Experts and Doctors on g protein coupled receptors in Denmark


Locale: Denmark
Topic: g protein coupled receptors

Top Publications

  1. Nygaard R, Valentin Hansen L, Mokrosinski J, Frimurer T, Schwartz T. Conserved water-mediated hydrogen bond network between TM-I, -II, -VI, and -VII in 7TM receptor activation. J Biol Chem. 2010;285:19625-36 pubmed publisher
  2. Bonde M, Yao R, Ma J, Madabushi S, Haunsø S, Burstein E, et al. An angiotensin II type 1 receptor activation switch patch revealed through evolutionary trace analysis. Biochem Pharmacol. 2010;80:86-94 pubmed publisher
    ..More broadly, these observations in the AT1 receptor are consistent with computational predictions of a generic role for this patch in 7TM receptor activation. ..
  3. Bahrami S, Duch M, Pedersen F. Ligand presentation on a synthetic flexible hinge in Moloney murine leukemia virus SU supports entry via a heterologous receptor. Virology. 2007;363:303-9 pubmed
    ..Hence, the immediate context of ligand presentation is critical for infectivity via a heterologous receptor. ..
  4. Kostenis E, Martini L, Ellis J, Waldhoer M, Heydorn A, Rosenkilde M, et al. A highly conserved glycine within linker I and the extreme C terminus of G protein alpha subunits interact cooperatively in switching G protein-coupled receptor-to-effector specificity. J Pharmacol Exp Ther. 2005;313:78-87 pubmed
  5. Frimurer T, Ulven T, Elling C, Gerlach L, Kostenis E, Hogberg T. A physicogenetic method to assign ligand-binding relationships between 7TM receptors. Bioorg Med Chem Lett. 2005;15:3707-12 pubmed
    ..A case targeting the newly identified prostaglandin D2 receptor CRTH2 serves as a primary example to illustrate the procedure. ..
  6. Kiryushko D, Novitskaya V, Soroka V, Klingelhofer J, Lukanidin E, Berezin V, et al. Molecular mechanisms of Ca(2+) signaling in neurons induced by the S100A4 protein. Mol Cell Biol. 2006;26:3625-38 pubmed
    ..Thus, glycosaminoglycans may act as coreceptors of S100 proteins in neurons. This may provide a mechanism by which S100 proteins could locally regulate neuronal plasticity in connection with brain lesions and neurological disorders. ..
  7. Eriksen J, Jørgensen T, Gether U. Regulation of dopamine transporter function by protein-protein interactions: new discoveries and methodological challenges. J Neurochem. 2010;113:27-41 pubmed publisher
  8. Rosenkilde M, Kledal T, Schwartz T. High constitutive activity of a virus-encoded seven transmembrane receptor in the absence of the conserved DRY motif (Asp-Arg-Tyr) in transmembrane helix 3. Mol Pharmacol. 2005;68:11-9 pubmed
    ..It is concluded that the Arg of the DRY motif in transmembrane helix 3 is not essential for G protein coupling based on the constitutive as well as the ligand-mediated activity observed for ORF74-EHV2. ..
  9. Kostenis E, Waelbroeck M, Milligan G. Techniques: promiscuous Galpha proteins in basic research and drug discovery. Trends Pharmacol Sci. 2005;26:595-602 pubmed
    ..Emphasis is given to novel promiscuous and chimeric Galpha proteins. Because of their ability to interact with a wide range of GPCRs, such novel G proteins are likely to be incorporated rapidly into drug discovery programmes. ..

More Information


  1. Wellendorph P, Brauner Osborne H. Molecular cloning, expression, and sequence analysis of GPRC6A, a novel family C G-protein-coupled receptor. Gene. 2004;335:37-46 pubmed
    ..Analysis of the intron-exon composition of the GPRC6A gene confirms that isoforms 2 and 3 are naturally occurring splice variants. ..
  2. Wellendorph P, Hansen K, Balsgaard A, Greenwood J, Egebjerg J, Brauner Osborne H. Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids. Mol Pharmacol. 2005;67:589-97 pubmed
    ..This study demonstrates the utility of a chimeric receptor approach in combination with molecular modeling, for elucidating agonist interaction with GPRC6A, a novel family C G-protein-coupled receptor. ..
  3. Benned Jensen T, Rosenkilde M. Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variants. Br J Pharmacol. 2010;159:1092-105 pubmed publisher
    ..In turn, our results indicate that the two human isoforms might serve tissue-specific functions. ..
  4. Hauser F, Cazzamali G, Williamson M, Blenau W, Grimmelikhuijzen C. A review of neurohormone GPCRs present in the fruitfly Drosophila melanogaster and the honey bee Apis mellifera. Prog Neurobiol. 2006;80:1-19 pubmed publisher
    ..This is in contrast to biogenic amine GPCRs, where evolutionarily unrelated GPCRs often bind to the same biogenic amine, suggesting frequent ligand exchanges ("ligand hops") during GPCR evolution...
  5. Svendsen A, Zalesko A, Kønig J, Vrecl M, Heding A, Kristensen J, et al. Negative cooperativity in H2 relaxin binding to a dimeric relaxin family peptide receptor 1. Mol Cell Endocrinol. 2008;296:10-7 pubmed publisher
    ..Dimerization and negative cooperativity appear to be general properties of LGRs involved in reproduction as well as other GPCRs. ..
  6. Holst B, Nygaard R, Valentin Hansen L, Bach A, Engelstoft M, Petersen P, et al. A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors. J Biol Chem. 2010;285:3973-85 pubmed publisher
    ..It is concluded that Phe-V:13 can serve as an aromatic lock for the proposed active conformation of the Trp-VI:13 rotameric switch, being involved in the global movement of TM-V and TM-VI in 7TM receptor activation. ..
  7. Storjohann L, Holst B, Schwartz T. Molecular mechanism of Zn2+ agonism in the extracellular domain of GPR39. FEBS Lett. 2008;582:2583-8 pubmed publisher
  8. Svendsen A, Vrecl M, Ellis T, Heding A, Kristensen J, Wade J, et al. Cooperative binding of insulin-like Peptide 3 to a dimeric relaxin family peptide receptor 2. Endocrinology. 2008;149:1113-20 pubmed
    ..Bioluminescence resonance energy transfer (BRET(2)) experiments confirmed that RXFP2 forms constitutive homodimers. Heterodimerization between RXFP2 and RXFP1 was also observed. ..
  9. Hauser F, Williamson M, Cazzamali G, Grimmelikhuijzen C. Identifying neuropeptide and protein hormone receptors in Drosophila melanogaster by exploiting genomic data. Brief Funct Genomic Proteomic. 2006;4:321-30 pubmed
    ..In this review, we will give an update about the current knowledge of all Drosophila neuropeptide and protein hormone receptors, and discuss their phylogenetic relationships. ..
  10. Frimurer T, Bywater R. Structure of the integral membrane domain of the GLP1 receptor. Proteins. 1999;35:375-86 pubmed
  11. Holst B, Egerod K, Schild E, Vickers S, Cheetham S, Gerlach L, et al. GPR39 signaling is stimulated by zinc ions but not by obestatin. Endocrinology. 2007;148:13-20 pubmed
    ..In contrast, the potency and efficacy of Zn(2+) in respect of activating signaling indicates that this metal ion could be a physiologically relevant agonist or modulator of GPR39. ..
  12. Brauner Osborne H, Jensen A, Sheppard P, Brodin B, Krogsgaard Larsen P, O HARA P. Cloning and characterization of a human orphan family C G-protein coupled receptor GPRC5D. Biochim Biophys Acta. 2001;1518:237-48 pubmed
  13. J rgensen L, Hauser F, Cazzamali G, Williamson M, Grimmelikhuijzen C. Molecular identification of the first SIFamide receptor. Biochem Biophys Res Commun. 2006;340:696-701 pubmed publisher
    ..This paper is the first report on the identification of a SIFamide receptor...
  14. Cazzamali G, Torp M, Hauser F, Williamson M, Grimmelikhuijzen C. The Drosophila gene CG9918 codes for a pyrokinin-1 receptor. Biochem Biophys Res Commun. 2005;335:14-9 pubmed
    ..This paper is the first conclusive report that CG9918 is a Drosophila pyrokinin-1 receptor gene. ..
  15. Hamid Y, Vissing H, Holst B, Urhammer S, Pyke C, Hansen S, et al. Studies of relationships between variation of the human G protein-coupled receptor 40 Gene and Type 2 diabetes and insulin release. Diabet Med. 2005;22:74-80 pubmed
    ..Variations in the coding region of GPR40 do not appear to be associated with Type 2 diabetes or insulin release alterations. ..
  16. Rosenkilde M, Benned Jensen T, Andersen H, Holst P, Kledal T, Lüttichau H, et al. Molecular pharmacological phenotyping of EBI2. An orphan seven-transmembrane receptor with constitutive activity. J Biol Chem. 2006;281:13199-208 pubmed
    ..3. Based on the constitutive signaling and cellular expression pattern of EBI2, it is suggested that it may function in conjunction with BILF1 in the reprogramming of the cell during EBV infection. ..
  17. Secher T, Lenz C, Cazzamali G, S rensen G, Williamson M, Hansen G, et al. Molecular cloning of a functional allatostatin gut/brain receptor and an allatostatin preprohormone from the silkworm Bombyx mori. J Biol Chem. 2001;276:47052-60 pubmed publisher
    ..To our knowledge, this is the first report on the molecular cloning and functional expression of an insect gut/brain peptide hormone receptor...
  18. Tams J, Knudsen S, Fahrenkrug J. Characterization of a G protein coupling "YL" motif of the human VPAC1 receptor, equivalent to the first two amino acids in the "DRY" motif of the rhodopsin family. J Mol Neurosci. 2001;17:325-30 pubmed
  19. Iversen A, Cazzamali G, Williamson M, Hauser F, Grimmelikhuijzen C. Molecular identification of the first insect ecdysis triggering hormone receptors. Biochem Biophys Res Commun. 2002;299:924-31 pubmed
    ..Ecdysis (cuticle shedding) is an important behaviour, allowing growth and metamorphosis in insects and other arthropods. Our paper is the first report on the molecular identification of ecdysis triggering hormone receptors from insects. ..
  20. Holst B, Cygankiewicz A, Jensen T, Ankersen M, Schwartz T. High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist. Mol Endocrinol. 2003;17:2201-10 pubmed
    ..It is suggested that inverse agonists for the ghrelin receptor could be particularly interesting for the treatment of obesity. ..
  21. Christiansen E, Urban C, Merten N, Liebscher K, Karlsen K, Hamacher A, et al. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem. 2008;51:7061-4 pubmed publisher
    ..The preferred compound 20 (TUG-424, EC(50) = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity. ..
  22. Stafflinger E, Hansen K, Hauser F, Schneider M, Cazzamali G, Williamson M, et al. Cloning and identification of an oxytocin/vasopressin-like receptor and its ligand from insects. Proc Natl Acad Sci U S A. 2008;105:3262-7 pubmed publisher
    ..To our knowledge, this is the first report on the molecular cloning of an oxytocin/vasopressin-like receptor and its ligand from arthropods...
  23. Hauser F, Cazzamali G, Williamson M, Park Y, Li B, Tanaka Y, et al. A genome-wide inventory of neurohormone GPCRs in the red flour beetle Tribolium castaneum. Front Neuroendocrinol. 2008;29:142-65 pubmed
    ..It also shows that Drosophila is not a good representative of all insects, because several of the hormonal systems that we now find in Tribolium do not exist in Drosophila. ..
  24. Egerod K, Holst B, Petersen P, Hansen J, Mulder J, Hokfelt T, et al. GPR39 splice variants versus antisense gene LYPD1: expression and regulation in gastrointestinal tract, endocrine pancreas, liver, and white adipose tissue. Mol Endocrinol. 2007;21:1685-98 pubmed
  25. Wellendorph P, Burhenne N, Christiansen B, Walter B, Schmale H, Brauner Osborne H. The rat GPRC6A: cloning and characterization. Gene. 2007;396:257-67 pubmed
    ..The presented quantitative pharmacological data underlines the evolutionary conservation of GPRC6A to the rat and signifies the physiological importance and emerging pharmacological potential of GPRC6A. ..
  26. L ttichau H, Johnsen A, Jurlander J, Rosenkilde M, Schwartz T. Kaposi sarcoma-associated herpes virus targets the lymphotactin receptor with both a broad spectrum antagonist vCCL2 and a highly selective and potent agonist vCCL3. J Biol Chem. 2007;282:17794-805 pubmed publisher
  27. Jørgensen E, Knigge U, Watanabe T, Warberg J, Kjaer A. Histaminergic neurons are involved in the orexigenic effect of orexin-A. Neuroendocrinology. 2005;82:70-7 pubmed
    ..We conclude that the orexigenic effect of orexin-A is dependent on an intact histaminergic neuronal system and seems to involve an H(1)-receptor mechanism. ..
  28. Lüttichau H. The herpesvirus 8 encoded chemokines vCCL2 (vMIP-II) and vCCL3 (vMIP-III) target the human but not the murine lymphotactin receptor. Virol J. 2008;5:50 pubmed publisher
  29. Kostenis E, Milligan G, Christopoulos A, Sanchez Ferrer C, Heringer Walther S, Sexton P, et al. G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor. Circulation. 2005;111:1806-13 pubmed
    ..Consequently, the AT1-Mas complex could be of great importance as a target for pharmacological intervention in cardiovascular diseases. ..
  30. Hansen K, Stafflinger E, Schneider M, Hauser F, Cazzamali G, Williamson M, et al. Discovery of a novel insect neuropeptide signaling system closely related to the insect adipokinetic hormone and corazonin hormonal systems. J Biol Chem. 2010;285:10736-47 pubmed publisher
    ..In particular, this frequent loss of hormonal systems is unique for arthropods compared with vertebrates. ..
  31. Hansen K, Hauser F, Cazzamali G, Williamson M, Grimmelikhuijzen C. Cloning and characterization of the adipokinetic hormone receptor from the cockroach Periplaneta americana. Biochem Biophys Res Commun. 2006;343:638-43 pubmed publisher
    ..This paper describes the first AKH receptor from a hemimetabolous insect...