Description

An orphan G-protein coupled receptor (GPCR) has previously been shown to be involved in estrogen signaling in breast cancer cells. Also, this GPCR has been suggested to be the membrane estrogen receptor (mER) mediating these estrogen effects. However, no reports were available demonstrating that the GPCR has the binding characteristics of an estrogen membrane receptor. Such reports would provide a means to develop new drugs and screen them for binding to a membrane estrogen receptor on breast cancer cells that would most likely participate in the estrogen stimulation of breast cancer. Additionally, the current treatment for breast cancer is Tamoxifen, which acts on the nuclear estrogen receptor as an antagonist. However, at somewhat higher concentrations, this drug can activate the GPCR which in turn activates growth factor pathways in breast cancer cells. This could explain the cancer-promoting effects of Tamoxifen treatment in certain breast cancer patients. Knowledge of the cDNAs would facilitate the development of new drugs that could attack both receptors. This would in turn provide for a safer and more effective treatment.

This technology demonstrates that the recombinant protein produced in mammalian cells has all the binding characteristics of an estrogen membrane receptor. This discovery has several potential uses. The most important use is that it enables selective membrane estrogen receptor antagonists (SMERAs) to be developed which are likely to have important therapeutic value in the treatment of estrogen dependent breast cancer. The mechanistic understanding provided by this discovery, as well as the development of a cell-based screening system to identify and test estrogen mER agonists and antagonists, will enable the development of a new class of drugs for a variety of clinical applications.

Benefits

• Provides a valuable diagnostic tool
  
• Provides a new receptor target for estrogenic and anti-estrogenic compounds
  
• Allows direct assessment of binding and potency of potential drugs
  
• Provides a mechanistic understanding of the nature of the receptor involved in mediating the pathway
  

Features

• Identifies ligands of normal and malignant tissues
  
• Nuclear and membrane estrogen receptors show no structural similarity.
  
• Membrane estrogen receptor has the characteristics of G-protein coupled receptors.
  
• Membrane estrogen receptor's specificity for natural and synthetic estrogens and anti-estrogens differs from those of estrogen receptor alpha and beta
  

Market Potential/Applications

In addition to breast cancer, other possible targets for intervention by agonists or antagonists for this receptor are the brain, cardiovascular tissue, prostate, ovaries, and testes.

IP Status

One U.S. Patent Application filed

For further information please contact:

University of Texas,
Austin, USA
Website : www.otc.utexas.edu