Article
NS1643 interacts around L529 of hERG to alter voltage sensor movement on the path to activation.
Biophysical journal - 24 Mar 2015
Guo Jiqing, Cheng Yen May, Lees-Miller James P, Perissinotti Laura L, Claydon Tom W, Hull Christina M, Thouta Samrat, Roach Daniel E, Durdagi Serdar, Noskov Sergei Y, Duff Henry J
Abstract excerpt
Activators of hERG1 such as NS1643 are being developed for congenital/acquired long QT syndrome. Previous studies identify the neighborhood of L529 around the voltage-sensor as a putative interacting site for NS1643. With NS1643, the V1/2 of activation of L529I (-34 ± 4 mV) is similar to wild-type (WT) (-37 ± 3 mV; P > 0.05). WT and L529I showed no difference in the slope factor in the absence of NS1643 (8 ± 0...
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