Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation
Authors:
- 13 June 2016
- journal article
- Published by Springer Nature in Nature Chemical Biology
- Vol. 12 (8) , 593-600
Abstract
A small-molecule compound binds to the RGS domain of axin, promotes the degradation of [beta]-catenin and Ras through the GSK3[beta]-mediated destruction complex, and reduces the growth of KRAS and APC mutant colorectal cancer cell lines.Keywords
This publication has 40 references indexed in Scilit:
- Role of Oncogenic K-Ras in Cancer Stem Cell Activation by Aberrant Wnt/β-Catenin SignalingJNCI: Journal of the National Cancer Institute, 2014
- Ras Stabilization Through Aberrant Activation of Wnt/β-Catenin Signaling Promotes Intestinal TumorigenesisScience Signaling, 2012
- The Protein Stability of Axin, a Negative Regulator of Wnt Signaling, Is Regulated by Smad Ubiquitination Regulatory Factor 2 (Smurf2)Journal of Biological Chemistry, 2010
- Mutated K‐rasAsp12 promotes tumourigenesis in ApcMin mice more in the large than the small intestines, with synergistic effects between K‐ras and Wnt pathwaysInternational Journal of Experimental Pathology, 2009
- The Axin1 scaffold protein promotes formation of a degradation complex for c‐MycThe EMBO Journal, 2009
- Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancerNature Chemical Biology, 2009
- Colorectal Cancer PreventionJournal of Clinical Oncology, 2005
- Multiple mutations and cancerProceedings of the National Academy of Sciences, 2003
- The genetic basis of colorectal cancer: Insights into critical pathways of tumorigenesisGastroenterology, 2000
- Requirement for glycogen synthase kinase-3β in cell survival and NF-κB activationNature, 2000