Small-molecule modulators of inward rectifier K+ channels: recent advances and future possibilities.

Bhave G, Lonergan D, Chauder BA, Denton JS
Future Med Chem. 2010 2 (5): 757-74

PMID: 20543968 · PMCID: PMC2883187 · DOI:10.4155/fmc.10.179

Inward rectifier potassium (Kir) channels have been postulated as therapeutic targets for several common disorders including hypertension, cardiac arrhythmias and pain. With few exceptions, however, the small-molecule pharmacology of this family is limited to nonselective cardiovascular and neurologic drugs with off-target activity toward inward rectifiers. Consequently, the actual therapeutic potential and 'drugability' of most Kir channels has not yet been determined experimentally. The purpose of this review is to provide a comprehensive summary of publicly disclosed Kir channel small-molecule modulators and highlight recent targeted drug-discovery efforts toward Kir1.1 and Kir2.1. The review concludes with a brief speculation on how the field of Kir channel pharmacology will develop over the coming years and a discussion of the increasingly important role academic laboratories will play in this progress.

MeSH Terms (6)

Animals Drug Discovery Humans Models, Molecular Potassium Channels, Inwardly Rectifying Small Molecule Libraries

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