Importance of interaction between C1 domain and lipids in protein kinase Cα activation:: Hydrophobic side chain direction in isobenzofuranone ligands controls enzyme activation level

被引:11
作者
Hirai, Go
Shimizu, Tadashi
Watanabe, Toru
Ogoshi, Yosuke
Ohkubo, Megumi
Sodeoka, Mikiko
机构
[1] Synthetic Organic Chemistry Laboratory, RIKEN, Wako-shi, Saitama 351-0198, 2-1, Hirosawa
[2] Institute of Multidisciplinary Research for Advanced Materials, Tohoku University, Aoba, Sendai, Miyagi 980-8577
关键词
D O I
10.1002/cmdc.200700080
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Substituent direction is important: Type A-D isobenzofuranone derivatives were synthesized with differently directed hydrophobic alkyl side chains. These ligands bind in a similar conformation to protein kinase Cα but have contrasting activation abilities, possibly owing to different interaction of the side chain with the membrane lipid. (Chemical Equation Presented) © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:1006 / 1009
页数:4
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