page_title: G protein-coupled receptor
hierarchical_section_title: G protein-coupled receptor
caption_attribution_description: English: The 7TM helixes of bovine rhodopsin. Based on PDB 1hzx and the Heller/Schaefer/Schulten lipid bilayer coordinates.
context_page_description: G protein-coupled receptors, also known as seven--transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors, is a large group of evolutionary related proteins that are cell surface receptor that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, 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.
  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.
context_section_description: G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), is a large group of evolutionary related proteins that are cell surface receptor that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, 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.
  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 the GDP bound to the G protein 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).
  GPCRs are an important drug target and approximately 34% of all Food and Drug Administration (FDA) approved drugs target 108 members of this family.  The global sales volume for these drugs is estimated to be 180 billion US dollars as of 2018.
caption: The seven-transmembrane α-helix structure of bovine rhodopsin
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