Advertisement

 

 

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

Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA.
Author Information (click to view)

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


Wynn JE, Zhang W, Tebit DM, Gray LR, Hammarskjold ML, Rekosh D, Santos WL, (click to view)

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

Advertisement
Share on FacebookTweet about this on TwitterShare on LinkedIn

Bioorganic & medicinal chemistry 2016 04 0524(17) 3947-52 doi 10.1016/j.bmc.2016.04.009

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.

Submit a Comment

Your email address will not be published. Required fields are marked *

5 − four =

[ HIDE/SHOW ]