Current Strategies for the Discovery of K+ Channel Modulators

Author(s): Deju Ye , Jiang Wang , Kunqian Yu , Yu Zhou , Hualiang Jiang , Kaixian Chen , Hong Liu .

Journal Name: Current Topics in Medicinal Chemistry

Volume 9 , Issue 4 , 2009

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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

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Article Details

Year: 2009
Page: [348 - 361]
Pages: 14
DOI: 10.2174/156802609788317865
Price: $58

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