Abstract
Ion channels are a large superfamily of membrane proteins that pass ions across membranes. They are critical to diverse physiological functions in both excitable and nonexcitable cells and underlie many diseases. As a result, they are an important target class which is proven to be highly “druggable”. However, for high throughput screening (HTS), ion channels are historically difficult as a target class due to their unique molecular properties and the limitations of assay technologies that are HTS-amendable. In this article, we describe the background of ion channels and current status and challenges for ion channel drug discovery, followed by an overview of both conventional and newly emerged ion channel screening technologies. The critical impact of such new technologies on current and future ion channel drug discovery is also discussed.
Keywords: Ion channel, automated patch clamp, high throughput screening, electrophysiology, drug discovery
Combinatorial Chemistry & High Throughput Screening
Title: Impact of Novel Screening Technologies on Ion Channel Drug Discovery
Volume: 11 Issue: 3
Author(s): Qiang Lu and W. Frank An
Affiliation:
Keywords: Ion channel, automated patch clamp, high throughput screening, electrophysiology, drug discovery
Abstract: Ion channels are a large superfamily of membrane proteins that pass ions across membranes. They are critical to diverse physiological functions in both excitable and nonexcitable cells and underlie many diseases. As a result, they are an important target class which is proven to be highly “druggable”. However, for high throughput screening (HTS), ion channels are historically difficult as a target class due to their unique molecular properties and the limitations of assay technologies that are HTS-amendable. In this article, we describe the background of ion channels and current status and challenges for ion channel drug discovery, followed by an overview of both conventional and newly emerged ion channel screening technologies. The critical impact of such new technologies on current and future ion channel drug discovery is also discussed.
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Cite this article as:
Lu Qiang and An Frank W., Impact of Novel Screening Technologies on Ion Channel Drug Discovery, Combinatorial Chemistry & High Throughput Screening 2008; 11 (3) . https://dx.doi.org/10.2174/138620708783877735
DOI https://dx.doi.org/10.2174/138620708783877735 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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