1437789-57-5Relevant articles and documents
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors
Bregman, Howard,Chakka, Nagasree,Guzman-Perez, Angel,Gunaydin, Hakan,Gu, Yan,Huang, Xin,Berry, Virginia,Liu, Jingzhou,Teffera, Yohannes,Huang, Liyue,Egge, Bryan,Mullady, Erin L.,Schneider, Steve,Andrews, Paul S.,Mishra, Ankita,Newcomb, John,Serafino, Randy,Strathdee, Craig A.,Turci, Susan M.,Wilson, Cindy,Dimauro, Erin F.
, p. 4320 - 4342 (2013/07/19)
Tankyrase (TNKS) is a poly-ADP-ribosylating protein (PARP) whose activity suppresses cellular axin protein levels and elevates β-catenin concentrations, resulting in increased oncogene expression. The inhibition of tankyrase (TNKS1 and 2) may reduce the levels of β-catenin-mediated transcription and inhibit tumorigenesis. Compound 1 is a previously described moderately potent tankyrase inhibitor that suffers from poor pharmacokinetic properties. Herein, we describe the utilization of structure-based design and molecular modeling toward novel, potent, and selective tankyrase inhibitors with improved pharmacokinetic properties (39, 40).
