A -- Indolicidin Derivatives: Potent Inhibitors of HIV-1 Integrase For Treatment of Retroviral Infection and HIV

The National Cancer Institute (NCI) seeks a Cooperative Research and Development Agreement (CRADA) collaborator to develop a series of short peptides derived from indolicidin. These peptides exhibit potent anti-retroviral activity by inhibiting HIV-1 integrase and possess higher antiviral and anti-integrase activity than indolicidin itself. Potential Commercial Applications: - Treatment of retroviral infections such as AIDS. - These compounds may be used alone, or in combination with other anti-viral therapies directed at other viral targets such as protease and reverse transcriptase. Main Advantages of the Technology: - Potential for high clinical utility since HIV-1 integrase is essential for viral replication and no counterpart exists in mammalian cells. Current State of Development: - Testing of tetrameric peptides show that these oligomers inhibit the action of integrase at nanomolar concentrations. Further R&D Required: - Enhancing the transport properties of the current agents - Evaluating toxicology and efficacy in vivo. Patent Status: - Three U.S. Patent Applications filed 1/06/2004, 2/25/2004, and 8/10/2004 Pertinent References: - Krajewski K, et al. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5595-8. - Krajewski K, et al. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3203-5. Contact Information: CRADA Contact: Steven C. Fausch, Ph.D., Technology Transfer Branch, NCI Phone: +1 (555) 000-0000; E-mail: contact@example.gov Licensing Contact: Sally Hu, Ph.D., M.B.A., Office of Technology Transfer, NIH Phone: +1 (555) 000-0000; E-mail: contact@example.gov