Current Strategies for the Discovery of K+ Channel Modulators
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: MAOS; Potassium channels; blocker; chemistry strategy; modulator; opener; virtual screening
Document Type: Research Article
Affiliations: Shanghai Institute of Materia Medica, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203.
Publication date: 01 March 2009
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