Identification of minimal sequence for HIV-1 fusion inhibitors

Hiroki Nishikawa, Shinya Oishi, Mizuno Fujita, Kentaro Watanabe, Rei Tokiwa, Hiroaki Ohno, Eiichi Kodama, Kazuki Izumi, Keiko Kajiwara, Takeshi Naitoh, Masao Matsuoka, Akira Otaka, Nobutaka Fujii

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)

Abstract

Emergence of multi-drug resistant HIV-1 is a serious problem for AIDS treatment. Recently, the virus-cell membrane fusion process has been identified as a promising target for the development of novel drugs against these resistant variants. In this study, we identified a 29-residue peptide fusion inhibitor, SC29EK, which shows activity comparable to the previously reported inhibitor SC35EK. Some residues in SC29EK not required for interaction with virus gp41 heptad repeat 1 (HR1) were replaced with a non-proteinogenic amino acid, 2-aminoisobutyric acid (Aib), to stabilize the α-helix structure and to provide resistance to peptidases.

Original languageEnglish
Pages (from-to)9184-9187
Number of pages4
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number20
DOIs
Publication statusPublished - 2008 Oct 15
Externally publishedYes

Keywords

  • Fusion inhibitor
  • HIV-1
  • Heptad repeat
  • α-Helix

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint

Dive into the research topics of 'Identification of minimal sequence for HIV-1 fusion inhibitors'. Together they form a unique fingerprint.

Cite this