with its agonist
G protein-coupled receptors (
GPCRs), also known as
seven-transmembrane domain receptors,
7TM receptors,
heptahelical receptors,
serpentine receptor, and
G protein-linked receptors (
GPLR), comprise a large
protein family of
transmembrane receptors that sense
molecules outside the
cell and activate inside
signal transduction pathways and, ultimately, cellular responses. 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 30% of all modern medicinal drugs. 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). ==Desensitization and neurotransmitter concentration==