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American Society for Microbiology, Antimicrobial Agents and Chemotherapy, 8(57), p. 4035-4038, 2013

DOI: 10.1128/aac.00237-13

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HIV-1 Resistance Mechanism to an Electrostatically Constrained Peptide Fusion Inhibitor That Is Active against T-20-Resistant Strains

Journal article published in 2013 by Kazuki Shimane, Kumi Kawaji, Fusako Miyamoto, Shinya Oishi, Kentaro Watanabe, Yasuko Sakagami, Nobutaka Fujii, Kazuya Shimura ORCID, Masao Matsuoka ORCID, Mitsuo Kaku, Stefan G. Sarafianos, Eiichi N. Kodama
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

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.