Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions.
This paper describes an approach to prevent HIV-cell fusion by disrupting the interaction between HIV protein gp120 and CD4 receptor. The CD4 residues Phe43 and Arg59 make important interactions with gp120. Small molecule analogues were made to mimic the crucial features of these residues. The analogues were assayed using a cellular 'FIGS' assay to measure inhibition of cell fusion and caused some inhibition.
Boussard
Cyrille
C
Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF, UK.
Klimkait
Thomas
T
Mahmood
Naheed
N
Pritchard
Martin
M
Gilbert
Ian H
IH
D000578:Amidines / Q000138:chemical synthesis / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015704:CD4 Antigens / Q000737:chemistry*; D015195:Drug Design; D019791:Guanidine / Q000138:chemical synthesis / Q000494:pharmacology; D015699:HIV Envelope Protein gp120 / Q000737:chemistry*; D023581:HIV Fusion Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008561:Membrane Fusion / Q000187:drug effects; D018716:Molecular Mimicry; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship
D000578:Amidines; D019380:Anti-HIV Agents; D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D023581:HIV Fusion Inhibitors; D019791:Guanidine