AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesInformation Science
SecretinReceptors, Gastrointestinal HormoneReceptors, G-Protein-CoupledPhotoaffinity LabelsReceptors, Vasoactive Intestinal PeptideVasoactive Intestinal PeptideCystadenocarcinoma, MucinousCHO CellsPancreasCystadenoma, SerousPancreatic JuiceCricetinaeFluorescence Resonance Energy TransferReceptors, CalcitoninCOS CellsCyclic AMPAdenocarcinoma, PapillaryCholecystokininCercopithecus aethiopsCricetulusAmino Acid SequenceMolecular Sequence DataAutoradiographyRadioligand AssayCarcinoma, Pancreatic DuctalCarcinoid TumorSecretory RateGastrointestinal HormonesProtein MultimerizationHydrochloric AcidSecond Messenger SystemsDuodenumLigandsBicarbonatesGTP-Binding ProteinsPeptidesGastrinsIodine RadioisotopesProtein Structure, SecondarySequence Homology, Amino AcidDimerizationAmylasesProtein BindingZollinger-Ellison Syndrome
GPCRProteinPeptideCalcitoninVasoactive intestinal polypeptidSeven transmembraneHuman secretin receptorGPCRsAgonist binding and acSecretionLigandSuperfamilyHigh affinityGeneFamilyLigandsProteinsAdenylate cyclaseIntracellularPancreatic vascularEncodesPancreasMolecularGenesDistinctInhibitionNeuropeptideBindVPAC2ExtracellularGastricPAC1RegulateScintigraphyEnergy expenditureSignalingPeroxisomeActivationHomoChannelsFunctionalActivates
GPCR9
  • This protein is a G protein-coupled receptor which binds secretin and is the leading member (i.e., first cloned) of the secretin receptor family, also called class B GPCR subfamily. (wikipedia.org)
  • While most membranous and disease related proteins are regulated by miRNAs, the G-protein coupled receptor (GPCR) family is an exception, being mostly unregulated by miRNAs. (frontiersin.org)
  • The Secretin family is a small family of 15 GPCRs (GPCR-B1) that all have an extracellular hormone-binding domain and bind peptide hormones . (axonmedchem.com)
  • The valuable source of large-scale genomic information initiated attempts to identify the origin(s) of G protein-coupled receptors (GPCR), count and categorize those genes, and follow their evolutionary history. (springer.com)
  • The chapter summarizes evolutionary processes working on GPCR genes and sheds light on their consequences at the levels of receptor structure and function. (springer.com)
  • Approximately half of the members of the human GPCR superfamily are chemosensory receptors, including odorant receptors (ORs), trace amine-associated receptors (TAARs), bitter taste receptors (TAS2Rs), sweet and umami taste receptors (TAS1Rs). (mdpi.com)
  • One mechanism is the binding of an extracellular ligand to a transmembrane G-protein-coupled receptor (GPCR). (pancreapedia.org)
  • GPCR family 3 receptors (also known as family C) are structurally similar to other GPCRs, but do not show any significant sequence similarity and thus represent a distinct group. (embl.de)
  • This entry represents the C-terminal region of family 3 GPCR receptor proteins, which contains the seven transmembrane region. (embl.de)
Protein31
  • The secretin receptor is a protein that in humans is encoded by the SCTR gene. (wikipedia.org)
  • A role for receptor kinases in the regulation of class II G protein-coupled receptors. (wikipedia.org)
  • Formation of oligomeric complexes of family A G protein-coupled receptors has been shown to influence their function and regulation. (aspetjournals.org)
  • We prepared tagged constructs expressing Renilla reniformis luciferase, yellow fluorescent protein, or cyan fluorescent protein at the carboxyl terminus of VPAC1, VPAC2, and secretin receptors, and performed BRET and morphologic fluorescence resonance energy transfer (FRET) studies with all combinations. (aspetjournals.org)
  • These studies provide new insight into the ability of family B G protein-coupled receptors to associate with each other in cells. (aspetjournals.org)
  • The secretin receptor is a prototypic class B G protein-coupled receptor that is activated by binding of its natural peptide ligand. (elsevierpure.com)
  • Insulation of a G protein-coupled receptor on the plasmalemmal surface of the pancreatic acinar cell. (nih.gov)
  • Derived from larger precursor proteins, most neuropeptides bind to G-protein coupled receptors (GPCRs) belonging to rhodopsin-β, rhodopsin-γ and secretin-type receptor families. (qmul.ac.uk)
  • these receptors comprise a distinct family of G protein-coupled seven transmembrane domain receptors. (jci.org)
  • Interestingly, the hCTR sequence is remotely related to the cAMP receptor of Dictyostelium discoideum (21% identical), but is not significantly related to other G protein-coupled receptor sequences now in the data bases. (jci.org)
  • Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino acid incretin hormone that binds to a seven-transmembrane G-protein-coupled receptor (GIP-R) that is expressed in numerous tissues including islet β-cells and α-cells ( 1 , 2 ). (diabetesjournals.org)
  • Schioth HB, Fredriksson R (2005) The GRAFS classification system of G-protein coupled receptors in comparative perspective. (springer.com)
  • Sequence comparison does not support an evolutionary link between halobacterial retinal proteins including bacteriorhodopsin and eukaryotic G-protein-coupled receptors. (springer.com)
  • Kim JY, Haastert PV, Devreotes PN (1996) Social senses: G-protein-coupled receptor signaling pathways in Dictyostelium discoideum . (springer.com)
  • Nordstrom KJ, Sallman Almen M, Edstam M et al (2011) Independent HHsearch, Needleman-Wunsch-based, and motif analyses reveal the overall hierarchy for most of the G protein-coupled receptor families. (springer.com)
  • Methuselah-like (Mth-l) proteins are G- protein coupled receptors of the Secretin-like receptor family. (wayne.edu)
  • Iguchi T, Sakata K, Yoshizaki K, Tago K, Mizuno N, Itoh H. Orphan G protein-coupled receptor GPR56 regulates neural progenitor cell migration via a G alpha 12/13 and Rho pathway. (medlineplus.gov)
  • Orphan G protein-coupled receptor GPR56 plays a role in cell transformation and tumorigenesis involving the cell adhesion pathway. (medlineplus.gov)
  • Melanocortin receptor 3 is a protein that in humans is encoded by the MC3R gene . (wikidoc.org)
  • This gene encodes MC 3 , a G-protein coupled receptor for melanocyte-stimulating hormone and adrenocorticotropic hormone that is expressed in tissues other than the adrenal cortex and melanocytes. (wikidoc.org)
  • G protein-coupled receptors (GPCRs) belong to the largest class of drug targets. (mdpi.com)
  • Vasoactive intestinal peptide (VIP) is a 28-amino acid neuropeptide which belongs to a glucagon/secretin superfamily, the ligand of class II G protein-coupled receptors. (rcsb.org)
  • Here, we present multiple lines of evidence to support the hypothesis that the orphan CG8422 G-protein-coupled receptor is a functional DH-R. When expressed in mammalian cells, CG8422 conferred selective sensitivity to DH, as indicated by translocation of aβ-arrestin-2-GFP reporter from the cytoplasm to the cell membrane. (silverchair.com)
  • is for the 7-transmembrane receptor protein in the secretin family. (mathworks.cn)
  • The receptor protein has seven transmembrane α-helices connected by alternating cytosolic and extracellular loops. (pancreapedia.org)
  • The protein is a seven-span transmembrane protein and a member of the secretin receptor family. (utsouthwestern.edu)
  • PACAP actions on cells can be mediated through G-protein-coupled receptors (GPCRs) from group II from the secretin receptor family members. (iwap2018.com)
  • G protein-coupled receptors (GPCRs) constitute a vast protein family that encompasses a wide range of functions, including various autocrine, paracrine and endocrine processes. (embl.de)
  • Receptor activity-modifying proteins (RAMPs) are a class of proteins that interact with and modulate the activities of several Class B G Protein-Coupled Receptors including the receptors for secretin, calcitonin (CT) and glucagon, RAMPs complex with Sumatriptan molecule [5]. (lupinepublishers.com)
  • The molecular docking study was carried out to explore the binding mode of serotonin derivatives (Table 2) within the binding energy of peroxisome proliferator-activated receptor gamma 3ADX and Receptor activity-modifying protein 1 2YX8. (lupinepublishers.com)
  • The proteins (Peroxisome proliferator-activated receptor gamma left, Receptor activity-modifying protein 1 right) (RCSB PDB CODE: 3ADX, 2YX8). (lupinepublishers.com)
Peptide4
  • The secretin receptor has been shown to interact with pituitary adenylate cyclase activating peptide. (wikipedia.org)
  • and the vasoactive intestinal peptide receptors (VIPR1, VIPR2). (axonmedchem.com)
  • A cyclic peptide (RO 25-1553) and a secretion analogue ([R16]chicken secretin) were identified as selective agonist peptides for the VIP2- and VIP1 receptors, respectively. (nih.gov)
  • In micelle-bound PACAP-38 (one of the glucagon/secretin superfamily peptide) structure, the identical hydrophobic residues form the micelle-binding interface. (rcsb.org)
Calcitonin3
  • Cloning, characterization, and expression of a human calcitonin receptor from an ovarian carcinoma cell line. (jci.org)
  • A human ovarian small cell carcinoma line (BIN-67) expresses abundant calcitonin (CT) receptors (CTR) (143,000 per cell) that are coupled, to adenylate cyclase. (jci.org)
  • We have cloned and sequenced a cDNA (RPR4) encoding a new member of the secretin/calcitonin/parathyroid hormone (PTH) receptor family. (wiley.com)
Vasoactive intestinal polypeptid2
  • Critical contributions of amino-terminal extracellular domains in agonist binding and activation of secretin and vasoactive intestinal polypeptide receptors. (wikipedia.org)
  • Here, we show that subtypes of human vasoactive intestinal polypeptide receptors (VPAC1 and VPAC2) that represent the closest structurally related receptors to the secretin receptor also form constitutive oligomers with themselves and with the secretin receptor. (aspetjournals.org)
Seven transmembrane1
  • Violin JD, Lefkowitz RJ (2007) Beta-arrestin-biased ligands at seven-transmembrane receptors. (springer.com)
Human secretin receptor1
GPCRs2
  • Examples of neuropeptides that act via secretin-type GPCRs are parathyroid hormone (PTH), a key regulator of calcium metabolism in vertebrates, and pigment dispersing factor (PDF), a key component of the insect circadian pacemaker. (qmul.ac.uk)
  • The aim of this project is to identify computationally and experimentally the neuropeptides that act as ligands for secretin-type GPCRs in an echinoderm, the starfish Asterias rubens. (qmul.ac.uk)
Agonist binding and ac1
  • Multiple extracellular loop domains contribute critical determinants for agonist binding and activation of the secretin receptor. (nih.gov)
Secretion4
  • High-resolution 3D structures of type 2 secretion system (T2SS) secretins revealed bimodular channels with a C-module, holding a conserved central gate and an optional top gate, followed by an N-module for which multiple structural organizations have been proposed. (bvsalud.org)
  • Our data illustrate how the gating properties of T2SS secretins allow these large channels to overcome the duality between the necessity of preserving the OM impermeability while simultaneously promoting the secretion of large, folded effectors. (bvsalud.org)
  • VIP resembles secretin, which stimulates the secretion of alkaline pancreatic juices. (medscape.com)
  • secretion (including his secretin). (who.int)
Ligand4
  • We previously used bioluminescence resonance energy transfer (BRET) to demonstrate that the prototypic family B secretin receptor forms ligand-independent oligomeric complexes. (aspetjournals.org)
  • Unlike secretin receptor oligomers that were unaffected by ligand binding, the VPAC receptor homo-oligomers were modulated by vasoactive intestinal polypeptide. (aspetjournals.org)
  • The VPAC1-VPAC2 hetero-oligomers were modulated by vasoactive intestinal polypeptide binding, whereas the secretin-VPAC1 and secretin-VPAC2 receptor hetero-oligomers were unaffected by ligand treatment. (aspetjournals.org)
  • We have explored the molecular basis for the coupling of each of these G proteins to this receptor using systematic sitedirected mutagenesis of key residues within each of the intracellular loop regions, and studying ligand binding and secretin-stimulated cAMP and calcium responses. (elsevierpure.com)
Superfamily2
  • However, little is known about the existence of such complexes for family B receptors in this superfamily. (aspetjournals.org)
  • PACAP can be a well-conserved person in the vasoactive intestinal polypeptide (VIP)-glucagon-secretin superfamily. (iwap2018.com)
High affinity5
  • We have, therefore, used in situ autoradiography, photoaffinity labeling, and RNase protection assays with healthy rat pancreas, dispersed acinar cells, and pancreas depleted of acinar cells to explore the cellular distribution and molecular identity of high-affinity secretin receptors in this complex organ. (elsevierpure.com)
  • The autoradiographic examination of 125 I-labeled [Tyr 10 ]rat secretin-27 binding to normal pancreas demonstrated saturable and specific high-affinity binding sites on both acinar and duct cells, with a uniform lobular distribution, but with no binding above background over islets or vascular structures. (elsevierpure.com)
  • Transfection of this cDNA into COS cells resulted in expression of receptors with high affinity for salmon CT (Kd = approximately 0.44 nM) and for human CT (Kd = approximately 5.4 nM). (jci.org)
  • Vasoactive Intestinal Polypeptide (VIP) exerts its biological effects through interaction with two high affinity receptors named the VIP1- and the VIP2 receptors. (nih.gov)
  • The iodinated peptides retained the high affinity and selectivity of the unlabelled peptides and were used for the mapping of each receptor subclass in rat brain. (nih.gov)
Gene4
  • Small Indels in the Androgen Receptor Gene: Phenotype Implications and Mechanisms of Mutagenesis. (medscape.com)
  • Animal steroid hormones initiate signaling by passive diffusion into cells and binding to their nuclear receptors to regulate gene expression. (biologists.com)
  • Gene Bank blast for a homologous nucleotide sequence revealed the same PPRE within the rat glucose-dependent insulinotropic polypeptide receptor (GIP-R) promoter sequence. (diabetesjournals.org)
  • Genetic drift and selective forces have shaped the individual structure of a given receptor gene but also of the species-specific receptor repertoire - a process that is still ongoing. (springer.com)
Family4
  • The apparent absence or extreme low density of similar secretin receptors on islets and pancreatic vascular structures suggests that the pharmacological effects of secretin on those cells may either be indirect or mediated by another secretin family receptor that recognizes this hormone with lower affinity. (elsevierpure.com)
  • Load the HMM profile structure of the 7 transmembrane receptor (Secretin family). (mathworks.com)
  • Rabbit polyclonal to SYK.Syk is a cytoplasmic tyrosine kinase of the SYK family containing two SH2 domains.Plays a central role in the B cell receptor (BCR) response. (bioskinrevive.com)
  • VIP has a molecular weight of 3381, consists of 28 amino acids, and belongs to the secretin-glucagon family. (medscape.com)
Ligands4
  • Functional characterisation of neuropeptides that act as ligands for secretin-type receptors in an echinoderm. (qmul.ac.uk)
  • Therefore, characterisation of neuropeptides that act as ligands for secretin-type receptors in A. rubens could provide new insights into the evolution and comparative physiology of this type of neuropeptide signalling. (qmul.ac.uk)
  • the predicted activity was LD 50 and prediction was done on similarity clusters with the leaders chosen as the best docked ligands on the Peroxisome proliferatoractivated receptor gamma. (lupinepublishers.com)
  • In this paper, a docking study, performed to identify the geometric description of the pharmacophore in the interaction of this class of ligands with the peroxisome proliferatoractivated receptor gamma, is reported. (lupinepublishers.com)
Proteins2
  • These data suggest that, while some receptor determinants are clearly shared, there are also distinct determinants for coupling with each of these G proteins. (elsevierpure.com)
  • Garcia, GL, Dong, M & Miller, LJ 2012, ' Differential determinants for coupling of distinct G proteins with the class B secretin receptor ', American Journal of Physiology - Cell Physiology , vol. 302, no. 8, pp. (elsevierpure.com)
Adenylate cyclase1
  • PAC1 not merely activates an average group II receptor sign cascade through adenylate cyclase (AC) [7] but can be coupled towards the phospholipase C (PLC) pathway [8]. (iwap2018.com)
Intracellular2
  • However, coexpression of secretin receptors with either type of VPAC receptor resulted in intracellular trapping of the hetero-oligomeric complexes within the biosynthetic pathway. (aspetjournals.org)
  • The signaling effects of this receptor are mediated by coupling with Gs, which activates cAMP production, and Gq, which activates intracellular calcium mobilization. (elsevierpure.com)
Pancreatic vascular1
  • Intra-arteniai infusion of secretin [1] and CCK vasodilates the pancreatic vascular bed. (erowid.org)
Encodes2
  • one encodes the PACAP-preferring Coptisine chloride receptor PAC1, whereas the additional two encode receptors that react to PACAP and VIP similarly, VPAC2 and VPAC1. (iwap2018.com)
  • This suggests that RPR4 encodes a novel VIP receptor which we have designated the VIP 2 receptor. (wiley.com)
Pancreas3
  • Conversely, even prolonged intra-arterial infusion of secretin does not release pancreatic stores of histamine: In fact, endogenous synthesis and release of histamine seem to play no role in the regulation of functional vasodilation in the pancreas. (erowid.org)
  • Atropine (250-550 mcg) inhibits vasodilation and decreases the secretory response of the pancreas to secreting Previous intra-arterial injection of bradykinin restores the secretory response of the pancreas, thus showing that inhibitory effect of, of the atropine on the secretory response of the pancreas to secretin is partly mediated by inhibition of secretin-induced vasodilation. (erowid.org)
  • Acetazolamide zones (50 mg) inhibits both the secretory and the vascular responses of the pancreas to an infusion of secretin. (erowid.org)
Molecular4
  • Secretin is an important regulator of pancreatic function, but the molecular basis of its actions is not well understood. (elsevierpure.com)
  • RNase protection assays confirmed the molecular identity of the secretin receptors expressed on these distinct cells. (elsevierpure.com)
  • Applying molecular biology techniques (transcriptome sequencing), the study found that the secretin receptor is also expressed in brown adipose tissue. (tum.de)
  • A method is described to dock a serotonin into a binding site in a peroxisome proliferator-activated receptor gamma on the basis of the complementarity of the inter-molecular atomic contacts. (lupinepublishers.com)
Genes1
  • Peroxisome proliferator-activated receptors are ligandactivated transcription factors that regulate genes important in cell differentiation and various metabolic processes, especially lipid and glucose homeostasis [4]. (lupinepublishers.com)
Distinct2
  • Direct identification of a second distinct site of contact between cholecystokinin and its receptor. (nih.gov)
  • Similar to other T3SSs, however, the apparatus is anchored within the needle complex by a network of flexible linkers that either adjust conformation to connect to equivalent patches on the secretin oligomer or bind distinct surface patches at the same height of the export apparatus. (bvsalud.org)
Inhibition1
  • Inhibition of Secretin/Secretin Receptor Axis Ameliorates NAFLD Phenotypes. (proquest.com)
Neuropeptide1
  • The identification of a Drosophila receptor for the DH neuropeptide provides a basis for genetic analysis of this critical factor's roles in maintaining physiological homeostasis. (silverchair.com)
Bind1
  • Additive effects were elicited by combining the effective mutations, while combining all the effective mutations resulted in a construct that continued to bind secretin normally, but that elicited no significant cAMP or calcium responses. (elsevierpure.com)
VPAC21
  • Morphologic FRET studies demonstrated that each of the homo-oligomers and the VPAC1-VPAC2 receptor hetero-oligomers reached the cell surface, where receptor interactions were clear. (aspetjournals.org)
Extracellular1
  • Secretins are outer membrane (OM) channels found in various bacterial nanomachines that secrete or assemble large extracellular structures. (bvsalud.org)
Gastric1
  • Orthologous to human GIPR (gastric inhibitory polypeptide receptor). (nih.gov)
PAC11
  • TgN cells included neuronal Schwann and ganglion cells, as well as the PAC1 receptor was indicated in both cell types. (iwap2018.com)
Regulate1
  • As these receptors regulate many important physiological processes they are potentially promising targets for drug development. (embl.de)
Scintigraphy1
Energy expenditure1
  • GIP receptor deletion in mice confers resistance to high-fat diet-induced obesity via alterations in energy expenditure and adipose tissue lipid metabolism. (nih.gov)
Signaling1
  • Insulin signaling through the insulin receptor increases linear growth through effects on bone and the GH-IGF-1 axis. (medscape.com)
Peroxisome1
  • We previously showed that peroxisome proliferator-activated receptor (PPAR)-γ in β-cells regulates pdx-1 transcription through a functional PPAR response element (PPRE). (diabetesjournals.org)
Activation2
  • Stimulation of this receptor with secretin led to an immediate activation of non-shivering thermogenesis in brown adipocytes. (tum.de)
  • Knowledge for the conformation of VIP bound to membrane is important because the receptor activation is initiated by membrane binding of VIP. (rcsb.org)
Homo1
Channels1
Functional1
  • In the moth Manduca and the cricket Acheta ,functional studies have shown that its cognate receptor (DH-R) is related to the mammalian CRF receptor. (silverchair.com)
Activates2
  • The long known gut hormone secretin has a newly discovered, additional function: It activates thermogenesis in brown fat, which triggers saturation. (tum.de)
  • The intestinal hormone secretin has a newly discovered, additional function: it activates the energy-consuming brown fatty tissue - the intestine talks to the brain and reports that saturation has set in. (tum.de)