Histidine at position 462 determines the low quinine sensitivity of ether-a-go-go channel superfamily member K_v 12.1.

ABSTRACT:

Background and purpose

The ether-à-go-go (Eag) K_v superfamily comprises closely related K_v 10, K_v 11, and K_v 12 subunits. K_v 11.1 (termed hERG in humans) gained much attention, as drug-induced inhibition of these channels is a frequent cause of sudden death in humans. The exclusive drug sensitivity of K_v 11.1 can be explained by central drug-binding pockets that are absent in most other channels. Currently, it is unknown whether K_v 12 channels are equipped with an analogous drug-binding pocket and whether drug-binding properties are conserved in all Eag superfamily members.

Experimental approach

We analysed sensitivity of recombinant K_v 12.1 channels to quinine, a substituted quinoline th

SUBMITTER: Dierich M 

PROVIDER: S-EPMC6609544 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature