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Ion Channel Drug Discovery

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Bottlenecks and potential improvements

28 September 2006 | By Carlo E.A. Jochems and Stefan Herzig, Department of Pharmacology, Faculty of Medicine, University of Köln

Ion channels are membrane proteins that regulate the entrance and departure of specific ions from cells, thus influencing the physiology of all cells. These ion flows also underlie electrical impulses required for sensory and motor functions of the brain, control of contraction of heart, skeletal, smooth and vascular muscle, as…

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A new approach to ion channel hit identification

11 November 2005 | By Martin J. Main, Karen Jones, Biological Chemistry, AstraZeneca R&D, UK, Mats A. Svensson, Dirk Weigelt and Markus Haeberlein, Chemistry, AstraZeneca R&D, Sweden

Advances in assay technology are driving an exciting new era in ion channel drug discovery. Here, we present a case study describing the use of computational chemistry and focussed library screening to drive rapid hit identification.

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The road ahead and how to get there

22 August 2005 | By James Herrington and Owen B. McManus, Department of Ion Channels, Laszlo Kiss, Pain Research, Merck Research Laboratories

Ion channels are membrane spanning proteins with narrow hydrophilic pores that support the passive flux of inorganic ions across the cell membrane.

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Patch clamp electrophysiology steps up a gear

20 May 2005 | By Derek J. Trezise, Assay Development & Compound Profiling, GlaxoSmithKline Research & Development

The advent of higher throughput patch clamp electrophysiology systems has begun to change the face of ion channel drug discovery. Systems such as IonWorksHT, PatchXpress and QPatch should allow electrophysiology to be re-positioned from an occasional reagent and compound ‘spot-check’ method, to a frontline gene expression analysis tool and drug…