"The peptides P20A (Ac-AAASGINAEWPLWPGEAGWGRLEGRRTYEAEI-NH 2 ) and biotin-P20A (biotin-PEG4-AAASGINAEWPLWPGEAGWGRLEGRRTYEAEI-NH2 ) were synthesized by CPC Scientific."
Abstract
We previously identified an HIV-1 fusion inhibitor P20A targeting HIV-1 gp41 6-HB fusion core. Using alanine scanning mutagenesis, we investigated the effect of 6-HB surface residue mutations on the binding affinity between P20A and 6-HB. Substitution of positively or negatively charged residues in the distal region of 6-HB with alanines resulted in significant decrease or increase of its binding affinity to P20A, respectively. The 6-HB with E630K, D632K, or E634K mutation exhibited enhanced binding affinity with P20A, suggesting that P20A blocks HIV-1 fusion through electrostatic interaction with the positively charged residues in the distal region of the gp41 fusion core.
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