Impact of novel screening technologies on ion channel drug discovery.
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.
Lü
Qiang
Q
Lead Finding Platform, Novartis Institutes for BioMedical Research, 250 Mass. Ave., Cambridge, MA 02139, USA. qiang.lu@novartis.com
An
W Frank
WF
D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000295:instrumentation / Q000379:methods* / Q000639:trends; D004594:Electrophysiology / Q000379:methods; D006801:Humans; D007473:Ion Channels / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000502:physiology; D018408:Patch-Clamp Techniques; D054852:Small Molecule Libraries; D013050:Spectrometry, Fluorescence / Q000379:methods
D007473:Ion Channels; D054852:Small Molecule Libraries