Design, synthesis and evaluation of peptide libraries as potential anti-HIV compounds, via inhibition of gp120/cell membrane interactions, using the gp120/cd4/fab17 crystal structure

Cyrille Boussard, Valerie E. Doyle, Naheed Mahmood, Thomas Klimkait, Martyn Pritchard, Ian H. Gilbert

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    The crystal structure of a gp120/CD4/Fab17b complex was analysed leading to the design of several peptide libraries in the hope of obtaining novel gp120/cell membrane receptor interaction inhibitors, especially inhibitors of gp120/CD4 and gp120/chemokine receptor interactions. Syntheses of tri- and tetra- and pentapeptides were performed via a solid phase synthesis methodology using a Rink Amide MBHA resin and a Fmoc strategy giving C-terminal amide form peptides. Compounds were assayed against C8166 cells infected by HIV-1 IIIB and screened using a gp120 binding assay and the FIGS reporter gene assay. (C) 2002 Published by Editions scientifiques et medicales Elsevier SAS.

    Original languageEnglish
    Pages (from-to)883-890
    Number of pages8
    JournalEuropean Journal of Medicinal Chemistry
    Issue number11
    Publication statusPublished - Nov 2002

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