AN OVERVIEW ON HUMAN ETHER-A-GO-GO-RELATED GENE ASSAYAbstract
hERG (human ether-à-go-go-related gene) encodes a potassium ion channel which involved in ventricular repolarization at the end of a cardiac action potential. Mutations in hERG channel result in torsade’s de pointes. The cardiotoxicity is mainly due to the prolongation of the QT interval caused by the blockage of hERG. Indeed, many therapeutic drugs are withdrawn from the market as well as drug candidates may fail in the late phases of drug discovery because of cardiotoxicity. The ICH S7B and ICH E14 are the safety pharmacology guidelines recommended for evaluating new chemical entities. In the early phase of drug discovery, it is important to screen the compound for the activity on the hERG channels. Many hERG assays are available, including Fluorescent Membrane Potential Sensitive Dye Method, Radioactive Ligand Binding Method, Fluorescence Polarization Ligand Binding Method and Rubidium Flux method, Manual Patch-Clamp Method and automated Patch-Clamp Method, Langendorff’s perfused isolated heart method, Non-Invasive Telemetry, and Wireless Telemetry. This review is focused on hERG assay and provides additional information about the long QT syndrome and molecular structure of hERG.
Arulkumar Vishali * and Muthuswamy Umamaheswari
Department of Pharmacology, Sri Ramakrishna Institute of Paramedical Sciences Coimbatore, Tamil Nadu, India.
12 November 2021
12 January 2022
27 January 2022
01 August 2022