Identification of undecylenic acid as EAG channel inhibitor using surface plasmon resonance-based screen of KCNH channels.

ABSTRACT:

Background

KCNH family of potassium channels is responsible for diverse physiological functions ranging from the regulation of neuronal excitability and cardiac contraction to the regulation of cancer progression. KCNH channels contain a Per-Arn-Sim (PAS) domain in their N-terminal and cyclic nucleotide-binding homology (CNBH) domain in their C-terminal regions. These intracellular domains shape the function of KCNH channels and are important targets for drug development.

Methods

Here we describe a surface plasmon resonance (SPR)-based screening method aimed in identifying small molecule binders of PAS and CNBH domains for three KCNH channel subfamilies: ether-à-go-go (EAG), EAG-related gene (ERG), and EAG-like K+ (ELK). The method involves purification of the PAS and CNBH d

SUBMITTER: Wang ZJ 

PROVIDER: S-EPMC6637479 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature