Pharmacological approaches to studying potassium channels

Mathie, Alistair, Veale, Emma L, Golluscio, Alessia, Holden, Robyn G and Walsh, Yvonne (2021) Pharmacological approaches to studying potassium channels. In: Handbook of Experimental Pharmacology. Springer, pp. 83-111. ISBN 0171-2004

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In this review, we consider the pharmacology of potassium channels from the perspective of these channels as therapeutic targets. Firstly, we describe the three main families of potassium channels in humans and disease states where they are implicated. Secondly, we describe the existing therapeutic agents which act on potassium channels and outline why these channels represent an under-exploited therapeutic target with potential for future drug development. Thirdly, we consider the evidence desired in order to embark on a drug discovery programme targeting a particular potassium channel. We have chosen two "case studies": activators of the two-pore domain potassium (K) channel TREK-2 (K10.1), for the treatment of pain and inhibitors of the voltage-gated potassium channel K1.3, for use in autoimmune diseases such as multiple sclerosis. We describe the evidence base to suggest why these are viable therapeutic targets. Finally, we detail the main technical approaches available to characterise the pharmacology of potassium channels and identify novel regulatory compounds. We draw particular attention to the Comprehensive in vitro Proarrhythmia Assay initiative (CiPA, ) project for cardiac safety, as an example of what might be both desirable and possible in the future, for ion channel regulator discovery projects.

Item Type: Book Section
Uncontrolled Keywords: CiPA, Kv1.3, Patch-clamp electrophysiology, Potassium channel, TREK-2, hERG
Subjects: Q Science > QP Physiology
R Medicine > RM Therapeutics. Pharmacology
Divisions: Faculty of Health & Science > Department of Science & Technology
Depositing User: Alistair Mathie
Date Deposited: 19 Jul 2021 10:30
Last Modified: 02 Feb 2023 10:23

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