Vasoactive intestinal peptide receptor

Last updated
vasoactive intestinal peptide receptor 1
Identifiers
SymbolVIPR1
Alt. symbolsRDC1, HVR1, VAPC1
NCBI gene 7433
HGNC 12694
OMIM 192321
RefSeq NM_004624
UniProt P32241
Other data
Locus Chr. 3 p22
vasoactive intestinal peptide receptor 2
Identifiers
SymbolVIPR2
Alt. symbolsVPAC2
NCBI gene 7434
HGNC 12695
OMIM 601970
RefSeq NM_003382
UniProt P41587
Other data
Locus Chr. 7 q36.3
adenylate cyclase activating polypeptide 1 (pituitary) receptor type I
Identifiers
SymbolADCYAP1R1
Alt. symbolsPACAPR
NCBI gene 117
HGNC 242
OMIM 102981
RefSeq NM_001118
UniProt P41586
Other data
Locus Chr. 7 p14

There are two known receptors for the vasoactive intestinal peptide (VIP) termed VPAC1 and VPAC2. [1] [2] These receptors bind both VIP and pituitary adenylate cyclase-activating polypeptide (PACAP) to some degree. Both receptors are members of the 7 transmembrane G protein-coupled receptor family.

VPAC1 is distributed widely in the CNS, liver, lung, intestine and T-lymphocytes.

VPAC2 is found in the CNS, pancreas, skeletal muscle, heart, kidney, adipose tissue, testis, and stomach.

Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) receptors are activated by the endogenous peptides VIP, PACAP-38, PACAP-27, peptide histidine isoleucineamide (PHI), peptide histidine methionineamide (PHM) and peptide histidine valine (PHV). “PACAP type II receptors” (VPAC1 and VPAC2 receptors) display comparable affinity for PACAP and VIP, whereas PACAP-27 and PACAP-38 are >100 fold more potent than VIP as agonists of most isoforms of the PAC1 receptor. [3]

Related Research Articles

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Corticotropes are basophilic cells in the anterior pituitary that produce pro-opiomelanocortin (POMC) which undergoes cleavage to adrenocorticotropin (ACTH), β-lipotropin (β-LPH), and melanocyte-stimulating hormone (MSH). These cells are stimulated by corticotropin releasing hormone (CRH) and make up 15–20% of the cells in the anterior pituitary. The release of ACTH from the corticotropic cells is controlled by CRH, which is formed in the cell bodies of parvocellular neurosecretory cells within the paraventricular nucleus of the hypothalamus and passes to the corticotropes in the anterior pituitary via the hypophyseal portal system. Adrenocorticotropin hormone stimulates the adrenal cortex to release glucocorticoids and plays an important role in the stress response.

Vasoactive intestinal peptide Hormone that affects blood pressure / heart rate

Vasoactive intestinal peptide, also known as vasoactive intestinal polypeptide or VIP, is a peptide hormone that is vasoactive in the intestine. VIP is a peptide of 28 amino acid residues that belongs to a glucagon/secretin superfamily, the ligand of class II G protein–coupled receptors. VIP is produced in many tissues of vertebrates including the gut, pancreas, and suprachiasmatic nuclei of the hypothalamus in the brain. VIP stimulates contractility in the heart, causes vasodilation, increases glycogenolysis, lowers arterial blood pressure and relaxes the smooth muscle of trachea, stomach and gallbladder. In humans, the vasoactive intestinal peptide is encoded by the VIP gene.

Histamine H<sub>2</sub> receptor

H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A. PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist.

The bradykinin receptor family is a group of G-protein coupled receptors whose principal ligand is the protein bradykinin.

There are two known parathyroid hormone receptors in mammals termed PTH1R and PTH2R. These receptors bind parathyroid hormone and are members of the GPCR family of transmembrane proteins.

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. PACAP is similar to vasoactive intestinal peptide. One of its effects is to stimulate enterochromaffin-like cells. It binds to vasoactive intestinal peptide receptor and to the PACAP receptor.

Secretin receptor

Human secretin receptor is a G protein-coupled receptor which binds secretin and is the leading member of the class B GPCR subfamily.

Peptide PHI

Peptide PHI, also known as peptide histidine isoleucine, is a peptide which functions as a hormone. This peptide contains a composition of 27 amino acids with histidine on the N-terminus and isoleucine on the C-terminus. It was originally isolated from mammalian small intestine amongst mammalian neurons called intramural neurons which function in motor activity of the intestinal walls. An example of this was revealed in a study that demonstrated that this peptide regulates water and electrolyte transportation in the human jejunum; similar to its inhibitory effects on fluid absorption in the small intestine of pigs and rats.

Receptor activity-modifying proteins (RAMPs) are a class of protein that interact with and modulate the activities of several Class B G protein-coupled receptors including the receptors for secretin, calcitonin (CT), glucagon, and vasoactive intestinal peptide (VIP). There are three distinct types of RAMPs in mammals, designated RAMP1, RAMP2, and RAMP3, each encoded by a separate gene.

Glucagon-like peptide-2 receptor

Glucagon-like peptide-2 receptor (GLP-2R) is a protein that in human is encoded by the GLP2R gene located on chromosome 17.

The relaxin receptors are a subclass of four closely related G protein-coupled receptors that bind relaxin peptide hormones.

The neuropeptide B/W receptors are members of the G-protein coupled receptor superfamily of integral membrane proteins which bind the neuropeptides B and W. These receptors are predominantly expressed in the CNS and have a number of functions including regulation of the secretion of cortisol.

Parathyroid hormone 1 receptor

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).

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.

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.

Galanin receptor 1

Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.

VIPR2

Vasoactive intestinal peptide receptor 2 also known as VPAC2, is a G-protein coupled receptor that in humans is encoded by the VIPR2 gene.

VIPR1 Protein-coding gene in humans

Vasoactive intestinal polypeptide receptor 1 also known as VPAC1, is a protein, that in humans is encoded by the VIPR1 gene. VPAC1 is expressed in the brain (cerebral cortex, hippocampus, amygdala), lung, prostate, peripheral blood leukocytes, liver, small intestine, heart, spleen, placenta, kidney, thymus and testis.

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.

References

  1. Laburthe M, Couvineau A, Marie JC (2002). "VPAC receptors for VIP and PACAP". Recept. Channels. 8 (3–4): 137–53. doi:10.1080/10606820213680. PMID   12529932.
  2. Laburthe M, Couvineau A (2002). "Molecular pharmacology and structure of VPAC Receptors for VIP and PACAP". Regul. Pept. 108 (2–3): 165–73. doi:10.1016/S0167-0115(02)00099-X. PMID   12220741. S2CID   21588275.
  3. "VIP and PACAP receptors". IUPHAR Guide to Pharmacology. The British Pharmacological Society (BPS) and the International Union of Basic and Clinical Pharmacology (IUPHAR).