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  • Title: Identification of minimal sequence for HIV-1 fusion inhibitors.
    Author: Nishikawa H, Oishi S, Fujita M, Watanabe K, Tokiwa R, Ohno H, Kodama E, Izumi K, Kajiwara K, Naitoh T, Matsuoka M, Otaka A, Fujii N.
    Journal: Bioorg Med Chem; 2008 Oct 15; 16(20):9184-7. PubMed ID: 18819810.
    Abstract:
    Emergence of multi-drug resistant HIV-1 is a serious problem for AIDS treatment. Recently, the virus-cell membrane fusion process has been identified as a promising target for the development of novel drugs against these resistant variants. In this study, we identified a 29-residue peptide fusion inhibitor, SC29EK, which shows activity comparable to the previously reported inhibitor SC35EK. Some residues in SC29EK not required for interaction with virus gp41 heptad repeat 1 (HR1) were replaced with a non-proteinogenic amino acid, 2-aminoisobutyric acid (Aib), to stabilize the alpha-helix structure and to provide resistance to peptidases.
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