FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1574657342> ?p ?o ?g. }

• W1574657342 endingPage "1738" @default.
• W1574657342 startingPage "1738" @default.
• W1574657342 abstract "Abstract The fibroblast growth factor (FGF) signaling axis is increasingly implicated in tumorigenesis and chemoresistance. Alterations in FGFR family members including focal amplification of FGF receptor 1 (FGFR1), mutations in FGFR 2, 3 and 4, translocations involving FGFR 2 and FGFR3, as well as amplification or transcriptional upregulation of various ligand family members have been associated with tumor growth and survival, suggesting that FGFR inhibitors may be a viable therapeutic option in subsets of various disease settings. A number of agents targeting the FGF signaling axis including small-molecule FGFR targeted agents, with diverse kinase inhibitory and pharmacological profiles, are currently in clinical development. JNJ-42756493 (first disclosure of the structure) has a pharmacological profile that is differentiated from other agents in this class currently under investigation. JNJ-42756493 displays single digit nanomolar FGFR (1, 2, 3 4) tyrosine kinase inhibitory activity. JNJ-42756493 inhibited recombinant FGFR kinase activity in vitro and suppressed FGFR signaling and growth in engineered cell lines and tumor cell lines dependent upon deregulated FGFR expression. JNJ-42756493 demonstrated highly specific tumor inhibitory effects in FGFR1-4 dependent cell lines, in vitro cell lines based xenografts and direct patient derived xenografts, with no discernible activity in models that were not dependent on FGFR signaling. JNJ-42756493 showed favorable drug like properties and displayed a high distribution to lung, liver and kidney tissue. JNJ-42756493 was well tolerated at efficacious doses and resulted in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components. Data presented here highlights JNJ-42756493 as a novel, highly potent and selective small-molecule inhibitor of all four known active FGFR kinase family members with potent antitumor activity against FGFR-dependent tumor models. These data, together with emerging observations from our ongoing Phase 1 clinical trial, position JNJ-42756493 as a differentiated FGFR 1, 2, 3 and 4 kinase inhibitor and support its continued clinical development in lung cancer and other malignancies associated with aberrant FGFR signaling. Citation Format: Timothy Perera, Eleanora Jovcheva, Jorge Vialard, Tinne Verhulst, Norbert Esser, Berthold Wroblowski, Ron Gilissen, Eddy Freyne, Peter King, Suso Platero, Olivier Querolle, Laurence Mevellec, Christopher Murray, Lynsey Fazal, Gordon Saxty, George Ward, Matthew Squires, Neil Thompson, David Newell, Patrick Angibaud. JNJ-42756493 is an inhibitor of FGFR-1, 2, 3 and 4 with nanomolar affinity for targeted therapy. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 1738. doi:10.1158/1538-7445.AM2014-1738" @default.
• W1574657342 created "2016-06-24" @default.
• W1574657342 creator A5000966714 @default.
• W1574657342 creator A5002070840 @default.
• W1574657342 creator A5007415160 @default.
• W1574657342 creator A5009105578 @default.
• W1574657342 creator A5014820758 @default.
• W1574657342 creator A5018819088 @default.
• W1574657342 creator A5019627613 @default.
• W1574657342 creator A5020501777 @default.
• W1574657342 creator A5030398228 @default.
• W1574657342 creator A5037778274 @default.
• W1574657342 creator A5041036069 @default.
• W1574657342 creator A5043267361 @default.
• W1574657342 creator A5044403338 @default.
• W1574657342 creator A5060008277 @default.
• W1574657342 creator A5060448906 @default.
• W1574657342 creator A5064747201 @default.
• W1574657342 creator A5066166158 @default.
• W1574657342 creator A5069716647 @default.
• W1574657342 creator A5071359664 @default.
• W1574657342 creator A5079588784 @default.
• W1574657342 date "2014-10-01" @default.
• W1574657342 modified "2023-09-24" @default.
• W1574657342 title "Abstract 1738: JNJ-42756493 is an inhibitor of FGFR-1, 2, 3and4 with nanomolar affinity for targeted therapy" @default.
• W1574657342 doi "https://doi.org/10.1158/1538-7445.am2014-1738" @default.
• W1574657342 hasPublicationYear "2014" @default.
• W1574657342 type Work @default.
• W1574657342 sameAs 1574657342 @default.
• W1574657342 citedByCount "7" @default.
• W1574657342 countsByYear W15746573422014 @default.
• W1574657342 countsByYear W15746573422016 @default.
• W1574657342 countsByYear W15746573422017 @default.
• W1574657342 countsByYear W15746573422023 @default.
• W1574657342 crossrefType "journal-article" @default.
• W1574657342 hasAuthorship W1574657342A5000966714 @default.
• W1574657342 hasAuthorship W1574657342A5002070840 @default.
• W1574657342 hasAuthorship W1574657342A5007415160 @default.
• W1574657342 hasAuthorship W1574657342A5009105578 @default.
• W1574657342 hasAuthorship W1574657342A5014820758 @default.
• W1574657342 hasAuthorship W1574657342A5018819088 @default.
• W1574657342 hasAuthorship W1574657342A5019627613 @default.
• W1574657342 hasAuthorship W1574657342A5020501777 @default.
• W1574657342 hasAuthorship W1574657342A5030398228 @default.
• W1574657342 hasAuthorship W1574657342A5037778274 @default.
• W1574657342 hasAuthorship W1574657342A5041036069 @default.
• W1574657342 hasAuthorship W1574657342A5043267361 @default.
• W1574657342 hasAuthorship W1574657342A5044403338 @default.
• W1574657342 hasAuthorship W1574657342A5060008277 @default.
• W1574657342 hasAuthorship W1574657342A5060448906 @default.
• W1574657342 hasAuthorship W1574657342A5064747201 @default.
• W1574657342 hasAuthorship W1574657342A5066166158 @default.
• W1574657342 hasAuthorship W1574657342A5069716647 @default.
• W1574657342 hasAuthorship W1574657342A5071359664 @default.
• W1574657342 hasAuthorship W1574657342A5079588784 @default.
• W1574657342 hasConcept C101544691 @default.
• W1574657342 hasConcept C121608353 @default.
• W1574657342 hasConcept C170493617 @default.
• W1574657342 hasConcept C184235292 @default.
• W1574657342 hasConcept C2778820342 @default.
• W1574657342 hasConcept C42362537 @default.
• W1574657342 hasConcept C49418065 @default.
• W1574657342 hasConcept C502942594 @default.
• W1574657342 hasConcept C54355233 @default.
• W1574657342 hasConcept C55493867 @default.
• W1574657342 hasConcept C62478195 @default.
• W1574657342 hasConcept C74373430 @default.
• W1574657342 hasConcept C82867764 @default.
• W1574657342 hasConcept C86803240 @default.
• W1574657342 hasConcept C95444343 @default.
• W1574657342 hasConceptScore W1574657342C101544691 @default.
• W1574657342 hasConceptScore W1574657342C121608353 @default.
• W1574657342 hasConceptScore W1574657342C170493617 @default.
• W1574657342 hasConceptScore W1574657342C184235292 @default.
• W1574657342 hasConceptScore W1574657342C2778820342 @default.
• W1574657342 hasConceptScore W1574657342C42362537 @default.
• W1574657342 hasConceptScore W1574657342C49418065 @default.
• W1574657342 hasConceptScore W1574657342C502942594 @default.
• W1574657342 hasConceptScore W1574657342C54355233 @default.
• W1574657342 hasConceptScore W1574657342C55493867 @default.
• W1574657342 hasConceptScore W1574657342C62478195 @default.
• W1574657342 hasConceptScore W1574657342C74373430 @default.
• W1574657342 hasConceptScore W1574657342C82867764 @default.
• W1574657342 hasConceptScore W1574657342C86803240 @default.
• W1574657342 hasConceptScore W1574657342C95444343 @default.
• W1574657342 hasIssue "19_Supplement" @default.
• W1574657342 hasLocation W15746573421 @default.
• W1574657342 hasOpenAccess W1574657342 @default.
• W1574657342 hasPrimaryLocation W15746573421 @default.
• W1574657342 hasRelatedWork W1510758377 @default.
• W1574657342 hasRelatedWork W1990233859 @default.
• W1574657342 hasRelatedWork W2019711215 @default.
• W1574657342 hasRelatedWork W2060563871 @default.
• W1574657342 hasRelatedWork W2148433207 @default.
• W1574657342 hasRelatedWork W2180677021 @default.
• W1574657342 hasRelatedWork W2331750244 @default.
• W1574657342 hasRelatedWork W2402660289 @default.
• W1574657342 hasRelatedWork W2790607578 @default.

• next