New avenues to target Wnt/β-catenin signaling

Drug Discov Today. 2011 Jan;16(1-2):35-41. doi: 10.1016/j.drudis.2010.11.007. Epub 2010 Nov 24.


Wnt/β-catenin signaling is an evolutionarily conserved signaling cascade with imperative roles during development and in adult stem cell maintenance. Hyperactivation of Wnt/β-catenin drives various cancers, whereas hypoactivation underlies bone malformations and neurodegenerative disorders. Although several small molecule modulators of Wnt/β-catenin signaling have been identified, none have progressed into clinical trials yet. Recent studies employing genomics and proteomics approaches have yielded more druggable targets, such as kinases and seven-transmembrane receptors. In addition, new assay methods enable a more targeted approach for high-throughput screening of this pathway and are expected to deliver clinical candidates in the coming decade.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Drug Discovery
  • Humans
  • Molecular Targeted Therapy / methods
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism*
  • Signal Transduction / drug effects
  • Wnt Proteins / genetics
  • Wnt Proteins / metabolism*
  • beta Catenin / genetics
  • beta Catenin / metabolism*


  • Antineoplastic Agents
  • Wnt Proteins
  • beta Catenin