Evaluation of series of isobenzofuranone dimers as PKCα ligands:: implication for the distance between the two ligand binding sites

被引:13
作者
Baba, Y
Mayumi, S
Hirai, G
Kawasaki, H
Ogoshi, Y
Yanagisawa, T
Hashimoto, Y
Sodeoka, M
机构
[1] Tohoku Univ, IMRAM, Sendai, Miyagi 9808577, Japan
[2] Sagami Chem Res Ctr, Kanagawa, Japan
[3] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan
基金
日本学术振兴会;
关键词
D O I
10.1016/j.bmcl.2004.02.098
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl chain dimers having a C-10-C-12 linker and for the C7 dimers having a C-14-C-16. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2969 / 2972
页数:4
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