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Two-Pore Domain Potassium Channels as Drug Targets: Anesthesia and Beyond

Mathie, Alistair, Veale, Emma L., Cunningham, Kevin P., Holden, Robyn G., Wright, Paul D. (2020) Two-Pore Domain Potassium Channels as Drug Targets: Anesthesia and Beyond. Annual Review of Pharmacology and Toxicology, 61 (1). ISSN 0362-1642. (doi:10.1146/annurev-pharmtox-030920-111536) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:82272)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided. (Contact us about this Publication)
Official URL
https://doi.org/10.1146/annurev-pharmtox-030920-11...

Abstract

Two-pore domain potassium (K2P) channels stabilize the resting membrane potential of both excitable and nonexcitable cells and, as such, are important regulators of cell activity. There are many conditions where pharmacological regulation of K2P channel activity would be of therapeutic benefit, including, but not limited to, atrial fibrillation, respiratory depression, pulmonary hypertension, neuropathic pain, migraine, depression, and some forms of cancer. Up until now, few if any selective pharmacological regulators of K2P channels have been available. However, recent publications of solved structures with small-molecule activators and inhibitors bound to TREK-1, TREK-2, and TASK-1 K2P channels have given insight into the pharmacophore requirements for compound binding to these sites. Together with the increasing availability of a number of novel, active, small-molecule compounds from K2P channel screening programs, these advances have opened up the possibility of rational activator and inhibitor design to selectively target K2P channels.

Item Type: Article
DOI/Identification number: 10.1146/annurev-pharmtox-030920-111536
Subjects: R Medicine > RM Therapeutics. Pharmacology
Divisions: Divisions > Division of Natural Sciences > Medway School of Pharmacy
Depositing User: Alistair Mathie
Date Deposited: 29 Jul 2020 10:53 UTC
Last Modified: 16 Feb 2021 14:14 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/82272 (The current URI for this page, for reference purposes)
Mathie, Alistair: https://orcid.org/0000-0001-6094-2890
Veale, Emma L.: https://orcid.org/0000-0002-6778-9929
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