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

Structure-activity relationship studies of small-molecule inhibitors of Wnt response.
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DOI:
10.1016/j.bmcl.2009.04.040
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发表时间:
2009-07-15
影响因子:
2.7
通讯作者:
Chen C
Chen C
中科院分区:
医学4区
文献类型:
--
作者:
Lu J;Ma Z;Hsieh JC;Fan CW;Chen B;Longgood JC;Williams NS;Amatruda JF;Lum L;Chen C

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抑制致癌Wnt介导的信号传导有望成为抗癌治疗策略。我们先前报道了一类新的小分子(IWR-1/2,Wnt反应抑制剂),通过稳定Axin破坏复合物来拮抗Wnt信号传导。在此,我们提出了这些化合物的结构/活性关系的研究结果。
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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