Current Strategies for the Discovery of K+ Channel Modulators

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.