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Literature DB >> 18677468

High throughput functional screening of an ion channel library for drug safety and efficacy.

Abstract

Development of a large, representative library of ion channel-expressing cell lines is described. Validation on a full range of automated patch clamp and fluorescence illumination platforms is ongoing. Library "books" can be mixed and matched into channel panels according to tissue, therapeutic area and ion channel family. Unexpected results using a cardiac channel panel show that this panel may serve as a biomarker for cardiac risk assessment.

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Year: 2008 PMID： 18677468 DOI： 10.1007/s00249-008-0356-2

Source DB: PubMed Journal: Eur Biophys J ISSN： 0175-7571 Impact factor: 1.733

4 in total

1. Variability in the measurement of hERG potassium channel inhibition: effects of temperature and stimulus pattern.

Authors: Glenn E Kirsch; Elena S Trepakova; Jessica C Brimecombe; Serguei S Sidach; Hope D Erickson; Mary C Kochan; Lisa M Shyjka; Antonio E Lacerda; Arthur M Brown
Journal: J Pharmacol Toxicol Methods Date: 2004 Sep-Oct Impact factor: 1.950

2. HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine.

Authors: M Roy; R Dumaine; A M Brown
Journal: Circulation Date: 1996-08-15 Impact factor: 29.690

3. Alfuzosin delays cardiac repolarization by a novel mechanism.

Authors: Antonio E Lacerda; Yuri A Kuryshev; Yuan Chen; Muthukrishnan Renganathan; Heather Eng; Sanjay J Danthi; James W Kramer; Tianen Yang; Arthur M Brown
Journal: J Pharmacol Exp Ther Date: 2007-11-06 Impact factor: 4.030

4. Variability of the QTc interval: impact on defining drug effect and low-frequency cardiac event.

Authors: J Morganroth; A M Brown; S Critz; W J Crumb; D L Kunze; A E Lacerda; H Lopez
Journal: Am J Cardiol Date: 1993-08-26 Impact factor: 2.778

4 in total

1. Profiling diverse compounds by flux- and electrophysiology-based primary screens for inhibition of human Ether-à-go-go related gene potassium channels.

Authors: Beiyan Zou; Haibo Yu; Joseph J Babcock; Pritam Chanda; Joel S Bader; Owen B McManus; Min Li
Journal: Assay Drug Dev Technol Date: 2010-12 Impact factor: 1.738

High throughput functional screening of an ion channel library for drug safety and efficacy.

1. Variability in the measurement of hERG potassium channel inhibition: effects of temperature and stimulus pattern.

2. HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine.

3. Alfuzosin delays cardiac repolarization by a novel mechanism.

4. Variability of the QTc interval: impact on defining drug effect and low-frequency cardiac event.

1. Profiling diverse compounds by flux- and electrophysiology-based primary screens for inhibition of human Ether-à-go-go related gene potassium channels.

2. Can robots patch-clamp as well as humans? Characterization of a novel sodium channel mutation.

3. Automated electrophysiology makes the pace for cardiac ion channel safety screening.

4. Effects of proarrhythmic drugs on relaxation time and beating pattern in rat engineered heart tissue.