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Details on Person PDGF dimer binds two receptors simultaneously
Class:Id BlackBoxEvent:186773
_displayName PDGF dimer binds two receptors simultaneously
_doRelease TRUE
_timestamp 2020-01-13 15:28:45
authored [InstanceEdit:382627] Garapati, P V, Jassal, B, 2008-11-24 10:14:27
compartment [Compartment:876] plasma membrane
created [InstanceEdit:186802] Jassal, B, 2006-08-15 13:51:10
edited [InstanceEdit:382627] Garapati, P V, Jassal, B, 2008-11-24 10:14:27
input [DefinedSet:186792] PDGFRA, PDGFRB [plasma membrane] [Homo sapiens] [DefinedSet:186792] PDGFRA, PDGFRB [plasma membrane] [Homo sapiens] [DefinedSet:380760] Active PDGF dimers (AA, AB, BB) [extracellular region] [Homo sapiens]
literatureReference [LiteratureReference:380735] Signal transduction via platelet-derived growth factor receptors [LiteratureReference:9673583] The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders [LiteratureReference:9674057] Pazopanib inhibits the activation of PDGFRβ-expressing astrocytes in the brain metastatic microenvironment of breast cancer cells [LiteratureReference:9674032] Inhibition of the platelet-derived growth factor receptor beta (PDGFRB) using gene silencing, crenolanib besylate, or imatinib mesylate hampers the malignant phenotype of mesothelioma cell lines [LiteratureReference:9674068] The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations [LiteratureReference:9674023] Crenolanib, a PDGFR inhibitor, suppresses lung cancer cell proliferation and inhibits tumor growth in vivo [LiteratureReference:9674200] Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays [LiteratureReference:9674255] Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib) [LiteratureReference:2077545] E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition [LiteratureReference:9674254] Inhibition of PDGF, TGF-β, and Abl signaling and reduction of liver fibrosis by the small molecule Bcr-Abl tyrosine kinase antagonist Nilotinib [LiteratureReference:9674181] BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy [LiteratureReference:9674295] Triple Angiokinase Inhibitor Nintedanib Directly Inhibits Tumor Cell Growth and Induces Tumor Shrinkage via Blocking Oncogenic Receptor Tyrosine Kinases [LiteratureReference:9674174] BAY 43-9006: preclinical data [LiteratureReference:9674258] Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment [LiteratureReference:9674233] In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship [LiteratureReference:9674288] Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor [LiteratureReference:9673974] Stromal platelet-derived growth factor receptor α (PDGFRα) provides a therapeutic target independent of tumor cell PDGFRα expression in lung cancer xenografts [LiteratureReference:9673955] Autocrine activation of PDGFRalpha promotes the progression of ovarian cancer [LiteratureReference:9674003] Targeting the {alpha} receptor for platelet-derived growth factor as a primary or combination therapy in a preclinical model of prostate cancer skeletal metastasis [LiteratureReference:9673963] Platelet-derived growth factor receptor-alpha: a novel therapeutic target in human hepatocellular cancer
modified [InstanceEdit:194433] Schmidt, EE, 2007-03-13 12:36:50 [InstanceEdit:380785] Garapati, P V, 2008-11-14 10:50:39 [InstanceEdit:382621] Garapati, P V, 2008-11-24 00:31:49 [InstanceEdit:382629] Garapati, P V, 2008-11-24 10:23:46 [InstanceEdit:389097] Garapati, P V, 2008-12-19 14:12:26 [InstanceEdit:392249] Garapati, P V, 2009-03-01 16:14:35 [InstanceEdit:9031949] Orlic-Milacic, Marija, 2017-12-04 [InstanceEdit:9674162] Rothfels, Karen, 2020-01-10 [InstanceEdit:9674434] Rothfels, Karen, 2020-01-13 [InstanceEdit:9674473] Rothfels, Karen, 2020-01-13 [InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
name PDGF dimer binds two receptors simultaneously
output [Complex:186766] PDGF:PDGF receptor dimer [plasma membrane] [Homo sapiens]
precedingEvent
regulatedBy [NegativeRegulation:9674159] Negative regulation by 'PDGFR:type II PDGFR-binding TKIs [plasma membrane]' [NegativeRegulation:9674160] Negative regulation by 'PDGFRA:olaratumab [plasma membrane]'
releaseDate 2009-04-01
reviewed [InstanceEdit:382617] Heldin, CH, 2008-11-23 19:29:34
reviewStatus [ReviewStatus:9821382] five stars
species [Species:48887] Homo sapiens
stableIdentifier [StableIdentifier:398336] R-HSA-186773.4
summation [Summation:186777] PDGF dimer binds two receptors simultaneously. The receptors...
(hasEvent) [Pathway:186797] Signaling by PDGF [Homo sapiens]
(normalReaction) [Reaction:9672168] Ligand-independent dimerization of PDGFR mutants [Homo sapiens]
(precedingEvent) [Reaction:186786] Autophosphorylation of PDGF beta receptors [Homo sapiens] [Reaction:389083] Autophosphorylation of PDGF alpha receptors [Homo sapiens] [Reaction:389086] Autophosphorylation of PDGF alpha/beta receptors [Homo sapiens]
(updatedInstance) [_UpdateTracker:9777393] Update Tracker - [BlackBoxEvent:186773] PDGF dimer binds two receptors simultaneously - v72:[addLiteratureReference, addRegulator, modifyText]
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