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Therapeutic scope of modulation of non-voltage-gated cation channels.

Li, Su and Gosling, Martin and Poll, Chris and Westwick, John and Cox, Brian (2005) Therapeutic scope of modulation of non-voltage-gated cation channels. Drug Discovery Today, 10 (2). pp. 129-137. ISSN 1359-6446

Abstract

Although widely regarded as attractive drug targets, less than a tenth of known ion channels are currently commercially exploited as therapeutic targets. Historically, drug discovery efforts on ion channel targets have been encumbered by a lack of molecular and structural information, sub-optimal screening technologies and a paucity of discriminating pharmacological tools. Although challenges remain, recent scientific and technological advances in the area of ion channel research and screening offer the exciting prospect of a new, more-predictive era of ion channel drug discovery. In this article, focusing primarily on non voltage gated cation channels, we describe the continuing evolution of approaches to ion channel drug discovery, highlight recent developments in the ion channel field and consider their potential impact on discovering and ascribing function to ion channel targets. We discuss the renaissance of known ion channel targets, such as nicotinic acetylcholine receptors and calcium-activated potassium channels, as well as the emergence of the transient receptor potential (TRP) channels as a gene family of cation channels with broad therapeutic potential.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Ion channels; Non-voltage gated cation channels; Electrophysiology; Hydroxytryptamine receptors; Sulfonylurea; Drug Discovery; Pharmaceutical Science; Biochemistry; Chemical Biology
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Date Deposited: 14 Dec 2009 13:56
Last Modified: 14 Dec 2009 13:56
URI: https://oak.novartis.com/id/eprint/665

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