Biosensor and use thereof to identify therapeutic drug molecules and molecules binding orphan receptors

摘要

A G protein biosensor cell comprises G protein beta, gamma or both beta and gamma subunits tagged with a fluorescent protein(s) expressed in living intact functional cells. The subcellular location of the fluorescent protein tagged beta, gamma or both beta and gamma subunits is strongly responsive to the activation state of specific G protein coupled receptors in the biosensor cell. The biosensor cell responds reproducibly to agonist and antagonist drug molecules specific for G protein coupled receptors by demonstrating translocation of the fluorescent protein tagged beta, gamma or both beta and gamma subunits from one part of the cell to another. The biosensor cells have utility in identifying and classifying candidate therapeutic drugs as to their therapeutic value.