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A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription

Ewan, Kenneth Burnside Ramsay ORCID:, Pajak, Bozena, Stubbs, M., Todd, H., Barbeau, O., Quevedo, C., Botfield, H., Young, R., Ruddle, R., Samuel, L., Battersby, Alysia Agnes, Raynaud, F., Allen, Nicholas Denby ORCID:, Wilson, Samuel, Latinkic, Branko ORCID:, Workman, P., McDonald, E., Blagg, J., Aherne, W. and Dale, Trevor Clive ORCID: 2010. A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. Cancer Research 70 (14) , pp. 5963-5973. 10.1158/0008-5472.CAN-10-1028

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The Wnt signaling pathway is frequently deregulated in cancer due to mutations in genes encoding APC, β-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 β-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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Neuroscience and Mental Health Research Institute (NMHRI)
European Cancer Stem Cell Research Institute (ECSCRI)
Subjects: Q Science > Q Science (General)
Publisher: AACR
ISSN: 0008-5472
Last Modified: 22 Jun 2023 10:01

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