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Identification of a beta3-peptide HIV fusion inhibitor with improved potency in live cells.


ABSTRACT: We recently reported a beta(3)-decapeptide, betaWWI-1, that binds a validated gp41 model in vitro and inhibits gp41-mediated fusion in cell culture. Here we report six analogs of betaWWI-1 containing a variety of non-natural side chains in place of the central tryptophan of the WWI-epitope. These analogs were compared on the basis of both gp41 affinity in vitro and fusion inibition in live, HIV-infected cells. One new beta(3)-peptide, betaWXI-a, offers a significantly improved CC(50)/EC(50) ratio in the live cell assay.

SUBMITTER: Bautista AD 

PROVIDER: S-EPMC2737262 | biostudies-literature | 2009 Jul

REPOSITORIES: biostudies-literature

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Identification of a beta3-peptide HIV fusion inhibitor with improved potency in live cells.

Bautista Arjel D AD   Stephens Olen M OM   Wang Ligong L   Domaoal Robert A RA   Anderson Karen S KS   Schepartz Alanna A  

Bioorganic & medicinal chemistry letters 20090515 14


We recently reported a beta(3)-decapeptide, betaWWI-1, that binds a validated gp41 model in vitro and inhibits gp41-mediated fusion in cell culture. Here we report six analogs of betaWWI-1 containing a variety of non-natural side chains in place of the central tryptophan of the WWI-epitope. These analogs were compared on the basis of both gp41 affinity in vitro and fusion inibition in live, HIV-infected cells. One new beta(3)-peptide, betaWXI-a, offers a significantly improved CC(50)/EC(50) rati  ...[more]

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