Proof-of-principle: oncogenic beta-catenin is a valid molecular target for the development of pharmacological inhibitors

Mol Cancer Ther. 2002 Dec;1(14):1355-9.

Abstract

Activation of beta-catenin is a critical step in the pathogenesis of many common human cancers and is the initiating event in adenocarcinoma of the colon. Because activation of beta-catenin provides a gain-of-function, it is tempting to speculate that specific pharmacological inhibition of activated beta-catenin might reverse the tumorigenic properties of human cancer cells and therefore form the basis of an effective anticancer strategy. In an effort to provide proof-of-principle for such a strategy, we used a novel clonal growth assay based on human somatic cell gene targeting to determine whether activated beta-catenin remains a necessary oncogenic stimulus in advanced human cancer cells. Using this approach, we demonstrate that beta-catenin is a necessary oncogene in human SW48 and DLD1 colon cancer cells but not in HCT116 cells. These data indicate that activated beta-catenin can remain a critical oncogenic stimulus throughout the progression of human colon cancer and suggest that the small molecule inhibitors of activated beta-catenin currently under development will be effective anticancer therapeutics in a subset of malignant colon cancers.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alleles
  • Animals
  • Cell Division
  • Colonic Neoplasms / metabolism
  • Cytoskeletal Proteins / chemistry
  • Cytoskeletal Proteins / metabolism*
  • Cytoskeletal Proteins / pharmacology*
  • Drug Evaluation, Preclinical*
  • Humans
  • Mice
  • Mice, Knockout
  • Mice, SCID
  • Neoplasm Transplantation
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Time Factors
  • Trans-Activators / chemistry
  • Trans-Activators / metabolism*
  • Trans-Activators / pharmacology*
  • Transfection
  • Tumor Cells, Cultured
  • beta Catenin

Substances

  • CTNNB1 protein, human
  • CTNNB1 protein, mouse
  • Cytoskeletal Proteins
  • Trans-Activators
  • beta Catenin