Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA |
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| Institution: | 1. Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via Moruzzi 13, 56124 Pisa, Italy;2. Departamento de Química, Universidad de Burgos, Plaza Misael Bañuelos s/n, 09001 Burgos, Spain;1. Department of Biomedical Sciences, University of Padova, Padova, Italy;2. CRIBI Biotechnology Centre, University of Padova, Padova, Italy;3. CNR Institute of Neurosciences, Padova, Italy;1. Department of Chemistry and Biochemistry, Jackson State University, Jackson, MS 39217, USA;2. Department of Chemistry, Louisiana State University, Baton Rouge, LA 70803, USA |
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| Abstract: | 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. |
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| Keywords: | HIV-1 RRE RNA Branched peptides Boronic acids p24 inhibition |
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