Ion channels as therapeutic targets: a drug discovery perspective.

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Bagal SK, Brown AD, Cox PJ, Omoto K, Owen RM, Pryde DC, Sidders B, Skerratt SE, Stevens EB, Storer RI, Swain NA

Ion channels as therapeutic targets: a drug discovery perspective.

J Med Chem. 2013 Feb 14;56(3):593-624. doi: 10.1021/jm3011433. Epub 2012 Nov 29.

PubMed ID

23121096 [ View in PubMed

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Abstract

Ion channels are membrane proteins expressed in almost all living cells. The sequencing of the human genome has identified more than 400 putative ion channels, but only a fraction of these have been cloned and functionally tested. The widespread tissue distribution of ion channels, coupled with the plethora of physiological consequences of their opening and closing, makes ion-channel-targeted drug discovery highly compelling. However, despite some important drugs in clinical use today, as a class, ion channels remain underexploited in drug discovery and many existing drugs are poorly selective with significant toxicities or suboptimal efficacy. This Perspective seeks to review the ion channel family, its structural and functional features, and the diseases that are known to be modulated by members of the family. In particular, we will explore the structure and properties of known ligands and consider the future prospects for drug discovery in this challenging but high potential area.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Lacosamide	Sodium channel protein type 9 subunit alpha	IC 50 (nM)	182	N/A	N/A	Details
Zaleplon	Gamma-aminobutyric acid receptor subunit alpha-1	EC 50 (nM)	290	N/A	N/A	Details