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

Kazuki Shimane, Kumi Kawaji, Fusako Miyamoto, Shinya Oishi, Kentaro Watanabe, Yasuko Sakagami, Nobutaka Fujii, Kazuya Shimura, Masao Matsuoka, Mitsuo Kaku, Stefan G. Sarafianos, Eiichi N. Kodama

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

T-20EK is a novel fusion inhibitor designed to have enhanced-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.

Original languageEnglish
Pages (from-to)4035-4038
Number of pages4
JournalAntimicrobial agents and chemotherapy
Volume57
Issue number8
DOIs
Publication statusPublished - 2013 Aug

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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