Structure-activity relationship studies of small-molecule inhibitors of Wnt response

Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. doi: 10.1016/j.bmcl.2009.04.040. Epub 2009 Apr 18.

Abstract

Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / chemistry*
  • Animals
  • Axin Protein
  • Imides / chemistry*
  • Repressor Proteins / metabolism
  • Signal Transduction
  • Structure-Activity Relationship
  • Tail
  • Wnt Proteins / antagonists & inhibitors*
  • Wnt Proteins / metabolism
  • Zebrafish / metabolism

Substances

  • Aminoquinolines
  • Axin Protein
  • Imides
  • Repressor Proteins
  • Wnt Proteins