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Topic: G protein-coupled receptor


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In the News (Mon 14 Dec 09)

  
 G-protein-coupled receptor - Wikipedia, the free encyclopedia
It is known that the inactive G protein is bound to the receptor in its inactive state.
Once the ligand is recognized, the receptor shifts conformation and thus mechanically activates the G protein, which detaches from the receptor.
Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain coming from the G protein (that was activated by the receptor) via adenylate cyclase and cyclic AMP (cAMP).
en.wikipedia.org /wiki/G_protein_coupled_receptor   (1145 words)

  
 Cell Signaling
T cells use a transmembrane dimeric protein as a receptor for a particular combination of antigen fragment nestled in the cleft of a glycoprotein encoded by genes in the major histocompatibility complex.
Steroid receptors are dimers of zinc-finger proteins that reside within the nucleus (except for the glucocorticoid receptor which resides in the cytosol until it binds its ligand).
In either case, binding triggers an allosteric change in the protein which, in turn, triggers the formation of a "second messenger" within the cell.
users.rcn.com /jkimball.ma.ultranet/BiologyPages/C/CellSignaling.html   (2087 words)

  
 Regulation of mGlu4 Metabotropic Glutamate Receptor Signaling by Type-2 G-Protein Coupled Receptor Kinase (GRK2) -- Iacovelli et al. 65 (5): 1103 -- Molecular Pharmacology
Mundell SJ, Pula G, Carswell K, Roberts PJ, and Kelly E (2003) Agonist-induced internalization of metabotropic glutamate receptor 1A: structural determinants for protein kinase C- and G protein-coupled receptor kinase-mediated internalization.
Aramori I, Ferguson SS, Bieniasz PD, Zhang J, Cullen B, and Caron MG (1997) Molecular mechanism of desensitization of the chemokine receptor CCR-5: receptor signaling and internalization are dissociable from its role as an HIV-1 co-receptor.
of all the pathways that are mediated by the receptor.
molpharm.aspetjournals.org /cgi/content/full/65/5/1103   (4354 words)

  
 G-protein coupled receptor
The melatonin 1 (MT 1) receptor, a G-protein-coupled receptor that is...
It acts by activating a seven transmembrane domain G protein- coupled receptor of 423 amino acids expressed by the somatotroph cells of the pituitary gland...
D151746 is an inhibitor of a G- protein coupled receptor (GPCR) encoded by a gene deCODE has shown to confer a two- to seven-fold increase in risk of...
www.mongabay.com /igapo/biotech/G-protein_coupled_receptor.html   (665 words)

  
 Molecular Modeling of G-protein Coupled Receptor Kinase 2: Docking and Biochemical Evaluation of Inhibitors
Agonist-dependent phosphorylation of the alpha 2-adrenergic receptor by the beta-adrenergic receptor kinase.
The conserved lysine of the catalytic domain of protein kinases is actively involved in the phosphotransfer reaction and not required for anchoring ATP.
Effects of suramin, an anti-human immunodeficiency virus reverse transcriptase agent, on protein kinase C: Differential activation and inhibition of protein kinase C isozymes.
www.aapspharmsci.org /view.asp?art=ps020102   (6090 words)

  
 Role of the G-Protein-Coupled Receptor GPR12 as High-Affinity Receptor for Sphingosylphosphorylcholine and Its Expression and Function in Brain Development -- Ignatov et al. 23 (3): 907 -- Journal of Neuroscience
Kochl R, Alken M, Rutz C, Krause G, Oksche A, Rosenthal W, Schulein R (2002) The signal peptide of the G protein-coupled human endothelin B receptor is necessary for translocation of the N-terminal tail across the endoplasmic reticulum membrane.
Zhu K, Baudhuin LM, Hong G, Williams FS, Cristina KL, Kabarowski JH, Witte ON, Xu Y (2001) Sphingosylphosphorylcholine and lysophosphatidylcholine are ligands for the G protein-coupled receptor GPR4.
The expression of RNA for the three receptors was probed by RT-PCR with primers common in mouse and human to amplify fragments of comparable lengths: 690 base pairs for GPR12, 769 base pairs for GPR4, and 714 base pairs for OGR1.
www.jneurosci.org /cgi/content/full/23/3/907   (4621 words)

  
 59451.010816&ELEMENT_SET=DECL
Activation of the GPCR is measured by a read-out for interaction of the receptor with a regulatory component such as arrestin, G-protein, GRK or other kinases, the binding of which to the receptor is dependent upon agonist occupation of the receptor.
The protein partners are expressed as fusion proteins to the mutant, complementing enzyme and are used to monitor activation of the GPCR.
A further aspect of the present invention is a method of assessing GPCR pathway activity in the presence of a test G-protein.
www.wipo.int /cgi-pct/guest/getbykey5?KEY=01/59451.010816&ELEMENT_SET=DECL   (4626 words)

  
 Human protein: O15552 - Free fatty acid receptor 2 (G-protein coupled receptor 43). EMBL Bioinformatics Harvester
The orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.
Belongs to the G-protein coupled receptor 1 family.
Receptor for short chain fatty acids through a G(i)- protein-mediated inhibition of adenylyl cyclase and elevation of intracellular calcium.
harvester.embl.de /harvester/O155/O15552.htm   (818 words)

  
 Heterodimeric Opioid G-Protein Coupled Receptor
Understanding possible differences in the affinity and efficacy of various agonists and antagonists for the various forms of these receptors and their differential ability to transmit signals will help explain the differences in the physiological responses induced and will be instrumental in identifying and developing novel therapeutic compounds and formulations.
Their current research relates to the discovery that the opioid receptors are capable of forming functional heterodimers.
There is a significant clinical need for the development of new, more selective, drugs that interact with the opioid system for the analgesic uses and for several other diseases where the opioid receptors interact with other receptors.
www.med.nyu.edu /oil/tech/therapeutics/topioid.html   (316 words)

  
 GeneCard for MRGPRD
Identification of G protein-coupled receptor genes from the human genome sequence.
Atypical expansion in mice of the sensory neuron-specific Mrg G protein-coupled receptor family.
Identification of a G protein-coupled receptor specifically responsive to beta-alanine.
www.genecards.org /cgi-bin/carddisp.pl?gene=MRGPRD   (616 words)

  
 Identification and Characterization of Mouse Metastasis-suppressor KiSS1 and Its G-Protein-coupled Receptor -- Stafford et al. 62 (19): 5399 -- Cancer Research
Inhibition of cell migration by activation of the mKiSS1 receptor.
in the mitogen-activated protein kinase signaling pathways and
M1R is a GPCR that is activated by carbachol and is used as the positive control in the experiment.
cancerres.aacrjournals.org /cgi/content/full/62/19/5399   (3846 words)

  
 Inhibition of Experimental Intimal Thickening in Mice Lacking a Novel G-Protein-Coupled Receptor -- Tsukada et al. 107 (2): 313 -- Circulation
Sequence alignment of the G-protein coupled receptor superfamily.
Structure and function of receptors coupled to G proteins.
G protein-coupled receptors: functional and mechanistic insights through altered gene expression.
circ.ahajournals.org /cgi/content/full/107/2/313   (2689 words)

  
 GPCRDB home page
Information on G proteins have been removed from the GPCRDB and are now available (24-May-05) via the GPCRIPDB (GPCR interacting partners DB) along with the RAMP proteins.
The GPCRDBsup in collaboration with L. Holm and A. Heger at the EBI (GPCRs and putative GPCRs entries in the TrEMBL databank).
There is a discussion forum on GPCRs provided by Scientist Solutions.
www.gpcr.org /7tm   (299 words)

  
 The Lymnaea Cardioexcitatory Peptide (LyCEP) Receptor: A G-Protein-Coupled Receptor for a Novel Member of the RFamide Neuropeptide Family -- Tensen et al. 18 (23): 9812 -- Journal of Neuroscience
and VI of G-protein-coupled neuropeptide receptors (Probst, 1992
Probst WC, Lenore AS, Schuster DI, Brosius J, Sealfon SC (1992) Sequence alignment of the G-protein-coupled receptor superfamily.
Okamoto T, Nishimoto I (1992) Detection of G protein-activator regions in M4 subtype muscarinic, cholinergic, and alpha 2-adrenergic receptors based upon characteristics in primary structure.
www.jneurosci.org /cgi/content/full/18/23/9812   (6152 words)

  
 Domain swapping in G-protein coupled receptor dimers
This may be interpreted by assuming that the basal activity of G-protein coupled receptors is related to the rate of dimer formation and that dimer formation is greatly assisted by agonist binding or a higher concentration of receptors.
The simulations are consistent with, but do not prove, the idea that the active high affinity form of the receptor is the domain swapped dimer, and that the role of agonist is to shift the equilibrium in favour of the domain swapped dimer.
The phenomena of regaining activity by mixing defective multimeric proteins has been known for a long time (Fincham, 1962, Fincham and Pateman, 1957, Garen and Garen, 1963, Schlesinger and Levinthal, 1963) and so it is quite plausible that similar mechanisms may occur for domain swapped multidomain proteins.
www.essex.ac.uk /bs/staff/reync/ds/dimer.html   (2990 words)

  
 G2A Is a Proton-sensing G-protein-coupled Receptor Antagonized by Lysophosphatidylcholine -- Murakami et al. 279 (41): 42484 -- Journal of Biological Chemistry
of the receptor protein on the plasma membrane of G2A-transfected
gene assay, the G2A signaling pathway is coupled to Rho GTPase.
response of the mutant protein to protons or because of the
www.jbc.org /cgi/content/full/279/41/42484   (5837 words)

  
 GPCR Subfamily Classifier
We have omitted several GPCR subfamily SVM classifiers from the system because they contain only one known member and this is insufficient to train good quality models.
All training data for the GPCR subfamily SVM classifiers was taken from the GPCRDB information system, a curated database of GPCRs developed by Gert Vriend and Florence Horn.
Hierarchical index of all GPCR subfamily training sets used to build the classifiers.
www.soe.ucsc.edu /research/compbio/gpcr-subclass   (334 words)

  
 A Novel G-Protein-Coupled Neuronal Receptor Active in Neurosecretion
It is an orphan receptor in that the actual endogenous ligand for it is not known.
In contrast with other known serpentine receptors, CIRL consists of two large subunits that are the result of endogenous proteolytic cleavage of a precursor polypeptide.
The second subunit of CIRL, p85, is an integral membrane protein with seven membrane-spanning segments and a large C-terminal cytoplasmic domain with proline-rich clusters.
www.med.nyu.edu /oil/tech/biotech/bpetrnk.html   (547 words)

  
 GeneCard for P2RY13
Wang L. Erlinge D. Identification of G protein-coupled receptor genes from the human genome sequence.
Lee D.K. O'Dowd B.F. Identification of a novel human ADP receptor coupled to Gi.
Takeda S. Mitaku S. P2Y(13): identification and characterization of a novel Galphai-coupled ADPreceptor from human and mouse.
www.genecards.org /cgi-bin/carddisp.pl?gene=P2RY13   (718 words)

  
 Kinetics of G-protein-coupled receptor signallingand desensitization
The kinetics of G-protein-coupled receptor activation and deactivation has, so far, been measured only
as G-protein subunit rearrangement) and the kinetics of receptor inactivation by arrestins (measured as
agonist (measured as conformational change in the receptor), the kinetics of G-protein activation (measured
biowww.net /detail-646.html   (152 words)

  
 Quantification of G-Protein Coupled Receptor Internalization Using G-Protein Coupled Receptor-Green Fluorescent Protein Conjugates with the ArrayScanTM High-Content Screening System -- Conway et al. 4 (2): 75 -- Journal of Biomolecular Screening
Quantification of G-Protein Coupled Receptor Internalization Using G-Protein Coupled Receptor-Green Fluorescent Protein Conjugates with the ArrayScanTM High-Content Screening System -- Conway et al.
Dynamic Interaction of Human Vasopressin/Oxytocin Receptor Subtypes with G Protein-coupled Receptor Kinases and Protein Kinase C after Agonist Stimulation
for receptor mimetics and antagonists of receptor internalization
jbx.sagepub.com /cgi/content/abstract/4/2/75   (528 words)

  
 www.gpcr.org
The GPCRDB: a Molecular-Specific Information System for G Protein-Coupled Receptors (created in 1994)
The GPCRIPDB: a Molecular-Specific Information System for GPCR Interacting Partners (G proteins & RAMPs) (created May, 23 2005)
Visit this site to get some information on the MCSIS methodology.
www.gpcr.org   (126 words)

  
 Dopamine receptor -- Facts, Info, and Encyclopedia article
The D1 receptor is coupled to (additional info and facts about adenylate cyclase) adenylate cyclase via a stimulatory (additional info and facts about G protein) G protein
The D5 receptor is coupled to (additional info and facts about adenylate cyclase) adenylate cyclase via a stimulatory (additional info and facts about G protein) G protein
The D2 receptor is negatively coupled to (additional info and facts about adenylate cyclase) adenylate cyclase via an inhibitory (additional info and facts about G protein) G protein
www.absoluteastronomy.com /encyclopedia/d/do/dopamine_receptor.htm   (146 words)

  
 G Protein Couple Receptors (GPCRs)
G Protein Coupled Receptors (GPCRs): Predicted Ligands and Coupled G Proteins
ENSEMBL:ENSP00000250298 Tax_Id=9606 G protein-coupled receptor homolog clone G3 (Fragment)
ENSEMBL:ENSP00000297912 Tax_Id=9606 G protein-coupled receptor homolog clone H8 (Fragment)
mathbio.nimr.mrc.ac.uk /goldstein/GPCR   (146 words)

  
 The SA-MRC/UK-MRC Transnational Research Group in Molecular Reproductive Endocrinology
The MRC Research Group for Receptor Biology has two major complementary research themes, the structure, function and theoretical pharmacology of G protein-coupled receptors and the role and regulation of G protein-coupled receptors in reproductive health and disease.
Lastly, We are investigating the structural basis of HIV recognition by the chemokine receptor CCR5, which is a G protein-coupled receptor and was found to be a necessary co-receptor in HIV infection.
Our extensive experience with GnRH receptors has allowed us to broaden our program to include other G protein-coupled receptor systems that affect reproductive health.
web.uct.ac.za /depts/mbi/groupkatz.htm   (146 words)

  
 British Journal of Pharmacology - Exploring the dynamics of regulation of G protein-coupled receptors using green fluorescent protein
ZHANG, J.,, FERGUSON, S.S.,, BARAK, L.S.,, ABER, M.J.,, GIROS, B.,, LEFKOWITZ, R.J. and, CARON, M.G. (1998a) Molecular mechanisms of G protein-coupled receptor signaling: role of G protein-coupled receptor kinase and arrestins in receptor desensitization and resensitization..
IACCARINO, G.,, TOMHAVE, E.D.,, LEFKOWITZ, R.J. and, KOCH, W.J. (1998) Reciprocal in vivo regulation of myocardial G protein-coupled receptor kinase expression by beta-adrenergic receptor stimulation and blockade..
As GFP is a 27 kDa protein it is greater than 50% of the size of the majority of family 1 and family 2 GPCRs.
www.nature.com /bjp/journal/v128/n3/full/0702824a.html   (146 words)

  
 Center for Matrix Biology - Vanderbilt University and Medical Center
CXCL1-2 proteins bind to a family of 7-transmembrane G-protein coupled receptors and binding to these receptors results in immediate changes in intracellular Ca+2, phosphorylation of the receptor itself, activation of tyrosine and serine protein kinases, and increases in GTP binding to G proteins coupled to the receptor.
Since the proteins which are involved in each of these processes have not been elucidated for the chemokine receptors, we are working to characterize chemokine receptor regulatory proteins, based upon our identification of proteins interacting with the carboxy-tail of the MGSA receptor using a two-hybrid screen.
» Fan, G H, Yang, W, Wang, X J, Qian, Q, Richmond, A Identification of a motif in the carboxyl terminus of CXCR2 that is involved in adaptin 2 binding and receptor internalization Biochemistry 2001.
www.mc.vanderbilt.edu /cmb/indiv_member.php?id=61   (146 words)

  
 Oligo Annotation AGhsA020203
cellular process -> cell communication -> signal transduction -> cell surface receptor linked signal transduction -> G-protein coupled receptor protein signaling pathway
cellular process -> cell communication -> signal transduction -> cell surface receptor linked signal transduction -> G-protein coupled receptor protein signaling pathway -> G-protein signaling, coupled to IP3 second messenger (phospholipase C activating) -> muscarinic acetylcholine receptor, phospholipase C activating pathway
guanine nucleotide binding protein (g protein), alpha 15 (gq class); gna15
bio.hitachi-sk.co.jp /acegene/human30k/search_30k/human30k_oligo_annotation/aghsa/020203.html   (1525 words)

  
 Mark E. Dumont - Faculty Page
Signal transduction by G protein coupled receptors occurs when an activated receptor interacts with a trimeric G protein in the cytoplasm, causing the G protein to release a bound molecule of GDP and to replace it with a molecule of GTP.
G protein signaling: G protein coupled receptors mediate cellular responses to a variety of sensory stimuli, hormones, growth factors, and neurotransmitters and are targets of a number of widely prescribed drugs.
We are using a combination of genetic and biochemical methods to study the yeast α-factor receptor that prepares yeast cells for mating in response to binding of the mating pheromone, α-factor.
dbb.urmc.rochester.edu /bcbp/members/faculty/Dumont_Mark.HTMl   (720 words)

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