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G-Protein Coupled Receptor Antagonists

Description of Invention:
This invention is a potentially broadly applicable method of disrupting the functioning of G-protein coupled receptors (GPCR). GPCRs are a large family of receptors involved in the regulation of physiological activities. GPCRs have seven transmembrane regions, i.e. they cross the cell membrane seven times. The inventors have found that if a peptide consisting of one of the transmembrane regions of a GPCR with an added charged amino acid on the extracellular side, is brought into contact with a cell having the same GPCR, the functioning of the GPCR is disrupted. It is thought that the added peptide interferes with the correct assembly of the GPCR. Cells containing the CXCR4 receptor, a co-receptor with CD4 for the entry of certain strains of HIV-1 into T-cells, are much less receptive to infection by HIV in the presence of a particular transmembrane peptide from the CXCR4 receptor. Therefore, this method of disrupting the functioning of particular GPCRs could be used to treat diseases which are mediated by functioning GPCRs, such as HIV.

Inventors:
Nadya I Tarasova (NCI)
Christopher J Michejda (NCI)


Patent Status:
HHS, Reference No. E-290-1997/0
PCT, Application No. PCT/US99/04438 filed 26 Feb 1999
US, , Patent No. 7,105,488, Issued 12 Sep 2006



For Licensing Information Please Contact:
Jennifer Wong
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: wongje@mail.nih.gov
Phone: 301-435-4633
Fax: 301-402-0220


Ref No: 50

Updated: 09/1998

 

 
 
 
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