Development of small molecules targeting the Wnt pathway for the treatment of colon cancer: a high-throughput screening approach.

Published

Journal Article (Review)

Wnt proteins play major roles in development and differentiation, and abnormalities in their regulation are believed to contribute to the formation of many cancers, including colorectal malignancies. As a result, there has been an interest in identifying small molecule inhibitors of Wnt signaling as tool compounds for research or as precursors to new generations of anticancer drugs. Advancements in robotic technology along with reductions in the costs of equipment, chemical libraries, and information handling have made high-throughput drug discovery programs possible in an academic setting. In this minireview we discuss the most plausible protein targets for inhibiting Wnt signaling in colon cancer therapy, list small molecule Wnt inhibitors that have been identified through recent drug discovery efforts, and provide our laboratory's strategy for identifying novel Wnt signaling antagonists using high-throughput screening. In particular, we summarize the results of a screen of over 1,200 drug and druglike compounds we recently completed in which niclosamide was identified as a Wnt pathway antagonist.

Full Text

Duke Authors

Cited Authors

  • Chen, W; Chen, M; Barak, LS

Published Date

  • August 2010

Published In

Volume / Issue

  • 299 / 2

Start / End Page

  • G293 - G300

PubMed ID

  • 20508156

Pubmed Central ID

  • 20508156

Electronic International Standard Serial Number (EISSN)

  • 1522-1547

Digital Object Identifier (DOI)

  • 10.1152/ajpgi.00005.2010

Language

  • eng

Conference Location

  • United States