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

• Published in: Drug discovery today Vol. 9; no. 24; pp. 1045 - 1054
• Main Authors: LI, Su, GOSLING, Martin, POLL, Chris T, WESTWICK, John, COX, Brian
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Science 15.12.2004
• Subjects: Animals; Biological and medical sciences; Cations - metabolism; Drug Design; General pharmacology; Humans; Ion Channel Gating - drug effects; Ion Channels - antagonists & inhibitors; Ion Channels - metabolism; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Technology, Pharmaceutical - methods; Technology, Pharmaceutical - trends; Ionic channel; Cations; Pharmaceutical technology; Treatment
• ISSN: 1359-6446; 1878-5832
• DOI: 10.1016/S1359-6446(04)03288-X

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.