A -- Development of Scytovirin, a Unique anti-HIV Protein, for Microbicidal and/or Therapeutic Use(s)

The National Cancer Institute (NCI) Molecular Targets Development Program (MTDP) seeks a Cooperative Research and Development Agreement (CRADA) collaborator to develop scytovirin, a new, 95 amino acid, anti-HIV protein isolated from aqueous extracts of the cultured cyanobacterium Scytonema varium. Scytovirin displayed potent anticytopathic activity against laboratory strains and primary isolates of HIV-1 (EC50 0.3 -22 nM). Scytovirin binds to the viral coat proteins gp120, gp160 and gp41 but not to the cellular receptor CD4 or other tested proteins. Scytovirin has been shown to bind to specific oligosaccharides on HIV Env glycoproteins with unique specificity. Potential Areas if Application: Potential anti-HIV microbicide as a female-controlled virucidal gel, cream or suppository. Also potential therapeutic agent for systemic use similar to Fuzeon®. Main Advantages of the Technology: Uniquely binds to specific oligosaccharides on HIV envelope. No toxicity displayed in host cells at highest tested concentrations. Has been produced recombinantly in E. coli. Current State of Development: On-going structural NMR and X-ray crystallographic studies as well as structural / thermodynamic binding studies to oligosaccharide molecular target. In vitro evaluation against additional viruses on-going. Further R&D Required: In vivo efficacy, immunogenicity, toxicity, pharmacokinetic, ADME and large-scale production studies. Patent Status and Pertinent References: a) U.S. Patent Application filed on May 16, 2002. b) H.R. Bokesch et al., Biochemistry, 2003, 42(9), 2578-2584. c) E.W. Adams et al., Chemistry and Biology, 2004, 875-881. Contact Information: Bjarne Gabrielsen, Ph.D., Technology Transfer Branch, NCI-Frederick, Fairview Center, Suite 500, 1003 - W. 7th Street, Frederick, MD 21701-8512. Phone: (301) 846-5465; email: [email protected]. Submitted: 9/1/2004