Abstract
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 smallmolecular 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.
Keywords: Potassium channels, modulator, blocker, opener, virtual screening, chemistry strategy, MAOS
Current Topics in Medicinal Chemistry
Title: Current Strategies for the Discovery of K+ Channel Modulators
Volume: 9 Issue: 4
Author(s): Deju Ye, Jiang Wang, Kunqian Yu, Yu Zhou, Hualiang Jiang, Kaixian Chen and Hong Liu
Affiliation:
Keywords: Potassium channels, modulator, blocker, opener, virtual screening, chemistry strategy, MAOS
Abstract: 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 smallmolecular 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.
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Cite this article as:
Ye Deju, Wang Jiang, Yu Kunqian, Zhou Yu, Jiang Hualiang, Chen Kaixian and Liu Hong, Current Strategies for the Discovery of K+ Channel Modulators, Current Topics in Medicinal Chemistry 2009; 9 (4) . https://dx.doi.org/10.2174/156802609788317865
DOI https://dx.doi.org/10.2174/156802609788317865 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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