HTRF Resource Library

Use of the IP-one HTRF® assay for HTS and secondary screening of Gq and Gα16 coupled receptor targets

By: Rochdi Bouhelal

Novartis Institutes of Biomedical Research, Basel, Switzerland

Abstract:
The two main HTS  technologies to monitor G protein-coupled receptors (GPCR) in a cellular context rely on measurements of intracellular cAMP and calcium. Monitoring calcium mobilization has now been widely utilized in the Pharma industry and have proven to be useful in lead discovery. However calcium screens using the FLIPR technology have few issues associated with the read-out kinetic mode that might slow down the discovery process. With the advent of the IP-One HTRF^® technology, it is possible to quickly characterize hits in HTS and secondary screening set-ups. The presentation will summarize our first experience with the IP-One assay with Gq and Ga16 coupled receptors currently running in Novartis. Our preliminary data indicate that IP-One play and important role in HTS of GPCRs.