Oncogenic ß-Catenin Targeted Human Cancer Cells for Identification and Testing of Novel Anticancer Drugs

Section: For Industry

Category(ies): Cancer Therapeutics

Reference #: WATO432802

OTC Contact: Tracy Bruehs, M.S., J.D. (Directory Information | Send a Message)

Description

A set of isogenic human colon cancer cells (HCT116) genetically identical except for the presence or complete absence of their endogenous wild-type or mutational activated ß-catenin gene. Activation of ß-catenin is a critical step in the pathogenesis of many human cancers and is the initiating event in adenocarcinoma of the colon. Activated ß-catenin, therefore, is a critical oncogenic stimulus throughout the progression of human colon cancer and is a useful target for screening small molecule inhibitors of activated ß-catenin.

Applications

Applications: Human somatic cell gene targeting to create an isogenic set of human colon cancer cells that differ only in the presence or absence of their endogenous wild-type or activated B-catenin gene. Such cells are well suited as a molecular target for development of anticancer pharmaceuticals.  These cells can be used in high throughput screens to identify novel B-catenin targeted agents and for secondary screens to test inhibitors identified in in-vitro assays.

Advantages:

  • Parental cells and cells retaining oncogenic B-catenin but deleted for wild-type ß -catenin serve as ideal isogenic controls allowing identification and testing of compounds with specific activity towards cancer cells with oncogenic ß –catenin
  • The cells are created by gene targeting (rather than siRNA/shRNA), resulting in complete abrogation of oncogene expression
  • Because activation of ß-catenin provides a gain-of-function, specific pharmacological inhibition of activated ß-catenin has been shown to reverse the tumorigenic properties of human cancer cells, and therefore, form the basis of an effective anticancer strategy.  

Advantages

Stage of Development

Inventor: Todd Waldman, M.D., Ph.D.

Relevant Publications

  • Kim JS, Crooks H, Dracheva T, Nishanian TG, Singh B, Jen J, Waldman T. Oncogenic B-Catenin is Required for BMP4 Expression in Human Cancer Cells. Cancer Research 62:2744, 2002. 
  • Kim JS, Crooks H, Foxworth A, Waldman T. B-Catenin is a Valid Molecular Target for the Development of Pharmacological Inhibitors. Molecular Cancer Therapeutics 1:1355, 2002.  

Patent Status

No current application pending.