Two-pore domain potassium channels as drug targets: anesthesia and beyond

Mathie, Alistair, Veale, Emma L, Cunningham, Kevin P, Holden, Robyn G and Wright, Paul D (2021) Two-pore domain potassium channels as drug targets: anesthesia and beyond. Annual review of pharmacology and toxicology, 61. pp. 401-420. ISSN 1545-4304

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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
Uncontrolled Keywords: K2P channel, inhalational anesthetic, negatively charged activators, cryptic binding site, TREK channels, TASK channels
Subjects: R Medicine > RM Therapeutics. Pharmacology
Divisions: Faculty of Health & Science > Department of Health Studies
Depositing User: Alistair Mathie
Date Deposited: 01 Mar 2021 10:47
Last Modified: 01 Mar 2021 10:47

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