Modulators of Large-Conductance Calcium-Activated Potassium (BK) Channels as Potential Therapeutic Targets

BK channels are large conductance calcium-activated potassium channels that are found in many tissues, including excitable cells such as myocytes and neurons. The high conductance and dependence on calcium of BK channels suggests that modulation of these channels may have a pronounced effect on tissues in which they are expressed. Within the past four years, a variety of small molecules and natural product-derived modulators of BK channels have been described. This review will focus on compounds which are openers and blockers of BK channels and their therapeutic potential, with introductory sections covering the biophysics, pharmacology and molecular biology of BK channels.