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Novel Benzindole Based Compounds for HIV Therapy
Description of Technology:
The HIV/AIDS epidemic continues despite efforts from scientists, drug companies, and non-profit organizations. Although the existing therapy is effective in the treatment of many infected individuals in developed nations, the infected individual is not cured and therapy must be life-long. There are problems with drug toxicity, the development of resistant viral strains, and with the cost of therapy. New anti-viral agents are needed for a more effective, and a more cost-effective, treatment of HIV.
The invention describes compounds based on a benzindole moiety, which alkylates DNA. The compounds comprise a benzindole moiety, a bifunctional linker, and a fatty acid residue or dendrimer residue comprising at least one fatty acid. Several benzindole derivatives are synthesized. The compounds bind to the minor groove of DNA and can be useful in the inhibition of gene expression. The advantage of the compounds is that they remain inactive until conformational change induced by DNA binding makes them active. The fatty acid moiety immobilizes them on the cytoplasmic side of the plasma membrane. These anchored compounds are specifically designed to inhibit retroviral DNA before it translocates to the host nucleus and integrates with the host genome.
Applications and Modality:
- Novel benzindole-based compounds for HIV therapy.
- Compounds are specifically designed to inhibit retroviral DNA before it can integrate with the host genome.
- Additionally, compounds might have potential anti-cancer activities.
Market:
- More than 45 million people are living with HIV/AIDS worldwide.
- More than 3 million estimated deaths due to HIV/AIDS occurred worldwide in 2003.
- HIV/AIDS epidemic has caused more than 30 million deaths.
Development Status:
The technology is currently in the pre-clinical stage of development.
Inventors:
Christopher J. Michejda, Stephen H. Hughes (NCI), et al.
Relevant Publication:
A manuscript directly related to the above technology will be available as soon as it is accepted for publication.
Patent Status:
DHHS Reference No. E-126-2006/0 --
PCT Application No. PCT/US2007/080957 filed 10 Oct 2007, which published as WO 2008/045945 on 17 Apr 2008, claiming priority to 10 Oct 2006
Licensing Status:
Available for exclusive and non-exclusive licensing.
Collaborative Research Opportunity:
The National Cancer Institute’s Structural Biophysics Laboratory is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize novel benzindole based compounds for HIV therapy. Please contact John D. Hewes, Ph.D. at 301-435-3121 or hewesj@mail.nih.gov for more information.
Portfolio:
Infectious Diseases - Therapeutics, anti-virals, AIDS
For additional information, please contact:
Betty Tong, Ph.D.
Office of Technology Transfer
National Institutes of Health
6011 Executive Boulevard, Suite 325
Rockville MD 20852
Phone: 301/594-6565
Fax: 301/402-0220
Email: tongb@mail.nih.gov
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