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  2. Structure-activity relationship studies of small-molecule inhibitors of Wnt response

Structure-activity relationship studies of small-molecule inhibitors of Wnt response

  • Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. doi: 10.1016/j.bmcl.2009.04.040.
Jianming Lu 1 Zhiqiang Ma Jen-Chieh Hsieh Chih-Wei Fan Baozhi Chen Jamie C Longgood Noelle S Williams James F Amatruda Lawrence Lum Chuo Chen
Affiliations

Affiliation

  • 1 Department of Biochemistry, The University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA.
Abstract

Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.

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