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  • Title: Progress in identifying peptides and small-molecule inhibitors targeted to gp41 of HIV-1.
    Author: Debnath AK.
    Journal: Expert Opin Investig Drugs; 2006 May; 15(5):465-78. PubMed ID: 16634685.
    Abstract:
    During the last decade, a great number of activities have been geared in identifying newer targets for inhibiting HIV infection as well as understanding the targets for already identified anti-HIV-1 agents. The success in converting a proof-of-concept peptide T-20 (previously named DP-178), from the C-terminal heptad repeat (CHR) region of the envelope glycoprotein gp41 of HIV-1, to a drug named enfuvirtide was one of the phenomenal successes in HIV-1 drug discovery research that has been made in recent years. There were many reports of modifying peptides from the N-terminal heptad repeat and CHR regions with the objective of improving their activity. A few laboratories also reported the identification of small-molecule inhibitors that apparently bind to the hydrophobic cavity identified in the gp41 core structure and prevent the CHR peptide binding to the N-terminal heptad repeat peptide, thereby prevent the formation of the typical six-helix bundle, which has been thought to be necessary for the fusion between HIV and cell membranes.
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