Secretin Receptor Family
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Secretin Receptor Family
Secretin family receptor proteins, also known as Family B or family 2 of G-protein coupled receptors are 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 7 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. Data minin ...
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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 protein family, evolutionarily-related proteins that are cell surface receptors that detect molecules outside the cell (biology), cell and activate cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) license. Ligands can bind either to extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices (Rhodopsin-like family). They are all activated by agonists although a spontaneous auto-activation of an empty receptor can also be observed. G protein-coupled receptors are found only in eukaryotes, including y ...
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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 ...
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Secretin Receptor
Human secretin receptor (gene name SCTR) is a G protein-coupled receptor which binds secretin and is the leading member (''i.e.'', first cloned) of the class B GPCR subfamily. Interactions Secretin receptor has been shown to interact with pituitary adenylate cyclase activating peptide Pituitary adenylate cyclase-activating polypeptide also known as PACAP is a protein that in humans is encoded by the ''ADCYAP1'' gene. pituitary adenylate cyclase-activating polypeptide is similar to vasoactive intestinal peptide. One of its effect .... References Further reading * * * * * * * * * * * * * * * * * External links IUPHAR GPCR Database - Secretin receptor* G protein-coupled receptors {{transmembranereceptor-stub ...
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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 (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. See also * Parathyroid hormone receptor References Further reading * * * * * * * * * * * External links

* * G protein-coupled receptors {{transmembranereceptor-stub ...
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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 ...
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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. 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 * Sermorelin Sermorelin acetate (; brand names Geref, Gerel), also known as GHRH (1-29), is a peptide analogue of growth hormone-releasing hormone (GHRH) which is used as a diagnos ...
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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 Glucago ...
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GLP1R
The glucagon-like peptide-1 receptor (GLP1R) is a receptor protein 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 G protein-coupled receptors. GLP1R is composed of two domains, one extracellular (ECD) that binds the C-terminal helix of GLP-1, and one transmembrane (TMD) domain that binds the N-terminal region of GLP-1. In the TMD domain there is a fulcrum of polar residues that regulates the biased signaling of the receptor while the transmembrane helical boundaries and extracellular surface are a trigger for biased agonism. Human receptor ligands GLP1R binds glucagon-like peptide-1 (GLP1) and glucagon as its natural endogenous agonists. Receptor agonists: *GLP-1 – endogenous in humans *glucagon – endogenous in humans *Oxyntomodulin * exendin- ...
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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, 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 responsible for the ensuing c ...
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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 Glucose-dependent insulinotropic polypeptide (GIP), also known as Gastric inhibitory polypeptide or gastric inhibitory peptide (also abbreviated as GIP), is an inhibiting hormone of the secretin family of hormones. While it is a weak inhibitor .... References External links * {{G protein-coupled receptors G protein-coupled receptors ...
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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 7-transmembrane protein family, a class of 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 Glucose-dependent insulinotropic polypeptide (GIP), also known as Gastric inhibitory polypeptide or gastric inhibitory peptide (also abbreviated as GIP), is an inhibiting hormone of the secretin family of hormones. While it is a weak inhibitor ... (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 subsequ ...
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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 aci ...
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