FIG 3.
Optimization of MCG analogs for their capacity to expose the CoRBS. Based on the structure of (S)-MCG-III-027-D05, 118 analogs were synthesized and purified. (A) Binding of the CD4i antibody 17b to HIV-1JR-FL EnvΔCT in the presence of analogs (50 μM) was evaluated by CBE. Analogs with higher activity (shown in red) were selected for further analysis. The mean RLU values from at least three independent experiments performed in quadruplicate are shown, with the signal obtained from wells transfected with an empty pcDNA3.1 plasmid (no Env) subtracted, normalized to Env levels as determined by 2G12 binding. Analogs and the positive control (+)-BNM-III-170 are plotted in decreasing order. (B) Structures of the selected analogs.