GPCRbaserte

GPCRbaserte describes approaches that rely on G protein-coupled receptor signaling. GPCRs are a large family of seven-transmembrane receptors activated by diverse ligands, including hormones, neurotransmitters, and photons. Activated GPCRs engage heterotrimeric G proteins (Gs, Gi/o, Gq/11, G12/13) and initiate second messenger pathways such as cAMP, Ca2+, and IP3/DAG, and can also signal via β-arrestin.

Because of their central role in physiology, GPCRs are major drug targets. GPCR-based strategies appear in drug discovery, functional assays, and diagnostic tools using readouts like cAMP, calcium, receptor internalization, or β-arrestin recruitment, measured with fluorescence, luminescence, BRET, or FRET.

GPCR-based tools include biosensors and engineered receptors that report on ligand activity or cellular state. Advances in optogenetics and chemogenetics use GPCR-derived actuators and reporters to control or monitor signaling in living cells and organisms.

Challenges include constitutive activity, signaling bias (functional selectivity), receptor desensitization, and context-dependent coupling in different cell types. Despite this, GPCR-based approaches continue to drive research and therapeutics, with many approved drugs targeting GPCRs and ongoing development of biased ligands and allosteric modulators.