An alpha-helical peptidomimetic inhibitor of the HIV-1 Rev-RRE interaction |
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Authors: | Mills Nicholas L Daugherty Matthew D Frankel Alan D Guy R Kiplin |
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Affiliation: | Department of Biochemistry and Biophysics, University of California, San Francisco, California 94143-2280, USA. |
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Abstract: | The interaction between the HIV-1 Rev protein and the Rev-Responsive Element (RRE) RNA is an attractive target for anti-viral therapy. We have designed alpha-helical peptidomimetics of Rev-like peptides using side chain-side chain macrolactam formation between positions i and i+4. One peptidomimetic having an appropriate location, orientation, and length of the macrolactam exhibited both significant helical character and specific RRE binding. This molecule displays 2-fold greater RNA specificity than the wild-type Rev peptide and more than 20-fold greater specificity than an uncyclized control peptide. Thus, specific, high affinity recognition of the RRE is feasible utilizing a small, relatively rigid peptidomimetic scaffold. |
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