Development and validation of BRET-based biosensors for drug candidate profiling
G protein coupled receptors (GCPRs) are proteins found at the surface of cells are responsible for activating numerous intracellular signaling pathways and thus are involved in regulating about every physiological response. Activation of GPCRs occurs by compounds as varied as photons, lipids, ions, small hormonal or neurotransmitter compounds or larger peptidic and protein molecules. As such, GPCRs are currently the target of up to 34% of marketed drugs. Although these drugs were believed to function as simple on/off switches able to activate or inhibit GPCR activity, recent findings have revealed that they produce parallel effects that may lead to undesirable responses. This new knowledge has opened up the possibility of developing unique molecules aimed at specifically blocking or activating the relevant therapeutic response while keeping unwanted deleterious effects at bay.