Current Strategies for the Discovery of K+ Channel Modulators

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.