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

TY - JOUR

T1 - 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

AU - Boussard, Cyrille

AU - Doyle, Valerie E.

AU - Mahmood, Naheed

AU - Klimkait, Thomas

AU - Pritchard, Martyn

AU - Gilbert, Ian H.

PY - 2002/11

Y1 - 2002/11

N2 - 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.

AB - 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.

U2 - 10.1016/S0223-5234(02)01412-5

DO - 10.1016/S0223-5234(02)01412-5

M3 - Article

SN - 0223-5234

VL - 37

SP - 883

EP - 890

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 11

ER -