Article
Analogs of MK-499 are differentially affected by a mutation in the S6 domain of the hERG K+ channel.
Biochemical pharmacology - 15 May 2009
Karczewski Jerzy, Wang Jixin, Kane Stefanie A, Kiss Laszlo, Koblan Kenneth S, Culberson J Christopher, Spencer Robert H
Abstract excerpt
Drug-induced long QT syndrome has been principally ascribed to block of the cardiac hERG K(+) channel. Methanesulfonanilides, such as MK-499, E-4031 and dofetilide, are potent hERG antagonists that likely bind along the S6 helix within the inner vestibule of the pore. To further investigate these...
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