PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 30969964-10 2019 Both were attenuated by the ERK1/2 signaling inhibitors, U0126 and AZD6244. AZD 6244 67-74 mitogen-activated protein kinase 3 Homo sapiens 28-34 31201369-10 2019 Based on the HPC3 cell model, we found that the DSTYK mutation promoted cell migration and invasion of HPC3 cells via activation of ERK1/2 signaling, which was inhibited by the MEK/ERK inhibitor AZD6244. AZD 6244 195-202 mitogen-activated protein kinase 3 Homo sapiens 132-138 33536190-8 2021 The AKT inhibitor MK-2206 reduced AKT1/2/3 phosphorylation in SW620 xenograft tumors 2 to 4 hours post-dose, and the MEK inhibitor selumetinib reduced MEK1/2 and ERK1/2 phosphorylation by up to 50% and >90%, respectively. AZD 6244 131-142 mitogen-activated protein kinase 3 Homo sapiens 162-168 32540097-7 2020 We demonstrate that the expression of point mutation of lamin A in muscle cells increases cellular stiffness compared with cells expressing wild type lamin A and that the chemical agent selumetinib, an inhibitor of the ERK1/2 signaling, reversed the mechanical alterations in mutated cells. AZD 6244 186-197 mitogen-activated protein kinase 3 Homo sapiens 219-225 31649535-3 2019 MK2206 or AZD6244, representative Akt and Erk1/2 inhibitors, respectively, profoundly sensitized bladder cancer cells to THP treatment. AZD 6244 10-17 mitogen-activated protein kinase 3 Homo sapiens 42-48 31461811-11 2019 After treatment with AZD6244 (5, 10 mumol/L), the level of p-ERK1/2 in OVCAR5 and OVCAR8 decreased significantly in dose-dependent manner. AZD 6244 21-28 mitogen-activated protein kinase 3 Homo sapiens 61-67 31461811-16 2019 AZD6244 could down-regulated the expression of p-ERK1/2 in ovarian cancer cells, accompanied by the decreased proliferation and increased cell apoptosis of ovarian cancer cells. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 49-55 29737325-13 2018 AZD6244 alone abolished phospho-ERK1/2 (pERK1/2) expression at 48 h, whereas vemurafenib alone downregulated pERK1/2 at 4-6 h, with rapid recovery of expression, reaching the highest level at 24-48 h. Combined treatment for 48 h completely inhibited pERK1/2 expression. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 32-38 29915160-0 2018 The Endosomal Protein CEMIP Links WNT Signaling to MEK1-ERK1/2 Activation in Selumetinib-Resistant Intestinal Organoids. AZD 6244 77-88 mitogen-activated protein kinase 3 Homo sapiens 56-62 30414267-12 2018 Selumetinib treatment had a synergistic effect with erythromycin to reduce the expression of p-MEK1 and p-ERK1, reduce cell proliferation, and increase cell apoptosis. AZD 6244 0-11 mitogen-activated protein kinase 3 Homo sapiens 106-110 29737325-17 2018 Combination treatment with vemurafenib and AZD6244 inhibited ERK signaling and caused cell cycle arrest, resulting in cell growth inhibition. AZD 6244 43-50 mitogen-activated protein kinase 3 Homo sapiens 61-64 27670699-6 2016 We show that inhibition of ERK1/2 activation using selumetinib efficiently inhibits the growth of lung SCC with TRA2B-DNAH5 fusion expression. AZD 6244 51-62 mitogen-activated protein kinase 3 Homo sapiens 27-33 28986121-4 2018 These death responses, however, were reverted to growth arrest responses upon titration of cellular phospho-ERK1/2 levels by the MEK1/2 inhibitor AZD6244. AZD 6244 146-153 mitogen-activated protein kinase 3 Homo sapiens 108-114 25857555-8 2015 Importantly, inhibition of ERK1/2 activation by PD0325901 (300 nM) or AZD6244 (5 or 10 microM) completely abolished the proliferative response. AZD 6244 70-77 mitogen-activated protein kinase 3 Homo sapiens 27-33 25959272-8 2015 Taken together, our data demonstrated that blockade of the EGFR might efficiently increase the antitumor activity of selumetinib in a subgroup of TNBC and that this phenomenon might be related to the effects of such combination on both ERK1/2 and AKT activation. AZD 6244 117-128 mitogen-activated protein kinase 3 Homo sapiens 236-242 25867065-7 2016 We found that both B-Raf (for example, PLX4032) and MEK inhibitors (for example, AZD6244 and PD0325901) effectively inhibited ERK1/2 phosphorylation and reduced DR5 levels in both human thyroid cancer and melanoma cells. AZD 6244 81-88 mitogen-activated protein kinase 3 Homo sapiens 126-132 24375836-10 2014 Downregulation of miR-92a by AZD6244 is mediated by the ERK1/2-AP1 signalling pathway. AZD 6244 29-36 mitogen-activated protein kinase 3 Homo sapiens 56-62 25379021-5 2014 Selumetinib inhibited phosphorylation of ERK1/2 and RSK and had no effect on AKT phosphorylation in both sensitive and resistant cells. AZD 6244 0-11 mitogen-activated protein kinase 3 Homo sapiens 41-47 24939055-8 2014 Western blot analysis and immunohistochemical staining revealed that AZD6244 alone reduced ERK1/2 phosphorylation, angiogenesis, and tumor cell proliferation. AZD 6244 69-76 mitogen-activated protein kinase 3 Homo sapiens 91-97 25624003-8 2015 We report here that both restoring the PGRN content, by suberoylanilide hydroxamic acid (SAHA) or chloroquine (CQ), as blocking ERK1/2 activation by selumetinib (AZD6244) or MEK162 (ARRY-162), normalized the CDK6/pRb pathway and the proliferative activity of PGRN deficient cells. AZD 6244 149-160 mitogen-activated protein kinase 3 Homo sapiens 128-134 25624003-8 2015 We report here that both restoring the PGRN content, by suberoylanilide hydroxamic acid (SAHA) or chloroquine (CQ), as blocking ERK1/2 activation by selumetinib (AZD6244) or MEK162 (ARRY-162), normalized the CDK6/pRb pathway and the proliferative activity of PGRN deficient cells. AZD 6244 162-169 mitogen-activated protein kinase 3 Homo sapiens 128-134 23234544-8 2013 Thus the combination of a BCL2 inhibitor and an ERK1/2 pathway inhibitor is synthetic lethal in ERK1/2-addicted tumour cells, delays the onset of acquired resistance and in some cases overcomes acquired resistance to selumetinib. AZD 6244 217-228 mitogen-activated protein kinase 3 Homo sapiens 48-54 23942066-5 2013 RESULTS: Selumetinib treatment induced tumour stasis and reduced ERK1/2 phosphorylation in both WM266.4 and Colo205 tumour xenografts. AZD 6244 9-20 mitogen-activated protein kinase 3 Homo sapiens 65-71 23255578-8 2013 Furthermore, AZD6244, a clinically relevant inhibitor of the ERK1/2 pathway, mitigated particle-induced inflammatory gene expression in osteoprogenitor cells and macrophages. AZD 6244 13-20 mitogen-activated protein kinase 3 Homo sapiens 61-67 23234544-1 2013 Tumour cells typically exhibit a G(1) cell cycle arrest in response to the MEK1/2 [mitogen-activated protein kinase/ERK (extracellular-signal-regulated kinase) kinase 1/2] inhibitor selumetinib, but do not die, and thus they acquire resistance. AZD 6244 182-193 mitogen-activated protein kinase 3 Homo sapiens 116-119 22260668-4 2012 Selumetinib-resistant cells were refractory to other MEK1/2 inhibitors in cell proliferation assays and exhibited a marked increase in MEK1/2 and ERK1/2 activity and cyclin D1 abundance when assessed in the absence of inhibitor. AZD 6244 0-11 mitogen-activated protein kinase 3 Homo sapiens 146-152 23362510-6 2012 Pharmacological blockade of ERK1/2 pathway with MEK1/2 inhibitors, U0126 and selumetinib (AZD6244) significantly attenuated the pro-apoptotic effects of field electric stimulation on the mutated LMNA iPSC-CMs. AZD 6244 77-88 mitogen-activated protein kinase 3 Homo sapiens 28-34 23362510-6 2012 Pharmacological blockade of ERK1/2 pathway with MEK1/2 inhibitors, U0126 and selumetinib (AZD6244) significantly attenuated the pro-apoptotic effects of field electric stimulation on the mutated LMNA iPSC-CMs. AZD 6244 90-97 mitogen-activated protein kinase 3 Homo sapiens 28-34 22821509-6 2012 Increased proliferation due to strong activation of extracellular-signal-regulated kinase 1/2 (ERK1/2) is caused by overexpression/activation of platelet-derived growth factor receptor-beta (PDGFR-beta) and ErbB2/3 which we successfully blocked with AZD6244, sorafenib, or lapatinib. AZD 6244 250-257 mitogen-activated protein kinase 3 Homo sapiens 95-101 22068161-6 2012 Selumetinib is an inhibitor of ERK1/2 signalling and has been given safely to human subjects in clinical trials for cancer. AZD 6244 0-11 mitogen-activated protein kinase 3 Homo sapiens 31-37 17699718-3 2007 AZD6244 (ARRY-142886) is a potent, selective, and ATP-uncompetitive inhibitor of MAPK/ERK kinase 1/2. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 81-85 21447798-3 2011 AZD6244-resistant derivatives were refractory to AZD6244-induced cell cycle arrest and death and exhibited a marked increase in ERK1/2 (extracellular signal-regulated kinases 1 and 2) pathway signaling and cyclin D1 abundance when assessed in the absence of inhibitor. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 128-134 21674991-4 2011 AZD6244-resistant derivatives were refractory to AZD6244-induced cell cycle arrest and death and exhibited a marked increase in ERK1/2 (extracellular signal-regulated kinases 1 and 2) pathway signaling and cyclin D1 abundance when assessed in the absence of inhibitor. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 128-134 21899882-7 2011 AZD6244 treatment, a potent inhibitor of the ERK pathway, attenuated particle mediated inflammatory osteolysis both in vivo and in vitro. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 45-48 20806365-9 2010 Pharmacodynamic studies indicated at this dose and schedule AZD6244 completely inhibited ERK1/2 phosphorylation. AZD 6244 60-67 mitogen-activated protein kinase 3 Homo sapiens 89-95 19804833-0 2010 Targeting ERK1/2 activation and proliferation in human primary schwannoma cells with MEK1/2 inhibitor AZD6244. AZD 6244 102-109 mitogen-activated protein kinase 3 Homo sapiens 10-16 19804833-5 2010 Here, we targeted MEK1/2 known as a convergence point for multiple cascades towards ERK1/2 activation and cell proliferation, using MEK1/2 inhibitor AZD6244 (ARRY-142886; Astra Zeneca). AZD 6244 149-156 mitogen-activated protein kinase 3 Homo sapiens 84-90 19804833-6 2010 We show that AZD6244 at low concentration completely abolished platelet-derived growth factor-DD-mediated ERK1/2 activation and cell proliferation in human primary schwannoma cells. AZD 6244 13-20 mitogen-activated protein kinase 3 Homo sapiens 106-112 19637312-0 2009 Intrinsic resistance to the MEK1/2 inhibitor AZD6244 (ARRY-142886) is associated with weak ERK1/2 signalling and/or strong PI3K signalling in colorectal cancer cell lines. AZD 6244 45-52 mitogen-activated protein kinase 3 Homo sapiens 91-97 19637312-2 2009 The MEK1/2-selective inhibitor, AZD6244 (ARRY-142886), blocks ERK1/2 activation and is currently undergoing clinical evaluation. AZD 6244 32-39 mitogen-activated protein kinase 3 Homo sapiens 62-68 19637312-2 2009 The MEK1/2-selective inhibitor, AZD6244 (ARRY-142886), blocks ERK1/2 activation and is currently undergoing clinical evaluation. AZD 6244 41-52 mitogen-activated protein kinase 3 Homo sapiens 62-68 19637312-7 2009 In cell lines with coincident ERK1/2 and PKB activation, sensitivity to AZD6244 could be re-imposed by any of the 3 distinct PI3K/mTOR inhibitors. AZD 6244 72-79 mitogen-activated protein kinase 3 Homo sapiens 30-36 19637312-9 2009 Sensitivity to MEK1/2 inhibition correlates with a biochemical signature; those cells with high ERK1/2 activity (whether mutant for BRAF or KRAS) evolve a dependency upon that pathway and tend to be sensitive to AZD6244 but this can be offset by high PI3K-dependent signalling. AZD 6244 212-219 mitogen-activated protein kinase 3 Homo sapiens 96-102 19366835-0 2009 In vitro and in vivo radiosensitization with AZD6244 (ARRY-142886), an inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase 1/2 kinase. AZD 6244 45-52 mitogen-activated protein kinase 3 Homo sapiens 117-158 17510321-3 2007 AZD6244 blocks constitutive and cytokine-stimulated ERK1/2 phosphorylation and inhibits proliferation and survival of human MM cell lines and patient MM cells, regardless of sensitivity to conventional chemotherapy. AZD 6244 0-7 mitogen-activated protein kinase 3 Homo sapiens 52-58 17699718-3 2007 AZD6244 (ARRY-142886) is a potent, selective, and ATP-uncompetitive inhibitor of MAPK/ERK kinase 1/2. AZD 6244 9-20 mitogen-activated protein kinase 3 Homo sapiens 81-85 17699718-6 2007 Chronic dosing with 25 mg/kg AZD6244 bd resulted in suppression of growth of Colo-205, Calu-6, and SW-620 xenografts, whereas an acute dose resulted in significant inhibition of ERK1/2 phosphorylation. AZD 6244 29-36 mitogen-activated protein kinase 3 Homo sapiens 178-184