Collation, assessment and analysis of literaturein vitrodata on hERG receptor blocking potency for subsequent modeling of drugs' cardiotoxic properties
10.1002/jat.1395
Crossref journal-article
Wiley
Journal of Applied Toxicology (311)
Abstract

AbstractThe assessment of the torsadogenic potency of a new chemical entity is a crucial issue during lead optimization and the drug development process. It is required by the regulatory agencies during the registration process. In recent years, there has been a considerable interest in developingin silicomodels, which allow prediction of drug–hERG channel interaction at the early stage of a drug development process. The main mechanism underlying an acquired QT syndrome and a potentially fatal arrhythmia called torsades de pointes is the inhibition of potassium channel encoded by hERG (the human ether‐a‐go‐go‐related gene). The concentration producing half‐maximal block of the hERG potassium current (IC50) is a surrogate marker for proarrhythmic properties of compounds and is considered a test for cardiac safety of drugs or drug candidates. The IC50values, obtained from data collected during electrophysiological studies, are highly dependent on experimental conditions (i.e. model, temperature, voltage protocol). For thein silicomodels' quality and performance, the data quality and consistency is a crucial issue. Therefore the main objective of our work was to collect and assess the hERG IC50data available in accessible scientific literature to provide a high‐quality data set for further studies. Copyright © 2008 John Wiley & Sons, Ltd.

Bibliography

Polak, S., Wiśniowska, B., & Brandys, J. (2008). Collation, assessment and analysis of literaturein vitrodata on hERG receptor blocking potency for subsequent modeling of drugs’ cardiotoxic properties. Journal of Applied Toxicology, 29(3), 183–206. Portico.

Authors 3
  1. Sebastian Polak (first)
  2. Barbara Wiśniowska (additional)
  3. Jerzy Brandys (additional)
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Dates
Type When
Created 16 years, 10 months ago (Nov. 5, 2008, 4:10 a.m.)
Deposited 7 months ago (Feb. 2, 2025, 9:10 a.m.)
Indexed 2 months, 3 weeks ago (June 9, 2025, 8:06 p.m.)
Issued 16 years, 10 months ago (Nov. 5, 2008)
Published 16 years, 10 months ago (Nov. 5, 2008)
Published Online 16 years, 10 months ago (Nov. 5, 2008)
Published Print 16 years, 5 months ago (April 1, 2009)
Funders 0

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@article{Polak_2008, title={Collation, assessment and analysis of literaturein vitrodata on hERG receptor blocking potency for subsequent modeling of drugs’ cardiotoxic properties}, volume={29}, ISSN={1099-1263}, url={http://dx.doi.org/10.1002/jat.1395}, DOI={10.1002/jat.1395}, number={3}, journal={Journal of Applied Toxicology}, publisher={Wiley}, author={Polak, Sebastian and Wiśniowska, Barbara and Brandys, Jerzy}, year={2008}, month=nov, pages={183–206} }