FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2887749223> ?p ?o ?g. }

• W2887749223 endingPage "4857" @default.
• W2887749223 startingPage "4857" @default.
• W2887749223 abstract "Abstract Protein arginine methyltransferase 5 (PRMT5) is the primary type II arginine methyltransferase responsible for symmetric dimethylation of protein arginine residues. PRMT5 utilizes S-adenosylmethionine (SAM) to methylate a number of cytoplasmic and nuclear substrates that are involved in tumorigenesis. A number of these substrates affect a variety of biologic functions including RNA splicing, transcriptional regulation and translation, all of which are dysregulated in cancer. The discovery of adenosine as an efficient inhibitor of PRMT5 catalyzed a medicinal chemistry effort aimed at nucleoside optimization. Protein structure-based and ligand property-based design were combined to deliver molecules with desirable potency, selectivity and ADME properties. Here we will describe a series of deazapurine nucleoside analogues that culminate in the identification of PF-06855800, a SAM competitive PRMT5 inhibitor with antiproliferative activity in both in vitro and in vivo models. Citation Format: Indrawan J. Mcalpine, John Tatlock, Joseph Billitti, John Braganza, Alexei Brooun, Deng Ya-Li, Brad Hirakawa, Kristen Jensen-Pergakes, Robert Kumpf, Wei Liu, Karen Maegley, Michele McTigue, Ryan Patman, Eugene Rui, Stephanie Scales, Noah Spiegel, Michelle Tran-Dubé, Fen Wang, Zhenxiong Wang, Shinji Yamazaki, Tao Zhang, Martin Wythes. Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 4857." @default.
• W2887749223 created "2018-08-22" @default.
• W2887749223 creator A5003348856 @default.
• W2887749223 creator A5006518535 @default.
• W2887749223 creator A5010968025 @default.
• W2887749223 creator A5018283590 @default.
• W2887749223 creator A5023836589 @default.
• W2887749223 creator A5031081898 @default.
• W2887749223 creator A5035701638 @default.
• W2887749223 creator A5039754491 @default.
• W2887749223 creator A5045935502 @default.
• W2887749223 creator A5049285430 @default.
• W2887749223 creator A5063500857 @default.
• W2887749223 creator A5064787088 @default.
• W2887749223 creator A5065104999 @default.
• W2887749223 creator A5069163138 @default.
• W2887749223 creator A5071037763 @default.
• W2887749223 creator A5071409456 @default.
• W2887749223 creator A5074538933 @default.
• W2887749223 creator A5074892381 @default.
• W2887749223 creator A5075130252 @default.
• W2887749223 creator A5079660804 @default.
• W2887749223 creator A5084016503 @default.
• W2887749223 creator A5089813007 @default.
• W2887749223 date "2018-07-01" @default.
• W2887749223 modified "2023-10-17" @default.
• W2887749223 title "Abstract 4857: Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity" @default.
• W2887749223 doi "https://doi.org/10.1158/1538-7445.am2018-4857" @default.
• W2887749223 hasPublicationYear "2018" @default.
• W2887749223 type Work @default.
• W2887749223 sameAs 2887749223 @default.
• W2887749223 citedByCount "4" @default.
• W2887749223 countsByYear W28877492232019 @default.
• W2887749223 countsByYear W28877492232020 @default.
• W2887749223 countsByYear W28877492232023 @default.
• W2887749223 crossrefType "journal-article" @default.
• W2887749223 hasAuthorship W2887749223A5003348856 @default.
• W2887749223 hasAuthorship W2887749223A5006518535 @default.
• W2887749223 hasAuthorship W2887749223A5010968025 @default.
• W2887749223 hasAuthorship W2887749223A5018283590 @default.
• W2887749223 hasAuthorship W2887749223A5023836589 @default.
• W2887749223 hasAuthorship W2887749223A5031081898 @default.
• W2887749223 hasAuthorship W2887749223A5035701638 @default.
• W2887749223 hasAuthorship W2887749223A5039754491 @default.
• W2887749223 hasAuthorship W2887749223A5045935502 @default.
• W2887749223 hasAuthorship W2887749223A5049285430 @default.
• W2887749223 hasAuthorship W2887749223A5063500857 @default.
• W2887749223 hasAuthorship W2887749223A5064787088 @default.
• W2887749223 hasAuthorship W2887749223A5065104999 @default.
• W2887749223 hasAuthorship W2887749223A5069163138 @default.
• W2887749223 hasAuthorship W2887749223A5071037763 @default.
• W2887749223 hasAuthorship W2887749223A5071409456 @default.
• W2887749223 hasAuthorship W2887749223A5074538933 @default.
• W2887749223 hasAuthorship W2887749223A5074892381 @default.
• W2887749223 hasAuthorship W2887749223A5075130252 @default.
• W2887749223 hasAuthorship W2887749223A5079660804 @default.
• W2887749223 hasAuthorship W2887749223A5084016503 @default.
• W2887749223 hasAuthorship W2887749223A5089813007 @default.
• W2887749223 hasConcept C104317684 @default.
• W2887749223 hasConcept C111819275 @default.
• W2887749223 hasConcept C121608353 @default.
• W2887749223 hasConcept C185592680 @default.
• W2887749223 hasConcept C202751555 @default.
• W2887749223 hasConcept C2777468819 @default.
• W2887749223 hasConcept C33288867 @default.
• W2887749223 hasConcept C515207424 @default.
• W2887749223 hasConcept C54355233 @default.
• W2887749223 hasConcept C54458228 @default.
• W2887749223 hasConcept C55493867 @default.
• W2887749223 hasConcept C67705224 @default.
• W2887749223 hasConcept C69366308 @default.
• W2887749223 hasConcept C71240020 @default.
• W2887749223 hasConcept C86803240 @default.
• W2887749223 hasConcept C91965660 @default.
• W2887749223 hasConceptScore W2887749223C104317684 @default.
• W2887749223 hasConceptScore W2887749223C111819275 @default.
• W2887749223 hasConceptScore W2887749223C121608353 @default.
• W2887749223 hasConceptScore W2887749223C185592680 @default.
• W2887749223 hasConceptScore W2887749223C202751555 @default.
• W2887749223 hasConceptScore W2887749223C2777468819 @default.
• W2887749223 hasConceptScore W2887749223C33288867 @default.
• W2887749223 hasConceptScore W2887749223C515207424 @default.
• W2887749223 hasConceptScore W2887749223C54355233 @default.
• W2887749223 hasConceptScore W2887749223C54458228 @default.
• W2887749223 hasConceptScore W2887749223C55493867 @default.
• W2887749223 hasConceptScore W2887749223C67705224 @default.
• W2887749223 hasConceptScore W2887749223C69366308 @default.
• W2887749223 hasConceptScore W2887749223C71240020 @default.
• W2887749223 hasConceptScore W2887749223C86803240 @default.
• W2887749223 hasConceptScore W2887749223C91965660 @default.
• W2887749223 hasIssue "13_Supplement" @default.
• W2887749223 hasLocation W28877492231 @default.
• W2887749223 hasOpenAccess W2887749223 @default.
• W2887749223 hasPrimaryLocation W28877492231 @default.
• W2887749223 hasRelatedWork W2032623135 @default.
• W2887749223 hasRelatedWork W2040733421 @default.
• W2887749223 hasRelatedWork W2063681641 @default.
• W2887749223 hasRelatedWork W2123306028 @default.

• next