Details

Autor(en) / Beteiligte

• Bregman, Howard
• Gunaydin, Hakan
• Gu, Yan
• Schneider, Steve
• Wilson, Cindy
• DiMauro, Erin F
• Huang, Xin

Titel

Discovery of a Class of Novel Tankyrase Inhibitors that Bind to Both the Nicotinamide Pocket and the Induced Pocket

Ist Teil von

• Journal of medicinal chemistry, 2013-02, Vol.56 (3), p.1341-1345

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2013

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.