Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease

Hiromi Naka, Kenta Teruya, Jeong Kyu Bang, Saburo Aimoto, Tadashi Tatsumi, Hiroyuki Konno, Kazuto Nosaka, Kenichi Akaji

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)

Abstract

Core sequences necessary for substrate recognition and its inhibition at the PR/p3 site of HTLV-1 protease were clarified for the first time. From the cleavage rates of peptides containing a part of the PR/p3 site, a heptapeptide was found to be the minimal sequence required for substrate recognition. The use of synthetic inhibitors containing hydroxyethylamine dipeptide isostere indicated that a tetrapeptide sequence was necessary to achieve potent inhibition.

Original languageEnglish
Pages (from-to)3761-3764
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number14
DOIs
Publication statusPublished - 2006 Jul 15
Externally publishedYes

Keywords

  • HTLV-1 protease
  • Hydroxyethylamine dipeptide isostere
  • Inhibitor
  • Substrate specificity

ASJC Scopus subject areas

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

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