Potent Protease-Resistant Inhibitors of HIV Entry, a Novel Compound for Treatment of AIDS
The present invention provides a new family of potent D-peptide inhibitors of HIV entry. These inhibitors have several advantages over Fuzeon, the only FDA-approved HIV entry inhibitor that is currently available. First, these inhibitors are resistant to proteases (potentially allowing oral bioavailability, long serum half-life, long shelf-life, infrequent dosing, and use as a microbicide); secondly, they target a highly conserved region of HIV that has been shown to be critical for viral infectivity, reducing the likelihood of resistance mutations; thirdly, they are small peptides with much simpler synthesis and purification than Fuzeon.
Currently, Fuzeon (Trimeris/Roche) is the only FDA-approved entry inhibitor for HIV infection. Fuzeon is a 36-amino acid peptide that is composed of natural L-amino acids. It is degraded extremely rapidly in the body by proteases, and thus it is administered in very high doses at very high cost (~$25,000/year).
The potent D-peptides provided by this invention can be used as an entry inhibitor in HIV patients and/or as a topical prophylactic microbicide. Also, they can be used as research tools for discovering small molecule inhibitors of HIV. The techniques used to discover these D-peptides can also be applied to other systems, particularly for other viruses with similar entry mechanisms (e.g., Ebola, Influenza, RSV).
Stage of Development
A provisional patent application has been requested.
This technology is part of an active and ongoing research program with several lab prototypes available. It is available for developmental research support or licensing under either exclusive or non-exclusive terms.
*Hamburger AE, Kim S, Welch BD, Kay MS. (2005) Steric accessibility of the HIV-1 gp41 N-trimer region. J Biol Chem. 280(13):12567-72.
Michael Kay, Brett Welch
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