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Effect of intercalator and Lewis acid-base branched peptide complex formation: boosting affinity towards HIV-1 RRE RNA.


ABSTRACT: High throughput screening of a 4096 compound library of boronic acid and acridine containing branched peptides revealed compounds that have dissociation constants in the low nanomolar regime for HIV-1 RRE IIB RNA. We demonstrate that branched peptide boronic acids A5, A6, and A7 inhibit the production of p24, an HIV-1 capsid protein, in a dose-dependent manner.

SUBMITTER: Wynn JE 

PROVIDER: S-EPMC4957400 | biostudies-literature | 2016 Jul

REPOSITORIES: biostudies-literature

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Effect of intercalator and Lewis acid-base branched peptide complex formation: boosting affinity towards HIV-1 RRE RNA.

Wynn Jessica E JE   Zhang Wenyu W   Tebit Denis M DM   Gray Laurie R LR   Hammarskjold Marie-Louise ML   Rekosh David D   Santos Webster L WL  

MedChemComm 20160606 7


High throughput screening of a 4096 compound library of boronic acid and acridine containing branched peptides revealed compounds that have dissociation constants in the low nanomolar regime for HIV-1 RRE IIB RNA. We demonstrate that branched peptide boronic acids <b>A5</b>, <b>A6</b>, and <b>A7</b> inhibit the production of p24, an HIV-1 capsid protein, in a dose-dependent manner. ...[more]

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