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J Med Chem. 2013 Feb 14;56(3):1341-5. doi: 10.1021/jm301607v. Epub 2013 Jan 23.

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

Author information

1
Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, USA.

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.

PMID:
23316926
DOI:
10.1021/jm301607v
[Indexed for MEDLINE]

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