Document Report Card

ID: ALA2311538

Journal: J Med Chem

Title: Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.

Authors: Bregman H, Gunaydin H, Gu Y, Schneider S, Wilson C, DiMauro EF, Huang X.

Abstract: Potent and selective inhibitors of tankyrases have recently been characterized to bind to an induced pocket. Here we report the identification of a novel potent and selective tankyrase inhibitor that binds to both the nicotinamide pocket and the induced pocket. The crystal structure of human TNKS1 in complex with this "dual-binder" provides a molecular basis for their strong and specific interactions and suggests clues for the further development of tankyrase inhibitors.

CiteXplore: 23316926

DOI: 10.1021/jm301607v