MCE special issue on signalling and regulation of GPCRs.

摘要

The G protein coupled receptors (GPCRs) form a large family of proteins that are all characterized by a 7-time transmembrane domain, looping in snake-like fashion through the plasma membrane, thus coining the alternative name 'serpentine receptors'. The family takes up a large chunk of the genome (nearly 1000 genes) and is involved in a wide variety of signalling: our senses taste, sight, smell, many important neuro-endocrine systems, ions and other transmission systems involving neurons. GPCRs are named after their coupling to the G proteins (Nobel Prize to Gillman and Rodbell in 1994), a versatile group of signalling proteins that relay the interaction of the ligand with the receptor to the intracellu-lar components involved in regulation of cell activities. The first GPCR genes were cloned in the 1980s while the crystal structure of the first GPCRs were revealed in the first years of this century. The GPCRs are important targets for drug development for the treatment of many diseases, and their function is therefore intensely studied in both academic and pharmaceutical institutes.