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

被引:10
作者
Naka, Hiromi
Teruya, Kenta
Bang, Jeong Kyu
Aimoto, Saburo
Tatsumi, Tadashi
Konno, Hiroyuki
Nosaka, Kazuto
Akaji, Kenichi [1 ]
机构
[1] Kyoto Prefectural Univ Med, Kyoto 6038334, Japan
[2] Osaka Univ, Inst Prot Res, Suita, Osaka 5650871, Japan
关键词
HTLV-1; protease; inhibitor; hydroxyethylamine dipeptide isostere; substrate specificity;
D O I
10.1016/j.bmcl.2006.04.056
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3761 / 3764
页数:4
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