G Protein-coupled Receptor
G protein coupled receptors (GPCRs), also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), constitute a large protein family of receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. They are called transmembrane receptors because they pass through the cell membrane, and they are called seven-transmembrane receptors because they pass through the cell membrane seven times.
G protein-coupled receptors are found only in eukaryotes, including yeast, choanoflagellates, and animals. The ligands that bind and activate these receptors include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. G protein-coupled receptors are involved in many diseases, and are also the target of approximately 40% of all modern medicinal drugs. The 2012 Nobel prize in chemistry was awarded to Brian Kobilka and Robert Lefkowitz for their work that was "crucial for understanding how G-protein–coupled receptors function."
There are two principal signal transduction pathways involving the G protein-coupled receptors: the cAMP signal pathway and the phosphatidylinositol signal pathway. When a ligand binds to the GPCR it causes a conformational change in the GPCR, which allows it to act as a guanine nucleotide exchange factor (GEF). The GPCR can then activate an associated G-protein by exchanging its bound GDP for a GTP. The G-protein's α subunit, together with the bound GTP, can then dissociate from the β and γ subunits to further affect intracellular signaling proteins or target functional proteins directly depending on the α subunit type (Gαs, Gαi/o, Gαq/11, Gα12/13).
Read more about G Protein-coupled Receptor: Classification, Physiological Roles, Receptor Structure, Structure-function Relationships, Mechanism, GPCR Signaling, Details of CAMP and PIP2 Pathways, Receptor Regulation, Receptor Oligomerization, Origin and Diversification of The Superfamily, Dictyostelium Discoideum
Famous quotes containing the word receptor:
“The disinterest [of my two great-aunts] in anything that had to do with high society was such that their sense of hearing ... put to rest its receptor organs and allowed them to suffer the true beginnings of atrophy.”
—Marcel Proust (18711922)