期刊
CANCER RESEARCH
卷 70, 期 14, 页码 5963-5973出版社
AMER ASSOC CANCER RESEARCH
DOI: 10.1158/0008-5472.CAN-10-1028
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资金
- Cardiff University
- CR-UK [C368/A5410, C368/A7505, C309/A2187, C309/A8274, C309/A8365]
- National Health Service
- Institute of Cancer Research
- Royal Marsden NHS Foundation Trust
- Biotechnology and Biological Sciences Research Council [BB/D00117X/1] Funding Source: researchfish
- BBSRC [BB/D00117X/1] Funding Source: UKRI
The Wnt signaling pathway is frequently deregulated in cancer due to mutations in genes encoding APC, beta-catenin, and axin. To identify small-molecule inhibitors of Wnt signaling as potential therapeutics, a diverse chemical library was screened using a transcription factor reporter cell line in which the activity of the pathway was induced at the level of Disheveled protein. A series of deconvolution studies was used to focus on three compound series that selectively killed cancer cell lines with constitutive Wnt signaling. Activities of the compounds included the ability to induce degradation of beta-catenin that had been stabilized by a glycogen synthase kinase-3 (GSK-3) inhibitor. This screen illustrates a practical approach to identify small-molecule inhibitors of Wnt signaling that can seed the development of agents suitable to treat patients with Wnt-dependent tumors. Cancer Res; 70(14); 5963-73. (C) 2010 AACR.
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