Assay technologies for screening ion channel targets.
The sequence of the human genome will soon provide researchers with hundreds of new ion channel genes. To create a successful ion channel drug discovery program, it is necessary to quickly develop reliable and robust high-throughput screening (HTS) assays for those ion channels implicated in important diseases. Ion channels are dynamic proteins, and therefore require assays that 'sense' their various functional states. Competition-binding assays, although successfully used for other target classes, often fail to identify ligands that modulate specific ion channel functions. Cell-based functional assays, therefore, are preferred for HTS of ion channel targets. In this review, we evaluate the various cell-based assays available for ion channels, and discuss future directions for assay improvements.
Mattheakis
L C
LC
Affymax Research Institute, 4001 Miranda Ave, Palo Alto, CA 94304, USA. lmattheakis@qdots.com
Savchenko
A
A
D000818:Animals; D001681:Biological Assay / Q000379:methods; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004594:Electrophysiology / Q000295:instrumentation / Q000379:methods*; D006801:Humans; D007473:Ion Channels / Q000187:drug effects / Q000378:metabolism / Q000502:physiology*
D007473:Ion Channels