An α-Helical Peptidomimetic Inhibitor of the HIV-1 Rev−RRE Interaction

摘要: The interaction between the HIV-1 Rev protein and Rev-Responsive Element (RRE) RNA is an attractive target for anti-viral therapy. We have designed α-helical peptidomimetics of Rev-like peptides using side chain−side chain macrolactam formation positions i i+4. One peptidomimetic having appropriate location, orientation, length exhibited both significant helical character specific RRE binding. This molecule displays 2-fold greater specificity than wild-type peptide more 20-fold uncyclized control peptide. Thus, specific, high affinity recognition feasible utilizing a small, relatively rigid scaffold.