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Topic: G protein coupled receptors

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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)

Cell Signaling 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). 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. 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)

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 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. 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. www.essex.ac.uk /bs/staff/reync/ds/dimer.html   (2990 words)

Inhibition of Experimental Intimal Thickening in Mice Lacking a Novel G-Protein-Coupled Receptor -- Tsukada et al. 107 (2): 313 -- Circulation Structure and function of receptors coupled to G proteins. G protein-coupled receptors: functional and mechanistic insights through altered gene expression. Sequence alignment of the G-protein coupled receptor superfamily. circ.ahajournals.org /cgi/content/full/107/2/313   (2689 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 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. Probst WC, Lenore AS, Schuster DI, Brosius J, Sealfon SC (1992) Sequence alignment of the G-protein-coupled receptor superfamily. www.jneurosci.org /cgi/content/full/18/23/9812   (6152 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)

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)

A Novel G-Protein-Coupled Neuronal Receptor Active in Neurosecretion 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. It is an orphan receptor in that the actual endogenous ligand for it is not known. www.med.nyu.edu /oil/tech/biotech/bpetrnk.html   (547 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)

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 currently analyzing classes of mutations that can provide information on the structure of the α-factor receptor, on interactions between receptors, and on the mechanism of activation of G proteins by receptors. dbb.urmc.rochester.edu /bcbp/members/faculty/Dumont_Mark.html   (720 words)

RECEPTORS.doc Metabotropic Receptors Aka G-protein-coupled receptors Activation of these receptors activates a G-protein (this is shorthand for a protein that binds guanosine triphosphate (GTP) and guanosine diphosphate (GDP)). Let’s take a closer look: There are 2 main types of receptors: Ionotropic Receptors Aka ligand-gated channels Activation of these receptor directly opens or closes and ion channel. The action of iontotropic receptors is fast-acting and short-lived, whereas metabotropic receptors are slower, but may have long-lasting effects. www.sci.sdsu.edu /classes/psychology/psy760/handouts/RECEPTORS.doc   (720 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   (720 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   (720 words)

G-protein-coupled receptor - Wikipedia, the free encyclopedia G protein-coupled receptors are integral membrane proteins that possess seven membrane-spanning domains or transmembrane helices. Early structural models for G protein coupled receptors were based on their weak analogy to bacteriorhodopsin for that a structure had been determined by both electron and X ray-based crystallography. It is known that the inactive G protein is bound to the receptor in its inactive state. en.wikipedia.org /wiki/G_protein-coupled_receptor   (720 words)

coursedetail This will be followed by lectures on the three major families of receptors: the G-protein-coupled receptors (GPCR), the tyrosine kinase receptors (TK), and the ligand-gated ion channel receptors. Introductory material will include an in-depth approach to the molecular dynamics of the ligand-receptor interaction. See your health care provider for specific medical advice. www.amc.edu /Academic/research/coursedetail.cfm?id=53   (720 words)

Mark E. Dumont - Faculty Page 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. 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. Genomic approaches to membrane protein structure and function: Although membrane proteins constitute 20-30% of the coding potential of genomes, methods for analyzing their structures and functions are still primitive compared to the approaches available for studies of soluble proteins. dbb.urmc.rochester.edu /bcbp/members/faculty/Dumont_Mark.html   (720 words)

GPP - Viewbook Page for Mayer, Mark The architecture of both families of glutamate activated signaling proteins is different from that for other ligand gated ion channels on the one hand and the majority of G-protein coupled receptors on the other. These are the AMPA, kainate, NMDA and delta subtypes of ligand gated ion channels and multiple subtypes of G-protein coupled receptors. The recent success of x-ray diffraction analysis of voltage gated ion channel proteins pioneered by Rod MacKinnon is starting to provide the necessary structural framework for interpretation of functional studies on many classes of ion channels and represents a major advance in both technique and conceptual approaches. gpp.nih.gov /Researchers/Members/NICHD/MarkMayer.htm   (720 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   (720 words)

7TM receptor G protein-coupled receptor), such as the receptors of the olfactory epithelium that bind odorants and the receptors of the neurotransmitter serotonin in the mammalian brain. In cell biology and biochemistry, a 7TM receptor (or seven transmembrane receptor) is an integral membrane protein belonging to a large and ancient superfamily of transmembrane receptors. The name derives from the proteins' structure or membrane topology, which exhibits seven membrane-spanning elements or transmembrane helices. encycl.opentopia.com /term/7TM_receptor   (134 words)

Ion Channel Physiology Group Publications: NIEHS Laboratory of Neurobiology Zhu, Y., and Yakel, J.L. (1997) Modulation of Ca currents by various G protein coupled receptors in sympathetic neurons of male rat pelvic ganglia. Shao, Z. and Yakel, J.L. (2000) Single channel properties of neuronal nicotinic ACh receptors in stratum radiatum interneurons of rat hippocampal slices. Jones, S., and Yakel, J.L. (2003) Casein kinase II (protein kinase CK2) regulates serotonin 5-HT receptor channel function in NG108-15 cells. dir.niehs.nih.gov /dirln/diricp/publications.htm   (134 words)

Discovery aids membrane protein studies It allows them for the first time to produce large quantities of crucial membrane proteins for structural study or therapeutic research, such as ion channels and the vast family of receptors called G-protein coupled receptors (GPCRs). While proteins that exist freely inside the cell can be studied relatively easily once they are cloned by inserting genes into bacteria such as Escherichia coli membrane proteins are designed to be embedded in the cell membrane to function properly. This means they need to be inserted into a cell membrane when they are created, but a good method of achieving this has eluded researchers. drugresearcher.com /news/news-ng.asp?n=58420-discovery-aids-membrane   (608 words)

G protein - Wikipedia, the free encyclopedia These proteins are activated by G-protein coupled receptors and are made up of alpha (α), beta (β) and gamma (γ) subunits. There are also "small" G proteins or small GTPases like ras that are monomeric and not membrane-associated, but also bind GTP and GDP and are involved in signal transduction. G-proteins, short for guanine nucleotide binding proteins, are a family of proteins involved in second messenger cascades. en.wikipedia.org /wiki/G_protein   (608 words)

Membrane Protein Folding These methods may now be applied to G-protein-coupled receptors or other integral membrane proteins that have been indentified as potential drug targets. To this end, we are working to increase expression levels of membrane proteins and we are developing protocols to refold membrane proteins in lipid and detergent environments. Several proteins, some of which with therapeutic interest are targeted in these studies. www.faculty.virginia.edu /tamm/pages/project_folding.html   (405 words)

NDI Terminology - G protein-coupled receptors G protein-linked (or coupled) receptors mediate the cellular responses to an enormous diversity of signaling molecules, including hormones, neurotransmitters, and local mediators, which are as varied in structure as they are in function: the list includes proteins and small peptides, as well as amino acid and fatty acid derivatives. Despite the chemical and functional diversity of the signaling molecules that bind to them, all of the G protein-linked receptors whose amino acid sequences are known from DNA sequencing studies have a similar structure and are almost certainly evolutionarily related. The members of this receptor family have conserved not only their amino acid sequence but also their functional relationship to G proteins by means of which they broadcast into the interior of the cell the message that an extracellular ligand is present. www.ndif.org /Terms/G_protein-coupled_receptors.html   (405 words)

G Protein-coupled Receptors Handbook:1588293653:Devi, Lakshmi A., Ph.D.; Engel, Andreas, Ph.D.; Palczewski, Krzysztof, Ph.D. :eCampus.com G Protein-coupled Receptors Handbook:1588293653:Devi, Lakshmi A., Ph.D.; Engel, Andreas, Ph.D.; Palczewski, Krzysztof, Ph.D. :eCampus.com www.ecampus.com /bk_detail.asp?isbn=1588293653   (405 words)

OSTM1 - osteopetrosis associated transmembrane protein 1 Endogenous GIPN is concentrated along the basolateral plasma membrane of proximal and distal tubules in rat kidney, where many G protein-coupled receptors and some G proteins are also located. OSTM1 is a homologue of Ostm1 (osteopetrosis associated transmembrane protein 1) from Mus musculus. These synonyms are used for gene OSTM1 (osteopetrosis associated transmembrane protein 1): GIPN, GL, HSPC019, Osteopetrosis associated transmembrane protein 1 precursor, UNQ6098/PRO21201. www.ihop-net.org /UniPub/iHOP/gi/98674.html   (146 words)

Hormonal Genomics -- Leo et al. 23 (3): 369 -- Endocrine Reviews Kudo M, Chen T, Nakabayashi K, Hsu SY, Hsueh AJ 2000 The nematode leucine-rich repeat-containing, G protein-coupled receptor (LGR) protein homologous to vertebrate gonadotropin and thyrotropin receptors is constitutively active in mammalian cells. DNA sequences to gene transcript expression to protein function. function as binding proteins for CRH and related ligands (89). edrv.endojournals.org /cgi/content/full/23/3/369   (8467 words)

Regulation of Dopamine D1 Receptor Trafficking by Protein Kinase A-Dependent Phosphorylation -- Mason et al. 61 (4): 806 -- Molecular Pharmacology Activation of Cyclic AMP-Dependent Protein Kinase Inhibits the Desensitization and Internalization of Metabotropic Glutamate Receptors 1a and 1b Involvement of G protein-coupled receptor kinase 4 and 6 in rapid desensitization of dopamine D1 receptor in rat IEC-6 intestinal epithelial cells The aim of this study was to use pharmacological inhibition of protein kinase A and mutation of potential protein kinase A molpharm.aspetjournals.org /cgi/content/abstract/61/4/806   (493 words)

Efficient signal transduction by a chimeric yeast-mammalian G protein alpha  subunit Gpa1-Gsalpha covalently fused to the yeast receptor Ste2 -- Medici et al. 16 (24): 7241 -- The EMBO Journal Saccharomyces cerevisiae uses G protein-coupled receptors for signal transduction. Efficient signal transduction by a chimeric yeast-mammalian G protein alpha  subunit Gpa1-Gsalpha covalently fused to the yeast receptor Ste2 -- Medici et al. Coupling of the Muscarinic m2 Receptor to G Protein-activated K+ Channels via Galpha z and a Receptor-Galpha z Fusion Protein. embojournal.npgjournals.com /cgi/content/abstract/16/24/7241   (493 words)

Integrin-associated protein (CD47): an unusual activator of G protein signaling -- Brown 107 (12): 1499 -- Journal of Clinical Investigation Coughlin, S.R. Expanding horizons for receptors coupled to G proteins: diversity and disease. G protein signaling, but that some necessary signal common to Rebres, R.A., Green, J.M., Reinhold, M.I., Ticchioni, M., and Brown, E.J. Membrane raft association of CD47 is necessary for actin polymerization and protein kinase C-theta translocation in its synergistic activation of T cells. www.jci.org /cgi/content/full/107/12/1499   (493 words)

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