CD4 mimics targeting the mechanism of HIV entry

A structure–activity relationship study was conducted of several CD4 mimicking small molecules which block the interaction between HIV-1 gp120 and CD4. These CD4 mimics induce a conformational change in gp120, exposing its co-receptor-binding site. This induces a highly synergistic interaction in the use in combination with a co-receptor CXCR4 antagonist and reveals a pronounced effect on the dynamic supramolecular mechanism of HIV-1 entry.

CD4 mimic small molecules interacting with a large cavity of HIV-1 gp120, which are targeted for the dynamic supramolecular mechanism of HIV entry, are reported.Figure optionsDownload as PowerPoint slide