Article
A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth.
Cancer research - 15 May 2013
Lau Ted, Chan Emily, Callow Marinella, Waaler Jo, Boggs Jason, Blake Robert A, Magnuson Steven, Sambrone Amy, Schutten Melissa, Firestein Ron, Machon Ondrej, Korinek Vladimir, Choo Edna, Diaz Dolores, Merchant Mark, Polakis Paul, Holsworth Daniel D, Krauss Stefan, Costa Mike
Abstract excerpt
Most colorectal cancers (CRC) are initiated by mutations of APC, leading to increased β-catenin-mediated signaling. However, continued requirement of Wnt/β-catenin signaling for tumor progression in the context of acquired KRAS and other mutations is less well-established. To attenuate Wnt/β-catenin signaling in tumors, we have developed potent and specific small-molecule tankyrase inhibitors, G007-LK and...
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