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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Wynn JE,Zhang W,Tebit DM,Gray LR,Hammarskjold ML,Rekosh D,Santos WL

doi

10.1016/j.bmc.2016.04.009

subject

Has Abstract

pub_date

2016-09-01 00:00:00

pages

3947-3952

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30243-7

journal_volume

24

pub_type

杂志文章

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