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

doi:10.1016/j.bmcl.2006.04.056

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 journal › Article › peer-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 language	English
Pages (from-to)	3761-3764
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2006.04.056
Publication status	Published - 2006 Jul 15
Externally published	Yes

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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Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease. / Naka, Hiromi; Teruya, Kenta; Bang, Jeong Kyu; Aimoto, Saburo; Tatsumi, Tadashi; Konno, Hiroyuki; Nosaka, Kazuto; Akaji, Kenichi.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 14, 15.07.2006, p. 3761-3764.

Research output: Contribution to journal › Article › peer-review

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