Literature DB >> 25062795

New strategies in ion channel screening for drug discovery: are there ways to improve its productivity?

Cecilia Farre1, Niels Fertig.   

Abstract

INTRODUCTION: From a drug discovery point of view, ion channels are very interesting and challenging targets. Over the past decade, great efforts have been made in developing platforms for patch clamp-based high-quality screening of ion channels in discovering new drug candidates as well for evaluating their safety profiles. Indeed, the automated patch clamp (APC) has recently reached the data throughput requirements of high-throughput screening (HTS) allowing for new screening strategies with ion channel active compounds. AREAS COVERED: This editorial article comments on the past and present developments of APC-based drug screening. Furthermore, it also looks at the implications of APC technology meeting HTS-standards as well as its use in compound safety evaluation. EXPERT OPINION: In the imminent future, we will see a paradigm shift in ion channel drug screening toward using APC-based platforms for primary drug library screens. This way, the redundancy of the drug discovery process and the risk of false-negatives could be drastically reduced. Furthermore, cardiac safety can be addressed early, avoiding late-phase withdrawals with promising drug candidates. It is our firm belief that APC-based ion channel HTS will facilitate the discovery of candidates, which otherwise would have not been found, and shorten the drug development cycle, saving time and cost.

Keywords:  automated patch clamp; drug discovery; high-throughput screening; ion channel screening

Mesh:

Substances:

Year:  2014        PMID: 25062795     DOI: 10.1517/17460441.2014.942217

Source DB:  PubMed          Journal:  Expert Opin Drug Discov        ISSN: 1746-0441            Impact factor:   6.098


  5 in total

1.  Dynamics of T-Junction Solution Switching Aimed at Patch Clamp Experiments.

Authors:  Jerónimo A Auzmendi; Mariano Smoler; Luciano Moffatt
Journal:  PLoS One       Date:  2015-07-15       Impact factor: 3.240

2.  Carcinoid heart disease involving the left heart: a case report and biomarker analysis.

Authors:  Michael Lichtenauer; Tristan Pichler; Sarah Eder; Moritz Mirna; Theresa Magnes; Bernhard Wernly; Vera Paar; Christian Jung; Erika Prinz; Rainald Seitelberger; Uta C Hoppe
Journal:  ESC Heart Fail       Date:  2019-01-08

3.  Identification of small-molecule ion channel modulators in C. elegans channelopathy models.

Authors:  Qiang Jiang; Kai Li; Wen-Jing Lu; Shuang Li; Xin Chen; Xi-Juan Liu; Jie Yuan; Qiurong Ding; Feng Lan; Shi-Qing Cai
Journal:  Nat Commun       Date:  2018-09-26       Impact factor: 14.919

Review 4.  Ion Channels as Therapeutic Targets for Viral Infections: Further Discoveries and Future Perspectives.

Authors:  Frank W Charlton; Hayley M Pearson; Samantha Hover; Jon D Lippiat; Juan Fontana; John N Barr; Jamel Mankouri
Journal:  Viruses       Date:  2020-08-03       Impact factor: 5.048

5.  Design and Fabrication of the Vertical-Flow Bioreactor for Compaction Hepatocyte Culture in Drug Testing Application.

Authors:  Liang Zhu; Zhenfeng Wang; Huanming Xia; Hanry Yu
Journal:  Biosensors (Basel)       Date:  2021-05-19
  5 in total

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