Literature DB >> 27038379

Contribution of Automated Technologies to Ion Channel Drug Discovery.

Arturo Picones1, Arlet Loza-Huerta2, Pedro Segura-Chama2, Cesar O Lara-Figueroa2.   

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.
© 2016 Elsevier Inc. All rights reserved.

Keywords:  Automated patch-clamp; Drug discovery; Fluorescence-based assays; High-throughput screening; Ion channels

Mesh:

Substances:

Year:  2016        PMID: 27038379     DOI: 10.1016/bs.apcsb.2016.01.002

Source DB:  PubMed          Journal:  Adv Protein Chem Struct Biol        ISSN: 1876-1623            Impact factor:   3.507


  4 in total

1.  Ion channels find a pathway for therapeutic success.

Authors:  Maria L Garcia; Gregory J Kaczorowski
Journal:  Proc Natl Acad Sci U S A       Date:  2016-05-04       Impact factor: 11.205

Review 2.  Bringing new dimensions to drug discovery screening: impact of cellular stimulation technologies.

Authors:  Elena Molokanova; Mark Mercola; Alex Savchenko
Journal:  Drug Discov Today       Date:  2017-02-04       Impact factor: 7.851

3.  In Silico Assessment of Efficacy and Safety of IKur Inhibitors in Chronic Atrial Fibrillation: Role of Kinetics and State-Dependence of Drug Binding.

Authors:  Nicholas Ellinwood; Dobromir Dobrev; Stefano Morotti; Eleonora Grandi
Journal:  Front Pharmacol       Date:  2017-11-07       Impact factor: 5.810

Review 4.  Physiological Roles and Therapeutic Potential of Ca2+ Activated Potassium Channels in the Nervous System.

Authors:  Aravind S Kshatri; Alberto Gonzalez-Hernandez; Teresa Giraldez
Journal:  Front Mol Neurosci       Date:  2018-07-30       Impact factor: 5.639

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.