Chlorpromazine binding to the PAS domains uncovers the effect of ligand modulation on EAG channel activity
Zejun Wang, Stephanie M. Soohoo, Purushottam B. Tiwari, Grzegorz Piszczek, Tinatin I. Brelidze
Abstract
channels and places the PAS domain as a new target for drug discovery in EAG and related channels. Up-regulation of EAG channel activity is linked to cancer and neurological disorders. Our study raises the possibility of repurposing the antipsychotic drug chlorpromazine for treatment of neurological disorders and cancer.
Topics & Concepts
GatingLigand (biochemistry)ChemistryPotassium channelBiophysicsInward-rectifier potassium ion channelIon channelTRPC1XenopusCell biologyBiochemistryBiologyReceptorGeneIon channel regulation and functionNeuroscience and Neuropharmacology ResearchCardiac electrophysiology and arrhythmias