title: Contribution of Automated Technologies to Ion Channel Drug Discovery.
abstract: Automated technologies are now resolving the historical relegation that ion channels have endured as targets for the new drug discovery and development global efforts. The richness and adequacy of functional assay methodologies, remarkably fluorescence-based detection of ions fluxes and patch-clamp electrophysiology recording of ionic currents, are now automated and increasingly employed for the analysis of ion channel activity. While the former is currently the most commonly applied, the latter is finally reaching the throughput capacity to be engaged in the primary screening of chemical libraries conformed by hundreds of thousands of compounds. The use of automated instrumentation for the study of ion channel functionality (and dysfunctionality), particularly in the search for novel pharmacological agents with therapeutic purposes, has now reached out beyond the industrial setting, its original natural enclave, and is making its way into a growing number of academic labs and core facilities. The present chapter reviews the increasing contributions accomplished by a variety of different key automated technologies which have revolutionized the strategies to approach the discovery and development of new drugs targeting ion channels.
authors.affiliation: Laboratorio Nacional de Canalopatías, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, México City, Mexico. Electronic address: arturopicones@yahoo.com.
authors.forename: Arturo
authors.initials: A
authors.lastname: Picones
authors.affiliation: Laboratorio Nacional de Canalopatías, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, México City, Mexico.
authors.forename: Arlet
authors.initials: A
authors.lastname: Loza-Huerta
authors.affiliation: Laboratorio Nacional de Canalopatías, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, México City, Mexico.
authors.forename: Pedro
authors.initials: P
authors.lastname: Segura-Chama
authors.affiliation: Laboratorio Nacional de Canalopatías, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, México City, Mexico.
authors.forename: Cesar O
authors.initials: CO
authors.lastname: Lara-Figueroa
mesh_terms: D055808:Drug Discovery / Q000379:methods*; D004594:Electrophysiology / Q000379:methods; D005453:Fluorescence; D006801:Humans; D007473:Ion Channels / Q000737:chemistry / Q000378:metabolism*; D058990:Molecular Targeted Therapy; D018408:Patch-Clamp Techniques / Q000379:methods; D054852:Small Molecule Libraries / Q000737:chemistry / Q000378:metabolism
chemical_list: D007473:Ion Channels; D054852:Small Molecule Libraries
keywords: Automated patch-clamp; Drug discovery; Fluorescence-based assays; High-throughput screening; Ion channels