Conduction and block of inward rectifier K+ channels: Predicted structure of a potent blocker of kir2.1
Dysfunction of Kir2.1, thought to be the major component of inward currents, IK1, in the heart, has been linked to various channelopathies, such as short Q-T syndrome. Unfortunately, currently no known blockers of Kir2.x channels exist. In contrast, Kir1.1b, predominantly expressed in the kidney, is potently blocked by an oxidation-resistant mutant of the honey bee toxin tertiapin (tertiapin-Q). Using various computational tools, we show that both channels are closed by a hydrophobic gating...[Show more]
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