Literature DB >> 35294752

Cell-Based hERG Channel Inhibition Assay in High-Throughput Format.

Jinghua Zhao1, Menghang Xia2.   

Abstract

Human ether-a-go-go-related gene (hERG) channel plays an essential role in the repolarization of the cardiac action potential. Genetic mutations and some chemicals/drugs interfere with hERG channel activity, which may prolong the QT interval and potentially cause long QT syndrome. The FluxOR™ thallium flux assay performed in two cell lines, U2OS and HEK293, with stable hERG expression can be used to identify compounds that inhibit hERG channel activity. This chapter describes a cell-based hERG channel inhibition assay that has been optimized and performed in a 1536-well plate format. The homogeneous and robust assay can be used to identify compounds that inhibit hERG channel activity.
© 2022. This is a U.S. government work and not under copyright protection in the U.S.; foreign copyright protection may apply.

Entities:  

Keywords:  1536-well plate format; Astemizole; Human ether-a-go-go-related gene (hERG); Thallium flux assay; hERG channel inhibition

Mesh：

Substances：

Year:  2022        PMID： 35294752      PMCID： PMC9436417          DOI： 10.1007/978-1-0716-2213-1_3

Source DB:  PubMed          Journal:  Methods Mol Biol        ISSN： 1064-3745


  9 in total

Review 1.  The HERG K+ channel: progress in understanding the molecular basis of its unusual gating kinetics.

Authors:  Jamie I Vandenberg; Allan M Torres; Terence J Campbell; Philip W Kuchel
Journal:  Eur Biophys J       Date:  2003-09-10       Impact factor: 1.733

2.  Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels.

Authors:  Menghang Xia; Sampada A Shahane; Ruili Huang; Steven A Titus; Enoch Shum; Yong Zhao; Noel Southall; Wei Zheng; Kristine L Witt; Raymond R Tice; Christopher P Austin
Journal:  Toxicol Appl Pharmacol       Date:  2011-02-26       Impact factor: 4.219

Review 3.  Translational toxicology and rescue strategies of the hERG channel dysfunction: biochemical and molecular mechanistic aspects.

Authors:  Kai-ping Zhang; Bao-feng Yang; Bao-xin Li
Journal:  Acta Pharmacol Sin       Date:  2014-11-24       Impact factor: 6.150

4.  Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting.

Authors:  Xi-Ping Huang; Thomas Mangano; Sandy Hufeisen; Vincent Setola; Bryan L Roth
Journal:  Assay Drug Dev Technol       Date:  2010-12       Impact factor: 1.738

5.  A high-throughput HERG potassium channel function assay: an old assay with a new look.

Authors:  Charles S Cheng; Dawn Alderman; Jennifer Kwash; John Dessaint; Rita Patel; Mary Kay Lescoe; Michele Bennett Kinrade; Weifeng Yu
Journal:  Drug Dev Ind Pharm       Date:  2002       Impact factor: 3.225

Review 6.  I(Kr): the hERG channel.

Authors:  G N Tseng
Journal:  J Mol Cell Cardiol       Date:  2001-05       Impact factor: 5.000

7.  Molecular determinants of hERG channel block by terfenadine and cisapride.

Authors:  Kaichiro Kamiya; Ryoko Niwa; Mikio Morishima; Haruo Honjo; Michael C Sanguinetti
Journal:  J Pharmacol Sci       Date:  2008-11-06       Impact factor: 3.337

8.  Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels.

Authors:  Peter J S Chiu; Karen F Marcoe; Sidney E Bounds; Chun-Hsiung Lin; Jin-Jye Feng; Atsui Lin; Fong-Chi Cheng; William J Crumb; Richard Mitchell
Journal:  J Pharmacol Sci       Date:  2004-07       Impact factor: 3.337

9.  A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel.

Authors:  Steven A Titus; Daniel Beacham; Sampada A Shahane; Noel Southall; Menghang Xia; Ruili Huang; Elizabeth Hooten; Yong Zhao; Louie Shou; Christopher P Austin; Wei Zheng
Journal:  Anal Biochem       Date:  2009-07-05       Impact factor: 3.365
  9 in total

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