133-140 tumor protein p63 Homo sapiens 197-200 32423802-8 2020 Treatment with EW-7197, a transforming growth factor-beta (TGF-beta) type I receptor kinase inhibitor, prevented all the effects of HMGB1 in Calu-3 cells. vactosertib 15-22 tumor necrosis factor Homo sapiens 26-57 32423802-8 2020 Treatment with EW-7197, a transforming growth factor-beta (TGF-beta) type I receptor kinase inhibitor, prevented all the effects of HMGB1 in Calu-3 cells. vactosertib 15-22 high mobility group box 1 Homo sapiens 132-137 32423802-10 2020 The effects of HMGB1 contribute to TGF-beta signaling and EW-7197 shows potential for use in therapy for HMGB1-induced airway inflammation. vactosertib 58-65 high mobility group box 1 Homo sapiens 105-110 31496148-1 2020 PURPOSE: To examine the therapeutic effect of Vactosertib, a small molecule inhibitor of transforming growth factor-beta (TGF-beta) type I receptor (activin receptor-like kinase-5, ALK5), in an experimental model of Peyronie"s disease (PD) and determining anti-fibrotic mechanisms of Vactosertib in primary fibroblasts derived from human PD plaques. vactosertib 46-57 transforming growth factor beta receptor 1 Homo sapiens 181-185 31496148-7 2020 RESULTS: Vactosertib induced significant regression of fibrotic plaques in PD rats in vivo through reduced infiltration of inflammatory cells and reduced expression of phospho-Smad2, which recovered erectile function. vactosertib 9-20 SMAD family member 2 Rattus norvegicus 176-181 31496148-8 2020 Vactosertib also abrogated TGF-beta1-induced enhancement of extracellular matrix protein production and hydroxyproline content in PD fibroblasts in vitro by hindering the TGF-beta1-induced Smad2/3 phosphorylation and nuclear translocation, and fibroblast-to-myofibroblast transdifferentiation. vactosertib 0-11 transforming growth factor, beta 1 Rattus norvegicus 27-36 31496148-8 2020 Vactosertib also abrogated TGF-beta1-induced enhancement of extracellular matrix protein production and hydroxyproline content in PD fibroblasts in vitro by hindering the TGF-beta1-induced Smad2/3 phosphorylation and nuclear translocation, and fibroblast-to-myofibroblast transdifferentiation. vactosertib 0-11 transforming growth factor, beta 1 Rattus norvegicus 171-180 31496148-8 2020 Vactosertib also abrogated TGF-beta1-induced enhancement of extracellular matrix protein production and hydroxyproline content in PD fibroblasts in vitro by hindering the TGF-beta1-induced Smad2/3 phosphorylation and nuclear translocation, and fibroblast-to-myofibroblast transdifferentiation. vactosertib 0-11 SMAD family member 2 Rattus norvegicus 189-194 31300967-0 2020 Pharmacokinetic characteristics of vactosertib, a new activin receptor-like kinase 5 inhibitor, in patients with advanced solid tumors in a first-in-human phase 1 study. vactosertib 35-46 transforming growth factor beta receptor 1 Homo sapiens 54-84 31300967-1 2020 Purposes Vactosertib is a new investigational inhibitor of activin receptor-like kinase 5. vactosertib 9-20 transforming growth factor beta receptor 1 Homo sapiens 59-89 32076068-6 2020 Particularly, the expression of tumour-suppressing gene Ccdc80 was induced by vactosertib and further induced by vactosertib in combination with nal-IRI/5-FU/LV. vactosertib 78-89 coiled-coil domain containing 80 Mus musculus 56-62 32076068-6 2020 Particularly, the expression of tumour-suppressing gene Ccdc80 was induced by vactosertib and further induced by vactosertib in combination with nal-IRI/5-FU/LV. vactosertib 113-124 coiled-coil domain containing 80 Mus musculus 56-62 32076068-8 2020 Collectively, these results indicate that combination treatment of vactosertib with nal-IRI/5-FU/LV improves overall survival rates in a mouse model of pancreatic cancer by suppressing invasion through CCDC80. vactosertib 67-78 coiled-coil domain containing 80 Mus musculus 202-208 31138521-5 2019 Inhibiting TGFbeta signaling in NK cells using the TGFbeta receptor 1 (R1) inhibitor (EW-7197) significantly enhanced VAY736-induced NK cell-mediated ALL killing. vactosertib 86-93 transforming growth factor beta 1 Homo sapiens 11-18 31138521-5 2019 Inhibiting TGFbeta signaling in NK cells using the TGFbeta receptor 1 (R1) inhibitor (EW-7197) significantly enhanced VAY736-induced NK cell-mediated ALL killing. vactosertib 86-93 CD1b molecule Homo sapiens 51-73 30135214-7 2018 Moreover, TEW7197, a specific TbetaR1 kinase inhibitor, reduces tumor formation in the NF2-model mouse (Postn-Cre;NF2f/f). vactosertib 10-17 trace amine associated receptor 1 Homo sapiens 30-37 30135214-7 2018 Moreover, TEW7197, a specific TbetaR1 kinase inhibitor, reduces tumor formation in the NF2-model mouse (Postn-Cre;NF2f/f). vactosertib 10-17 neurofibromin 2 Mus musculus 87-90 30135214-8 2018 Gene expression profiling reveals that TEW7197 treatment induces the expression of lipid metabolism-related gene set, such as NF2-restored cells in HEI-193 (NF2-deficient Schwannoma). vactosertib 39-46 neurofibromin 2 Mus musculus 126-129 30135214-8 2018 Gene expression profiling reveals that TEW7197 treatment induces the expression of lipid metabolism-related gene set, such as NF2-restored cells in HEI-193 (NF2-deficient Schwannoma). vactosertib 39-46 neurofibromin 2 Mus musculus 157-160