Current Strategies for the Discovery of K+ Channel Modulators

被引：7

作者：

Ye, Deju ^{[1
]}

Wang, Jiang ^{[1
]}

Yu, Kunqian ^{[1
]}

Zhou, Yu ^{[1
]}

Jiang, Hualiang ^{[1
,2
]}

Chen, Kaixian ^{[1
]}

Liu, Hong ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res,Ctr Drug Discovery & Desig, Shanghai 201203, Peoples R China

[2] E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2009年 / 9卷 / 04期

基金：

中国国家自然科学基金;

关键词：

Potassium channels; modulator; blocker; opener; virtual screening; chemistry strategy; MAOS; KV1.5 POTASSIUM CHANNEL; 1,4-BENZOXAZINE DERIVATIVES; DYNAMICS SIMULATIONS; CRYSTAL-STRUCTURE; DRUG DISCOVERY; ION CHANNELS; IN-VIVO; BLOCKERS; CHEMISTRY; SHAKER;

D O I：

10.2174/156802609788317865

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potassium ion (K+) channels consist of a ubiquitous family of membrane proteins that play critical roles in a wide variety of physiological processes, such as the regulation of neuronal excitability, muscle contraction, cell proliferation, and insulin secretion. Due to their pivotal functions in biological systems, K+ channels have long been attractive targets for the rational drug design on the basis of their structures and interaction mechanisms. Various small-molecular compounds and toxins have been discovered to act as K+ channel modulators. In the present review, we will first briefly discuss current knowledge of the structures and functions of K+ channels, and then review the recent strategies for the discovery of K+ channel modulators, focusing especially on the virtual screening approaches and chemical synthesis technologies.

引用

页码：348 / 361

页数：14