Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease
Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease
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DOI：
10.1016/j.bmcl.2006.04.056
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发表时间：
2006-07-15
影响因子：
2.7
通讯作者：
Akaji, Kenichi
中科院分区：
文献类型：
--
作者：
Naka, Hiromi;Teruya, Kenta;Akaji, Kenichi
首次阐明了HTLV-1蛋白酶PR/p3位点底物识别及其抑制所必需的核心序列。从含有PR/p3位点的一部分的肽的切割速率，发现七肽是底物识别所需的最小序列。使用含有羟乙胺二肽等排体的合成抑制剂表明，四肽序列是实现有效抑制所必需的。(c)2006爱思唯尔有限公司保留所有权利。
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.