Identification of Anti-HIV Compounds Inhibiting Virus Assembly and Binding of Nucleocapsid Protein to Nucleic Acid


The subject invention identified two groups of active anti-viral compounds. The first group comprises aromatic, antimony-containing compounds, while the second group comprises aromatic tricarboxylic acid. Both groups were shown to inhibit viral particle assembly and inhibit the binding of nucleocapsid protein to nucleic acid. Recently, the first group also demonstrated the capability of blocking HIV-1 viral entry into CD4+ cells through binding to CD4 and inhibiting gp120-CD4 interaction, and they are well tolerated in vivo. Hence, these compounds are potent inhibitors of HIV and act via a novel mechanism, ideal for developing a new generation of anti-HIV medicine.

Potential Commercial Applications: Competitive Advantages:
HIV treatment and prevention 


Development Stage:
In vivo preclinical data available, including data from efficacy, pharmacokinetics and preliminary toxicity studies.

Inventors:

Robert Shoemaker (NCI)  ➽ more inventions...

Michael Currens (NCI)  ➽ more inventions...

Alan Rein (NCI)  ➽ more inventions...

Ya-xiong Feng (NCI)  ➽ more inventions...

Robert Fisher (NCI)  ➽ more inventions...

Andrew Stephen (NCI)  ➽ more inventions...

Karen Worthy (NCI)  ➽ more inventions...

Shizuko Sei (NCI)  ➽ more inventions...

Bruce Crise (NCI)  ➽ more inventions...

Louis Henderson (NCI)  ➽ more inventions...


Intellectual Property:
US Application No. 03773233.6
EP Application No. PCT/US03/32086
PCT Application No. 60/416,854

Publications:
QE Yang et al. Discovery of small-molecule human immunodeficiency virus type 1 entry inhibitors that target the gp120-binding domain of CD4. J Virol. 2005 May;79(10):6122-6133. PubMed abs

Collaboration Opportunity:

The NCI HIV DRP Retroviral Replication Laboratory is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize these active anti-viral compounds. Please contact John D. Hewes, Ph.D. at 301-435-3121 or hewesj@mail.nih.gov for more information.


Licensing Contact:
Jasmine Yang, Ph.D.
Email: jasmine.yang@nih.gov
Phone: 301-624-8746

OTT Reference No: E-121-2002-0
Updated: Jun 16, 2010