Article
Pore Polarity and Charge Determine Differential Block of Kir1.1 and Kir7.1 Potassium Channels by Small-Molecule Inhibitor VU590.
Molecular pharmacology - 1 Sept 2017
Kharade Sujay V, Sheehan Jonathan H, Figueroa Eric E, Meiler Jens, Denton Jerod S
Abstract excerpt
VU590 was the first publicly disclosed, submicromolar-affinity (IC50 = 0.2 μM), small-molecule inhibitor of the inward rectifier potassium (Kir) channel and diuretic target, Kir1.1. VU590 also inhibits Kir7.1 (IC50 ∼ 8 μM), and has been used to reveal new roles for Kir7.1 in regulation of myometrial contractility and melanocortin signaling. Here, we employed molecular modeling, mutagenesis, and patch clamp...
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