Potassium Channels

Potassium channel blockers and openers target the largest and most diverse family of ion channels. Potassium (K+) channels set the resting membrane potential and shape action potentials, hormone secretion and immune cell activation. The 1998 crystal structure of the potassium channel from Streptomyces lividans (KcsA) showed how a narrow selectivity filter passes K+ ions but excludes sodium ions. Major families include voltage-gated (Kv), calcium-activated (KCa) and inward-rectifier (Kir) channels. Adenosine triphosphate (ATP)-sensitive K+ (KATP) channels pair a Kir6.2 pore with a sulfonylurea receptor (SUR) subunit. The sulfonylureas glimepiride and glyburide close KATP channels, whereas minoxidil is studied as a channel opener. TRAM-34 blocks the intermediate-conductance KCa3.1 channel, and PAP-1 blocks Kv1.3, two channels studied in T lymphocyte activation.

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