FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2064235684> ?p ?o ?g. }

• W2064235684 endingPage "9919" @default.
• W2064235684 startingPage "9897" @default.
• W2064235684 abstract "A series of dimeric compounds based on the AVPI motif of Smac were designed and prepared as antagonists of the inhibitor of apoptosis proteins (IAPs). Optimization of cellular potency, physical properties, and pharmacokinetic parameters led to the identification of compound 14 (AZD5582), which binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively). This compound causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, 14 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with 14 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors. As a result of its in vitro and in vivo profile, 14 was nominated as a candidate for clinical development." @default.
• W2064235684 created "2016-06-24" @default.
• W2064235684 creator A5001077804 @default.
• W2064235684 creator A5001466285 @default.
• W2064235684 creator A5003196865 @default.
• W2064235684 creator A5003991876 @default.
• W2064235684 creator A5015943859 @default.
• W2064235684 creator A5018575107 @default.
• W2064235684 creator A5019269693 @default.
• W2064235684 creator A5021755913 @default.
• W2064235684 creator A5024517878 @default.
• W2064235684 creator A5028512226 @default.
• W2064235684 creator A5034508167 @default.
• W2064235684 creator A5037050717 @default.
• W2064235684 creator A5037497696 @default.
• W2064235684 creator A5049852492 @default.
• W2064235684 creator A5052925180 @default.
• W2064235684 creator A5054565788 @default.
• W2064235684 creator A5066063012 @default.
• W2064235684 creator A5066691449 @default.
• W2064235684 creator A5068941202 @default.
• W2064235684 creator A5070605323 @default.
• W2064235684 creator A5076814949 @default.
• W2064235684 creator A5085296684 @default.
• W2064235684 date "2013-12-13" @default.
• W2064235684 modified "2023-10-15" @default.
• W2064235684 title "Discovery of a Novel Class of Dimeric Smac Mimetics as Potent IAP Antagonists Resulting in a Clinical Candidate for the Treatment of Cancer (AZD5582)" @default.
• W2064235684 cites W1203651314 @default.
• W2064235684 cites W1492587973 @default.
• W2064235684 cites W1498354276 @default.
• W2064235684 cites W1915374685 @default.
• W2064235684 cites W1966409661 @default.
• W2064235684 cites W1966472904 @default.
• W2064235684 cites W1968115396 @default.
• W2064235684 cites W1969185542 @default.
• W2064235684 cites W1973462203 @default.
• W2064235684 cites W1976353819 @default.
• W2064235684 cites W1980961479 @default.
• W2064235684 cites W1982413281 @default.
• W2064235684 cites W1986320887 @default.
• W2064235684 cites W1993262772 @default.
• W2064235684 cites W1996066245 @default.
• W2064235684 cites W2000342880 @default.
• W2064235684 cites W2003926188 @default.
• W2064235684 cites W2008443832 @default.
• W2064235684 cites W2014569891 @default.
• W2064235684 cites W2016408686 @default.
• W2064235684 cites W2023056845 @default.
• W2064235684 cites W2025522492 @default.
• W2064235684 cites W2034827192 @default.
• W2064235684 cites W2039597975 @default.
• W2064235684 cites W2040370168 @default.
• W2064235684 cites W2050397722 @default.
• W2064235684 cites W2052853635 @default.
• W2064235684 cites W2063690467 @default.
• W2064235684 cites W2064299413 @default.
• W2064235684 cites W2069179251 @default.
• W2064235684 cites W2069800916 @default.
• W2064235684 cites W2073760928 @default.
• W2064235684 cites W2075318845 @default.
• W2064235684 cites W2078594099 @default.
• W2064235684 cites W2091269867 @default.
• W2064235684 cites W2107890932 @default.
• W2064235684 cites W2116609506 @default.
• W2064235684 cites W2117692326 @default.
• W2064235684 cites W2122978471 @default.
• W2064235684 cites W2123513769 @default.
• W2064235684 cites W2125715557 @default.
• W2064235684 cites W2135732933 @default.
• W2064235684 cites W2144841919 @default.
• W2064235684 cites W2145006562 @default.
• W2064235684 cites W2145593053 @default.
• W2064235684 cites W2146226667 @default.
• W2064235684 cites W2160029849 @default.
• W2064235684 cites W2330446921 @default.
• W2064235684 cites W2952082761 @default.
• W2064235684 cites W84531549 @default.
• W2064235684 doi "https://doi.org/10.1021/jm401075x" @default.
• W2064235684 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24320998" @default.
• W2064235684 hasPublicationYear "2013" @default.
• W2064235684 type Work @default.
• W2064235684 sameAs 2064235684 @default.
• W2064235684 citedByCount "69" @default.
• W2064235684 countsByYear W20642356842014 @default.
• W2064235684 countsByYear W20642356842015 @default.
• W2064235684 countsByYear W20642356842016 @default.
• W2064235684 countsByYear W20642356842017 @default.
• W2064235684 countsByYear W20642356842018 @default.
• W2064235684 countsByYear W20642356842019 @default.
• W2064235684 countsByYear W20642356842020 @default.
• W2064235684 countsByYear W20642356842021 @default.
• W2064235684 countsByYear W20642356842022 @default.
• W2064235684 countsByYear W20642356842023 @default.
• W2064235684 crossrefType "journal-article" @default.
• W2064235684 hasAuthorship W2064235684A5001077804 @default.
• W2064235684 hasAuthorship W2064235684A5001466285 @default.
• W2064235684 hasAuthorship W2064235684A5003196865 @default.
• W2064235684 hasAuthorship W2064235684A5003991876 @default.

• next