FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2012169430> ?p ?o ?g. }

• W2012169430 endingPage "20676" @default.
• W2012169430 startingPage "20666" @default.
• W2012169430 abstract "A number of human malignancies exhibit sustained stimulation, mutation, or gene amplification of the receptor tyrosine kinase human mesenchymal-epithelial transition factor (c-Met). ARQ 197 is a clinically advanced, selective, orally bioavailable, and well tolerated c-Met inhibitor, currently in Phase 3 clinical testing in non-small cell lung cancer patients. Herein, we describe the molecular and structural basis by which ARQ 197 selectively targets c-Met. Through our analysis we reveal a previously undisclosed, novel inhibitory mechanism that utilizes distinct regulatory elements of the c-Met kinase. The structure of ARQ 197 in complex with the c-Met kinase domain shows that the inhibitor binds a conformation that is distinct from published kinase structures. ARQ 197 inhibits c-Met autophosphorylation and is highly selective for the inactive or unphosphorylated form of c-Met. Through our analysis of the interplay between the regulatory and catalytic residues of c-Met, and by comparison between the autoinhibited canonical conformation of c-Met bound by ARQ 197 to previously described kinase domains of type III receptor tyrosine kinases, we believe this to be the basis of a powerful new in silico approach for the design of similar inhibitors for other protein kinases of therapeutic interest." @default.
• W2012169430 created "2016-06-24" @default.
• W2012169430 creator A5007582656 @default.
• W2012169430 creator A5029374868 @default.
• W2012169430 creator A5041253361 @default.
• W2012169430 creator A5053232883 @default.
• W2012169430 creator A5057399487 @default.
• W2012169430 creator A5065252606 @default.
• W2012169430 date "2011-06-01" @default.
• W2012169430 modified "2023-09-27" @default.
• W2012169430 title "Discovery of a Novel Mode of Protein Kinase Inhibition Characterized by the Mechanism of Inhibition of Human Mesenchymal-epithelial Transition Factor (c-Met) Protein Autophosphorylation by ARQ 197" @default.
• W2012169430 cites W1969507272 @default.
• W2012169430 cites W1969672293 @default.
• W2012169430 cites W1977244487 @default.
• W2012169430 cites W1978329718 @default.
• W2012169430 cites W1980785869 @default.
• W2012169430 cites W1983523339 @default.
• W2012169430 cites W1986232164 @default.
• W2012169430 cites W1987789520 @default.
• W2012169430 cites W1992031126 @default.
• W2012169430 cites W1998971866 @default.
• W2012169430 cites W2000390423 @default.
• W2012169430 cites W2009222632 @default.
• W2012169430 cites W2018656850 @default.
• W2012169430 cites W2024403886 @default.
• W2012169430 cites W2027161653 @default.
• W2012169430 cites W2031588228 @default.
• W2012169430 cites W2037147205 @default.
• W2012169430 cites W2040840060 @default.
• W2012169430 cites W2041415161 @default.
• W2012169430 cites W2047613898 @default.
• W2012169430 cites W2049507332 @default.
• W2012169430 cites W2052092007 @default.
• W2012169430 cites W2055453661 @default.
• W2012169430 cites W2056163848 @default.
• W2012169430 cites W2057069307 @default.
• W2012169430 cites W2071500926 @default.
• W2012169430 cites W2073597573 @default.
• W2012169430 cites W2080251114 @default.
• W2012169430 cites W2092817365 @default.
• W2012169430 cites W2096844786 @default.
• W2012169430 cites W2125519805 @default.
• W2012169430 cites W2138896702 @default.
• W2012169430 cites W2139073495 @default.
• W2012169430 cites W2170129858 @default.
• W2012169430 cites W2171883378 @default.
• W2012169430 cites W4245967957 @default.
• W2012169430 doi "https://doi.org/10.1074/jbc.m110.213801" @default.
• W2012169430 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3121448" @default.
• W2012169430 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21454604" @default.
• W2012169430 hasPublicationYear "2011" @default.
• W2012169430 type Work @default.
• W2012169430 sameAs 2012169430 @default.
• W2012169430 citedByCount "122" @default.
• W2012169430 countsByYear W20121694302012 @default.
• W2012169430 countsByYear W20121694302013 @default.
• W2012169430 countsByYear W20121694302014 @default.
• W2012169430 countsByYear W20121694302015 @default.
• W2012169430 countsByYear W20121694302016 @default.
• W2012169430 countsByYear W20121694302017 @default.
• W2012169430 countsByYear W20121694302018 @default.
• W2012169430 countsByYear W20121694302019 @default.
• W2012169430 countsByYear W20121694302020 @default.
• W2012169430 countsByYear W20121694302021 @default.
• W2012169430 countsByYear W20121694302022 @default.
• W2012169430 countsByYear W20121694302023 @default.
• W2012169430 crossrefType "journal-article" @default.
• W2012169430 hasAuthorship W2012169430A5007582656 @default.
• W2012169430 hasAuthorship W2012169430A5029374868 @default.
• W2012169430 hasAuthorship W2012169430A5041253361 @default.
• W2012169430 hasAuthorship W2012169430A5053232883 @default.
• W2012169430 hasAuthorship W2012169430A5057399487 @default.
• W2012169430 hasAuthorship W2012169430A5065252606 @default.
• W2012169430 hasBestOaLocation W20121694301 @default.
• W2012169430 hasConcept C101544691 @default.
• W2012169430 hasConcept C150109051 @default.
• W2012169430 hasConcept C184235292 @default.
• W2012169430 hasConcept C185592680 @default.
• W2012169430 hasConcept C42362537 @default.
• W2012169430 hasConcept C502942594 @default.
• W2012169430 hasConcept C55493867 @default.
• W2012169430 hasConcept C62478195 @default.
• W2012169430 hasConcept C86803240 @default.
• W2012169430 hasConcept C95444343 @default.
• W2012169430 hasConcept C97029542 @default.
• W2012169430 hasConceptScore W2012169430C101544691 @default.
• W2012169430 hasConceptScore W2012169430C150109051 @default.
• W2012169430 hasConceptScore W2012169430C184235292 @default.
• W2012169430 hasConceptScore W2012169430C185592680 @default.
• W2012169430 hasConceptScore W2012169430C42362537 @default.
• W2012169430 hasConceptScore W2012169430C502942594 @default.
• W2012169430 hasConceptScore W2012169430C55493867 @default.
• W2012169430 hasConceptScore W2012169430C62478195 @default.
• W2012169430 hasConceptScore W2012169430C86803240 @default.
• W2012169430 hasConceptScore W2012169430C95444343 @default.
• W2012169430 hasConceptScore W2012169430C97029542 @default.
• W2012169430 hasIssue "23" @default.
• W2012169430 hasLocation W20121694301 @default.

• next