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. published the artcile< Discovery of Novel, Induced-Pocket Binding Oxazolidinones as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors>, Recommanded Product: Methyl 3-fluoroisonicotinate, the main research area is preparation SAR oxazolidinone orally bioavailable tankyrase inhibitor mol modeling.
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 I is a previously described moderately potent tankyrase inhibitor that suffers from poor pharmacokinetic properties. Herein, we describe the utilization of structure-based design and mol. modeling toward novel, potent, and selective tankyrase inhibitors with improved pharmacokinetic properties (II, III).
Journal of Medicinal Chemistry published new progress about Axins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 876919-08-3 belongs to class pyridine-derivatives, and the molecular formula is C7H6FNO2, Recommanded Product: Methyl 3-fluoroisonicotinate.