Design of new inhibitors for CDC2 kinase based on a multiple pseudosubstrate structure

被引:15
|
作者
Sasaki, S [1 ]
Hashimoto, T
Obana, N
Yasuda, H
Uehara, Y
Maeda, A
机构
[1] Kyushu Univ, Fac Pharmaceut Sci, Fukuoka 8128582, Japan
[2] Tokyo Univ Pharm & Life Sci, Sch Life Sci, Hachioji, Tokyo 19203, Japan
[3] Natl Inst Infect Dis, Tokyo 162, Japan
关键词
D O I
10.1016/S0960-894X(98)00163-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different structural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys-Lys-NHMe, and ethyloxy group between the two components. Inhibitory activities toward cdc2 and other protein kinases were investigated, and the compound (21) with Ac-Cys-Pro-Lys-Lys-NHMe connected with the triethylene glycol spacer exhibited the most potent inhibition with relatively high selectivity. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1019 / 1022
页数:4
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