2. Academic Validation
  3. Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket

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

  • J Med Chem. 2013 Feb 14;56(3):1341-5. doi: 10.1021/jm301607v.
Howard Bregman 1,  Hakan Gunaydin,  Yan Gu,  Steve Schneider,  Cindy Wilson,  Erin F DiMauro,  Xin Huang
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, USA.
PMID: 23316926 DOI: 10.1021/jm301607v
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.

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