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Details on Person Anti-MET small tyrosine kinase inhibitors bind MET
Class:Id Reaction:9735946
_displayName Anti-MET small tyrosine kinase inhibitors bind MET
_doRelease TRUE
_timestamp 2021-08-10 14:23:21
authored [InstanceEdit:9734140] Orlic-Milacic, Marija, 2021-06-15
compartment [Compartment:876] plasma membrane [Compartment:70101] cytosol
created [InstanceEdit:9735948] Orlic-Milacic, Marija, 2021-07-06
edited [InstanceEdit:9750145] Orlic-Milacic, Marija, 2021-08-10
input [Complex:6806956] HGF:MET dimer [plasma membrane] [Homo sapiens] [CandidateSet:9735962] Anti-MET TKIs [cytosol] [CandidateSet:9735962] Anti-MET TKIs [cytosol]
isChimeric FALSE
literatureReference [LiteratureReference:9736224] ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity [LiteratureReference:9736234] Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET [LiteratureReference:9736017] Tivantinib, A c-Met Inhibitor in Clinical Trials, Is Susceptible to ABCG2-Mediated Drug Resistance [LiteratureReference:9736183] Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth [LiteratureReference:9736177] Cabozantinib suppresses tumor growth and metastasis in hepatocellular carcinoma by a dual blockade of VEGFR2 and MET [LiteratureReference:9736184] Modulating the function of ATP-binding cassette subfamily G member 2 (ABCG2) with inhibitor cabozantinib [LiteratureReference:9736137] Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases [LiteratureReference:9736185] Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks [LiteratureReference:9736276] Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring MET Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models [LiteratureReference:9736134] A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo [LiteratureReference:9736285] SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo [LiteratureReference:9736172] A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase [LiteratureReference:9736281] In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models [LiteratureReference:9736044] Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily [LiteratureReference:9736030] Synergistic activities of MET/RON inhibitor BMS-777607 and mTOR inhibitor AZD8055 to polyploid cells derived from pancreatic cancer and cancer stem cells [LiteratureReference:9736216] A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3 [LiteratureReference:9736055] Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer [LiteratureReference:9736271] Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models [LiteratureReference:9736129] Synthesis, Evaluation, and Mechanism Study of New Tepotinib Derivatives as Antiproliferative Agents [LiteratureReference:9736096] OMO-1 reduces progression and enhances cisplatin efficacy in a 4T1-based non-c-MET addicted intraductal mouse model for triple-negative breast cancer [LiteratureReference:9736261] E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models [LiteratureReference:9736039] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor [LiteratureReference:9736273] An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms [LiteratureReference:9736260] A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors [LiteratureReference:9734139] Known and novel roles of the MET oncogene in cancer: a coherent approach to targeted therapy [URL:9750163] https://cancerres.aacrjournals.org/content/78/13_Supplement/4791 [LiteratureReference:9750173] Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines
modified [InstanceEdit:9735980] Orlic-Milacic, Marija, 2021-07-06 [InstanceEdit:9736289] Orlic-Milacic, Marija, 2021-07-06 [InstanceEdit:9736295] Orlic-Milacic, Marija, 2021-07-06 [InstanceEdit:9736301] Orlic-Milacic, Marija, 2021-07-06 [InstanceEdit:9750145] Orlic-Milacic, Marija, 2021-08-10 [InstanceEdit:9750148] Orlic-Milacic, Marija, 2021-08-10 [InstanceEdit:9750149] Orlic-Milacic, Marija, 2021-08-10 [InstanceEdit:9750164] Orlic-Milacic, Marija, 2021-08-10 [InstanceEdit:9750178] Orlic-Milacic, Marija, 2021-08-10 [InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
name Anti-MET small tyrosine kinase inhibitors bind MET
output [Complex:9735965] HGF:MET dimer:TKIs [plasma membrane] [Homo sapiens]
releaseDate 2021-09-15
reviewed [InstanceEdit:9750147] Kadambat Nair, Sisira, 2021-08-05
reviewStatus [ReviewStatus:9821382] five stars
species [Species:48887] Homo sapiens
stableIdentifier [StableIdentifier:9735949] R-HSA-9735946.2
summation [Summation:9735947] Several tyrosine kinase inhibitors (TKIs) have MET as their ...
(hasEvent) [Pathway:9734091] Drug-mediated inhibition of MET activation [Homo sapiens]
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