Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors
Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors
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DOI：
10.1016/j.bmcl.2007.04.019
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发表时间：
2007-06-15
影响因子：
2.7
通讯作者：
Kiso, Yoshiaki
中科院分区：
文献类型：
--
作者：
Kimura, Tooru;Nguyen, Jeffrey-Tri;Kiso, Yoshiaki
人类T细胞白血病病毒1型（HTLV-I）导致成人T细胞白血病和几种严重的慢性疾病。HTLV-I蛋白酶（PR）抑制作用可阻止病毒的繁殖。本文中，对有效的八肽HTLV-1 PR抑制剂KNI-10161进行截短研究，以衍生活性有所损失的小的六肽KNI-10127。对化合物KNI-10127进行残基取代研究后，在抑制剂KNI-10166中恢复了HTLV-I PR抑制活性。(c)2007爱思唯尔有限公司保留所有权利。
The human T-cell leukemia virus type 1 (HTLV-I) causes adult T-cell leukemia and several severe chronic diseases. HTLV-I protease (PR) inhibition stops the propagation of the virus. Herein, truncation studies were performed on potent octapeptidie HTLV-I PR inhibitor KNI-10161 to derive small hexapeptide KNI-10127 with some loss in activity. After performing residue-substitution studies on compound KNI-10127, HTLV-I PR inhibitory activity was recovered in inhibitor KNI-10166. (c) 2007 Elsevier Ltd. All rights reserved.