HIV-1 resistance mechanism to an electrostatically constrained peptide fusion inhibitor that is active against T-20-resistant strains.

Abstract:

:T-20EK is a novel fusion inhibitor designed to have enhanced α-helicity over T-20 (enfuvirtide) through engineered electrostatic interactions between glutamic acid (E) and lysine (K) substitutions. T-20EK efficiently suppresses wild-type and T-20-resistant variants. Here, we selected T-20EK-resistant variants. A combination of L33S and N43K substitutions in gp41 were required for high resistance to T-20EK. While these substitutions also caused resistance to T-20, they did not cause cross-resistance to other known fusion inhibitors.

authors

Shimane K,Kawaji K,Miyamoto F,Oishi S,Watanabe K,Sakagami Y,Fujii N,Shimura K,Matsuoka M,Kaku M,Sarafianos SG,Kodama EN

doi

10.1128/AAC.00237-13

subject

Has Abstract

pub_date

2013-08-01 00:00:00

pages

4035-8

issue

8

eissn

0066-4804

issn

1098-6596

pii

AAC.00237-13

journal_volume

57

pub_type

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