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Class B GPCR
Secretin receptor family (class B G-protein coupled receptors, GPCR subfamily) consists of secretin receptors regulated by peptide hormones from the glucagon hormone family. The family is different from adhesion G protein-coupled receptors. The secretin-receptor family of GPCRs include vasoactive intestinal peptide receptors and receptors for secretin receptor, secretin, calcitonin receptor, calcitonin and parathyroid hormone receptor, parathyroid hormone/parathyroid hormone-related peptides. These receptors activate adenylyl cyclase and the Phospholipase C#Effects, phosphatidyl-inositol-calcium pathway. The receptors in this family have seven Transmembrane domain, transmembrane Alpha helix, helices,; ; like rhodopsin-like GPCRs. However, there is no significant sequence identity between these two GPCR families and the secretin-receptor family has its own characteristic Seven transmembrane protein, 7TM signature. The secretin-receptor family GPCRs exist in many animal species. D ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
G-protein Coupled Receptors
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. They are coupled with G proteins. They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins, an N-terminal extracellular region and a C-terminal intracellular region) of amino acid residues, which is why they are sometimes referred to as seven-transmembrane receptors. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) licence/ref> Ligands can bind either to the extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ADCYAP1R1
Pituitary adenylate cyclase-activating polypeptide type I receptor also known as PAC1, is a protein that in humans is encoded by the ''ADCYAP1R1'' gene. This receptor binds pituitary adenylate cyclase activating peptide. Function PAC1 is a membrane-associated protein and shares significant homology with members of the G-protein coupled class B glucagon/ secretin receptor family. This receptor mediates diverse biological actions of adenylate cyclase activating polypeptide 1 and is positively coupled to adenylate cyclase. Alternative splicing of two exons of this gene generates four major splice variants, but their full-length nature has not been determined. PAC1 is expressed in the adrenal medulla, pancreatic acini, uterus, myenteric plexus and brain. It is also expressed in the trigeminal In neuroanatomy, the trigeminal nerve ( lit. ''triplet'' nerve), also known as the fifth cranial nerve, cranial nerve V, or simply CN V, is a cranial nerve responsible for sensatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PTHR2
Parathyroid hormone 2 receptor is a protein that in humans is encoded by the ''PTH2R'' gene. Function The protein encoded by this gene is a member of the G protein-coupled receptor family 2. This protein is a receptor for parathyroid hormone (PTH). This receptor is more selective in ligand recognition and has a more specific tissue distribution compared to parathyroid hormone 1 receptor ( PTH1R). It is activated by PTH but not by parathyroid hormone-like hormone (PTHLH) and is particularly abundant in the brain and pancreas. The molecular interaction of the PTH2 receptor with the peptide TIP39 has been characterized in full 3D molecular detail, identifying among other residues Tyr-318 in transmembrane helix 5 as a key residue for high affinity binding. Mechanism It is a member of the secretin family of G protein-coupled receptors. The activity of this receptor is mediated by Gs protein, which activates adenylyl cyclase Adenylate cyclase (EC 4.6.1.1, also commonly known a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PTHR1
Parathyroid hormone/parathyroid hormone-related peptide receptor, also known as parathyroid hormone 1 receptor (PTH1R), is a protein that in humans is encoded by the ''PTH1R'' gene. PTH1R functions as a receptor for parathyroid hormone ( PTH) and for parathyroid hormone-related protein (PTHrP), also called parathyroid hormone-like hormone (PTHLH). Function This "classical" PTH receptor is expressed in high levels in bone and kidney and regulates calcium ion homeostasis through activation of adenylate cyclase and phospholipase C. In bone, it is expressed on the surface of osteoblasts. When the receptor is activated through PTH binding, osteoblasts express RANKL (Receptor Activator of Nuclear Factor kB Ligand), which binds to RANK (Receptor Activator of Nuclear Factor kB) on osteoclasts. This turns on osteoclasts to ultimately increase the resorption rate. Mechanism It is a member of the secretin family of G protein-coupled receptors. The activity of this receptor is mediated by ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Growth Hormone Releasing Hormone Receptor
The growth-hormone-releasing hormone receptor (GHRHR) is a G-protein-coupled receptor that binds growth hormone-releasing hormone. The GHRHR activates a Gs protein that causes a cascade of cAMP via adenylate cyclase. GHRHR is distinct from the growth hormone secretagogue receptor (also known as the ghrelin receptor), where growth hormone releasing peptides act to release growth hormone. Function This gene, expressed in the pituitary, encodes a receptor for growth-hormone-releasing hormone. Binding of this hormone to the receptor leads to synthesis and release of growth hormone. Mutations in this gene have been associated with isolated growth-hormone deficiency (IGHD), also known as Dwarfism of Sindh, a disorder characterized by short stature. Many alternate transcriptional splice variants encoding different isoforms have been described, but only two have been characterized to date. Ligands Agonists * CJC-1295 * Dumorelin * GHRH (somatorelin) * Rismorelin * Sermoreli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GLP2R
Glucagon-like peptide-2 receptor (GLP-2R) is a protein that in human is encoded by the ''GLP2R'' gene located on chromosome 17. Function The GLP2 receptor (GLP2R) is a G protein-coupled receptor superfamily member closely related to the glucagon receptor ( GLP1 receptor). Glucagon-like peptide-2 (GLP2) is a 33-amino acid proglucagon-derived peptide produced by intestinal enteroendocrine cells. Like glucagon-like peptide-1 (GLP1) and glucagon itself, it is derived from the proglucagon peptide encoded by the GCG gene. GLP2 stimulates intestinal growth and upregulates villus height in the small intestine, concomitant with increased crypt cell proliferation and decreased enterocyte apoptosis. Moreover, GLP2 prevents intestinal hypoplasia resulting from total parenteral nutrition. GLP2R, a G protein-coupled receptor superfamily member is expressed in the gut and closely related to the glucagon receptor (GCGR) and the receptor for GLP1 (GLP1R). See also *Glucagon-like peptide-2 Gluca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GLP1R
The glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor (GPCR) found on beta cells of the pancreas and on neurons of the brain. It is involved in the control of blood sugar level by enhancing insulin secretion. In humans it is synthesised by the gene ''GLP1R'', which is present on chromosome 6. It is a member of the glucagon receptor family of GPCRs. GLP1R is composed of two domains, one extracellular (ECD) that binds the C-terminal helix of GLP-1, and one transmembrane domain (TMD) that binds the N-terminal region of GLP-1. In the TMD domain a fulcrum of polar residues regulates the biased signaling of the receptor while the transmembrane helical boundaries and extracellular surface are a trigger for biased agonism. Ligands GLP1R binds glucagon-like peptide-1 (GLP1) and glucagon as its natural endogenous agonists. Agonists: *GLP-1 – endogenous in humans *glucagon – endogenous in humans * oxyntomodulin * exendin-4, * exenatide * lixisenatide * albigl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GCGR
The glucagon receptor is a 62 kDa protein that is activated by glucagon and is a member of the class B G-protein coupled family of receptors (secretin receptor family), coupled to G alpha i, Gs and to a lesser extent G alpha q. Stimulation of the receptor results in the activation of adenylate cyclase and phospholipase C and in increased levels of the secondary messengers intracellular cAMP and calcium. In humans, the glucagon receptor is encoded by the gene. Glucagon receptors are mainly expressed in liver and in kidney with lesser amounts found in heart, adipose tissue, spleen, thymus, adrenal glands, pancreas, cerebral cortex, and gastrointestinal tract. Signal transduction pathway A glucagon receptor, upon binding with the signaling molecule glucagon, initiates a signal transduction pathway that begins with the activation of adenylate cyclase, which in turn produces cyclic AMP (cAMP). Protein kinase A, whose activation is dependent on the increased levels of cAMP, is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glucagon Receptor Family
The glucagon receptor family is a group of closely related G-protein coupled receptors which include: * Glucagon receptor * Glucagon-like peptide 1 receptor * Glucagon-like peptide 2 receptor * Gastric inhibitory polypeptide receptor The first three receptors bind closely related peptide hormones (glucagon, glucagon-like peptide-1, glucagon-like peptide-2) derived from the proglucagon polypeptide. The last receptor binds gastric inhibitory polypeptide Gastric inhibitory polypeptide (GIP), also known as glucose-dependent insulinotropic polypeptide, is an inhibiting hormone of the secretin family of hormones. While it is a weak inhibitor of gastric acid secretion, its main role, being an incr .... References External links * {{G protein-coupled receptors G protein-coupled receptors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GIPR
The gastric inhibitory polypeptide receptor (GIP-R), also known as the glucose-dependent insulinotropic polypeptide receptor, is a protein that in humans is encoded by the ''GIPR'' gene. GIP-R is a member of the class B family of G protein–coupled receptor, G protein coupled receptors. GIP-R is found on beta-cells in the pancreas where it serves as the receptor for the hormone Gastric inhibitory polypeptide (GIP). Function Gastric inhibitory polypeptide, also called glucose-dependent insulinotropic polypeptide, is a 42-amino acid polypeptide synthesized by K cells of the duodenum and small intestine. It was originally identified as an activity in gut extracts that inhibited gastric acid secretion and gastrin release, but subsequently was demonstrated to stimulate insulin release potently in the presence of elevated glucose. The insulinotropic effect on pancreatic islet beta-cells was then recognized to be the principal physiologic action of GIP. Together with glucagon-li ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Corticotropin Releasing Hormone Receptor 2
Corticotropin-releasing hormone receptor 2 (CRHR2) is a protein, also known by the IUPHAR-recommended name CRF2, that is encoded by the CRHR2 gene and occurs on the surfaces of some mammalian cells. CRF2 receptors are type 2 G protein-coupled receptors for corticotropin-releasing hormone (CRH) that are resident in the plasma membranes of hormone-sensitive cells. CRH, a peptide of 41 amino acids synthesized in the hypothalamus, is the principal neuroregulator of the hypothalamic-pituitary-adrenal axis, signaling via guanine nucleotide-binding proteins (G proteins) and downstream effectors such as adenylate cyclase. The CRF2 receptor is a multi-pass membrane protein with a transmembrane domain composed of seven helices arranged in a V-shape. CRF2 receptors are activated by two structurally similar peptides, urocortin II, and urocortin III, as well as CRH. Properties The human CRHR2 gene contains 12 exons. Three major functional isoforms, alpha (411 amino acids), beta (438 amino a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Corticotropin Releasing Hormone Receptor 1
Corticotropin-releasing hormone receptor 1 (CRHR1) is a protein, also known as CRF1, with the latter (CRF1) now being the IUPHAR-recommended name. In humans, CRF1 is encoded by the ''CRHR1'' gene at region 17q21.31, beside micrototubule-associated protein tau MAPT. Structure The human CRHR1 gene contains 14 exons over 20 kb of DNA, and its full gene product is a peptide composed of 444 amino acids. Excision of exon 6 yields in the Messenger RNA, mRNA for the primary functional CRF1, which is a peptide composed of 415 amino acids, arranged in seven Hydrophobe, hydrophobic Alpha helix, alpha-helices. The CRHR1 gene is alternatively Alternative splicing, spliced into a series of variants. These variants are generated through deletion of one of the 14 exons, which in some cases causes a Frameshift mutation, frame-shift in the open reading frame, and encode corresponding Protein isoform, isoforms of CRF1. Though these Protein isoform, isoforms have not been identified in native tiss ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
