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NEW FLASH IMAGERS: facilitating higher throughput functional GPCR assays! Winter 2003

The recent availability of tailored automation solutions that combine liquid handling at the reading position with the latest innovations in low light imaging technology are providing screeners with new tools for the measurement of high throughput flash luminescence. These systems are proving particularly suited to the study of GPCR activation, using photoproteins such as aequorin as indicators of intracellular calcium.This article reviews the advantages of aequorin flash luminescence, compares the latest detection instrumentation, discusses the availability of new aequorin-based assay services and highlights the development of several new and improved photoproteins that have potential in the detection of calcium release triggered by several receptors.

Deja vu all over again: emerging concepts of G protein-coupled receptor (GPCR) function and drug discovery; Winter 06

G protein-coupled cell surface receptors (GPCRs) have served a fundamental role in modern pharmacology, due to their central importance in cell communication, and have been the target for the discovery of a large number of drugs. By one estimate, more than 40% of marketed drugs target GPCRs.