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

Posted Jun 15 2010 5:00pm

Description of Invention:
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.

HIV treatment and prevention

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

Robert H Shoemaker (NCI)
Michael J Currens (NCI)
Alan R Rein (NCI)
Ya-xiong Feng (NCI)
Robert J Fisher (NCI)
Andrew G Stephen (NCI)
Karen Worthy (NCI)
Shizuko Sei (NCI)
Bruce Crise (NCI)
Louis E Henderson (NCI)

Patent Status:
HHS, Reference No. E-121-2002/0
US, , Patent No. 7,572,828, Issued 11 Aug 2009
EP, Application No. 03773233.6 filed 08 May 2005
PCT, Application No. PCT/US03/32086 filed 08 Oct 2003

Relevant Publication:
  1. 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 ]

Licensing Status:
Available for exclusive and non-exclusive licensing.

Collaborative Research 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 for more information.

Infectious Diseases
Infectious Diseases - Therapeutics
In-vivo Data

For Additional Information Please Contact:
Sally Hu Ph.D., M.B.A.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325 Room 21,
Rockville, MD 20852
United States
Phone: 301-435-5606
Fax: 301-402-0220

Ref No: 665

Updated: 06/2010

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