Abstract
Ion channels are at present the third biggest target class in drug discovery. Primary research is continually uncovering potential new ion channel targets in indications such as cancer, diabetes and respiratory diseases, as well as the more established fields of pain, cardiovascular disease, and neurological disorders. Despite the physiological significance and therapeutic relevance in a wide variety of biological systems, ion channels still remain under exploited as drug targets. This is to a large extent resulting from the historical lack of screening technologies to provide the throughput and quality of data required to support medicinal chemistry. Although technical challenges still lie ahead, this historic bottleneck in ion channel drug discovery is now being overcome by novel technologies that can be integrated into lead generation stages of ion channel drug discovery to allow the development of novel therapeutic agents. This review describes the variety of technologies available for ion channel screening and discusses the opportunities these technologies provide. The challenges that remain to be addressed are highlighted.
Keywords: Ion channels, targets, drug discovery, screening technologies, automated electrophysiology platforms, fluorescence dye assays, ion flux assays
CNS & Neurological Disorders - Drug Targets
Title: Ion Channel Screening Technology
Volume: 7 Issue: 2
Author(s): Michael A. Dabrowski, Kim Dekermendjian, Per-Eric Lund, Johannes J. Krupp, Jon Sinclair and Olof Larsson
Affiliation:
Keywords: Ion channels, targets, drug discovery, screening technologies, automated electrophysiology platforms, fluorescence dye assays, ion flux assays
Abstract: Ion channels are at present the third biggest target class in drug discovery. Primary research is continually uncovering potential new ion channel targets in indications such as cancer, diabetes and respiratory diseases, as well as the more established fields of pain, cardiovascular disease, and neurological disorders. Despite the physiological significance and therapeutic relevance in a wide variety of biological systems, ion channels still remain under exploited as drug targets. This is to a large extent resulting from the historical lack of screening technologies to provide the throughput and quality of data required to support medicinal chemistry. Although technical challenges still lie ahead, this historic bottleneck in ion channel drug discovery is now being overcome by novel technologies that can be integrated into lead generation stages of ion channel drug discovery to allow the development of novel therapeutic agents. This review describes the variety of technologies available for ion channel screening and discusses the opportunities these technologies provide. The challenges that remain to be addressed are highlighted.
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Cite this article as:
Dabrowski A. Michael, Dekermendjian Kim, Lund Per-Eric, Krupp J. Johannes, Sinclair Jon and Larsson Olof, Ion Channel Screening Technology, CNS & Neurological Disorders - Drug Targets 2008; 7 (2) . https://dx.doi.org/10.2174/187152708784083867
DOI https://dx.doi.org/10.2174/187152708784083867 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
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