A "Target Class" Screen to Identify Activators of Two-Pore Domain Potassium (K2P) Channels.

ABSTRACT: Two-pore domain potassium (K2P) channels carry background (or leak) potassium current and play a key role in regulating resting membrane potential and cellular excitability. Accumulating evidence points to a role for K2Ps in human pathophysiologies, most notably in pain and migraine, making them attractive targets for therapeutic intervention. However, there remains a lack of selective pharmacological tools. The aim of this work was to apply a "target class" approach to investigate the K2P superfamily and identify novel activators across all the described subclasses of K2P channels. Target class drug discovery allows for the leveraging of accumulated knowledge and maximizing synergies across a family of targets and serves as an additional approach to standard target-based screening. A comm

SUBMITTER: McCoull D 

PROVIDER: S-EPMC7900820 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature