title: Flux assays in high throughput screening of ion channels in drug discovery.
abstract: Ion channels have been identified as therapeutic targets in various disorders, such as cardiovascular disease, neurological disease, and cystic fibrosis. Flux assays to detect functional ionic flux through ion channels are becoming increasingly popular as tools for screening compounds. In an optimized flux assay, modulation of ion channel activity may produce readily detectable changes in radiolabeled or nonradiolabeled ionic flux. Technologies based on flux assays are currently available in a fully automated high throughput format for efficient screening. This application offers sensitive, precise, and reproducible measurements giving accurate drug rank orders matching those of patch clamp data. Conveniently, the flux assay is amenable to adaptation for different ion channels, such as potassium, sodium, calcium, and chloride channels, by using suitable tracer ions. The nonradiolabeled rubidium-based flux assay coupled with the ion channel reader (ICR) technology has become very successful in ion channel activity analysis and is emerging as a popular technique in modern drug discovery.
authors.affiliation: Aurora Biomed Inc, Vancouver, BC, Canada. gill@aurorabiomed.com
authors.forename: Sikander
authors.initials: S
authors.lastname: Gill
authors.forename: Raj
authors.initials: R
authors.lastname: Gill
authors.forename: Soo Sen
authors.initials: SS
authors.lastname: Lee
authors.forename: J Christian
authors.initials: JC
authors.lastname: Hesketh
authors.forename: David
authors.initials: D
authors.lastname: Fedida
authors.forename: Saman
authors.initials: S
authors.lastname: Rezazadeh
authors.forename: Larisa
authors.initials: L
authors.lastname: Stankovich
authors.forename: Dong
authors.initials: D
authors.lastname: Liang
mesh_terms: D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000295:instrumentation / Q000379:methods*; D006801:Humans; D007473:Ion Channels / Q000032:analysis / Q000187:drug effects* / Q000502:physiology*; D017136:Ion Transport / Q000187:drug effects* / Q000502:physiology*; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D018408:Patch-Clamp Techniques / Q000295:instrumentation / Q000379:methods*; D011869:Radioligand Assay / Q000295:instrumentation / Q000379:methods*; D013050:Spectrometry, Fluorescence / Q000295:instrumentation / Q000379:methods*; D013673:Technology Assessment, Biomedical
chemical_list: D007473:Ion Channels