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Automation of Predictor™ hERG Fluorescence Polarization Assay using Precision™ Automated Pipetting System for Serial Dilution of Small Molecule Drugs for IC50 Determinations下載
April 29, 2009
Authors: Kevin Lowitz, Bryan Marks, David Piper, Invitrogen; Wendy Goodrich, Peter Banks, Pete Brescia, Paul Held, Brad Larson, Gary Prescott, BioTek Instruments
The vast majority of drugs associated with acquired QT prolongation are known to interact with hERG. Due to the awareness of the potential danger of such QT drugs, the regulatory authorities issued recommendations for the establishment of cardiac safety testing during preclinical drug development. Traditionally, lead compounds in late stage preclinical studies were tested for hERG binding using electrophysiology. These are laborious methods, requiring significant skill in the end-user to perform a successful assay. Furthermore, many researchers wish to test lead compounds for safety earlier in the process of drug development. This requires a higher throughput type of assay. Here we describe methods for the automation of hERG screening using Invitrogen’s fluorescence polarization based Predictor™ assay using the Precision™ Automated Pipetting System for the serial dilution of known inhibitors of hERG to generate IC50 data. FP-based IC50 data will be compared to electrophysiology and radiometric data.