Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

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

Ewan, Kenneth Burnside Ramsay, 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, Wilson, Samuel, Latinkic, Branko, Workman, P., McDonald, E., Blagg, J., Aherne, W. and Dale, Trevor Clive 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

Full text not available from this repository.

Abstract

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)
Subjects: Q Science > Q Science (General)
Publisher: AACR
ISSN: 0008-5472
Last Modified: 06 Aug 2019 22:27
URI: http://orca-mwe.cf.ac.uk/id/eprint/23606

Citation Data

Cited 54 times in Google Scholar. View in Google Scholar

Cited 76 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item