Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 24, Issue 17, Pages 3947-3952Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.04.009
Keywords
HIV-1; RRE RNA; Branched peptides; Boronic acids; p24 inhibition
Funding
- National Institutes of Health [R01GM093834, R01GM110009]
- University of Virginia
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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 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 regions of the RNA, which induces enzymatic cleavage of the internal loops of RRE IIB upon binding. (C) 2016 Elsevier Ltd. All rights reserved.
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