Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA

摘要

A branched peptide containing multiple boronic acids was found to bind RRE IIB selectively and inhibit HIV-1 p24 capsid production in a dose-dependent manner. Structure-activity relationship studies revealed that branching in the peptide is crucial for the low micromolar binding towards RRE IIB, and that the peptide demonstrates selectivity towards RRE IIB in the presence of tRNA. Footprinting studies suggest a binding site on the upper stem and internal loop region of the RNA, which induces enzymatic cleavage of the internal loops of RRE IIB upon binding.