Research Topics
| M M RosenkildeSummaryAffiliation: Laboratory for Molecular Pharmacology Country: Denmark Publications
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Publications
Molecular pharmacological phenotyping of EBI2. An orphan seven-transmembrane receptor with constitutive activityMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, University of Copenhagen, Denmark
J Biol Chem 281:13199-208. 2006..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...- Virus-encoded chemokine receptors--putative novel antiviral drug targetsMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, Buildn 18 6, Blegdamsvej 3, 2200 Copenhagen N, Denmark
Neuropharmacology 48:1-13. 2005..as novel antiviral strategies--will be highlighted here together with the potentials of the virus-encoded chemokines and chemokine-binding proteins as novel anti-inflammatory biopharmaceutical strategies... - Conformational constraining of inactive and active States of a seven transmembrane receptor by metal ion site engineering in the extracellular end of transmembrane segment VMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, Denmark
Mol Pharmacol 70:1892-901. 2006..Based on the complex action of Zn(II) and on the chemokine interaction for [R208H;R212H]-ORF74, we conclude that the extracellular end of TM-V is important for the activation of this CXC-chemokine receptor... - The chemokine system -- a major regulator of angiogenesis in health and diseaseMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, Copenhagen, Denmark
APMIS 112:481-95. 2004.... - GluVII:06--a highly conserved and selective anchor point for non-peptide ligands in chemokine receptorsMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, Copenhagen University, Denmark
Curr Top Med Chem 6:1319-33. 2006..It is envisioned that knowledge of this binding mode can be exploited in structure-based discovery and design of novel chemokine receptor ligands and especially ligands with specifically optimized properties... - Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptorMette M Rosenkilde
Department of Pharmacology, University of Copenhagen, The Panum Institute, DK 2200 Copenhagen, Denmark
J Biol Chem 279:3033-41. 2004..We suggest that non-peptide antagonists with, for example, improved oral bioavailability can be designed to mimic this interaction and thereby efficiently and selectively block the CXCR4 receptor... - High constitutive activity of a virus-encoded seven transmembrane receptor in the absence of the conserved DRY motif (Asp-Arg-Tyr) in transmembrane helix 3Mette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute 18 6, Blegdamsvej 3, 2200 Copenhagen N, Denmark
Mol Pharmacol 68:11-9. 2005..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... - Targeting herpesvirus reliance of the chemokine systemMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, Panum Institute, University of Copenhagen, Copenhagen, Denmark
Curr Drug Targets 7:103-18. 2006..Therefore, blocking the signaling of these receptors will provide an efficient and highly specific way to inhibit viral replication in vivo and disease progression in the hosts... - Potency of ligands correlates with affinity measured against agonist and inverse agonists but not against neutral ligand in constitutively active chemokine receptorM M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, DK 2200 Copenhagen, Denmark
Mol Pharmacol 57:602-9. 2000.... - Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptorMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, The Panum Institute, University of Copenhagen, Copenhagen DK 2200, Denmark
J Biol Chem 282:27354-65. 2007..It is suggested that the remaining cyclam ring of AMD3465, which ensures the efficacious blocking of the receptor, in a similar manner can be replaced by chemical moieties allowing for, for example, oral bioavailability... 
Structural motifs of importance for the constitutive activity of the orphan 7TM receptor EBI2: analysis of receptor activation in the absence of an agonistTau Benned-Jensen
Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, The Panum Institute, Copenhagen University, Blegdamsvej 2, 2200 Copenhagen, Denmark
Mol Pharmacol 74:1008-21. 2008....
Tumorigenesis induced by the HHV8-encoded chemokine receptor requires ligand modulation of high constitutive activityP J Holst
Laboratory for Molecular Pharmacology, Department of Pharmacology, Panum Institute, University of Copenhagen, Copenhagen, Denmark
J Clin Invest 108:1789-96. 2001..These results indicate that induction of the KS-like disease in transgenic mice by ORF74 requires not only high constitutive signaling activity but also modulation of this activity by endogenous chemokines...- Virally encoded 7TM receptorsM M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, Panum Institute, DK-2200, Denmark
Oncogene 20:1582-93. 2001..Thus, this and other virally encoded 7TM receptors appear to be attractive future drug targets... - The carboxyl terminus of human cytomegalovirus-encoded 7 transmembrane receptor US28 camouflages agonism by mediating constitutive endocytosisMaria Waldhoer
Laboratory for Molecular Pharmacology, Panum Institute, University of Copenhagen, Copenhagen DK 2200, Denmark
J Biol Chem 278:19473-82. 2003..This demonstrates for the first time that the endocytic properties of a 7TM receptor can camouflage the agonist properties of a ligand... - Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2P C Jensen
Department of Neuroscience and Pharmacology, Copenhagen University, Copenhagen, Denmark
Br J Pharmacol 166:258-75. 2012..Here we describe a novel piperidine-based compound with structural similarity to previously described CCR8-specific agonists, but containing a unique phenyl-tetrazol moiety which, in addition to activity at CCR8 was also active at CCR1... - Targeting CXCR4 in HIV cell-entry inhibitionA Steen
Department of Neuroscience and Pharmacology, Faculty of Health Sciences, Copenhagen University, Copenhagen, Denmark
Mini Rev Med Chem 9:1605-21. 2009.... - Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variantsT Benned-Jensen
Department of Neuroscience and Pharmacology, The Panum Institute, Copenhagen University, Denmark
Br J Pharmacol 159:1092-105. 2010..Hence, we investigated gene expression and ligand-binding profiles of both splice variants and furthermore uncovered and characterized constitutive activity of both isoforms... - Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interactionArne Heydorn
Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Copenhagen, Denmark
Mol Pharmacol 66:250-9. 2004.... - Similar activation of signal transduction pathways by the herpesvirus-encoded chemokine receptors US28 and ORF74Katherine A McLean
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, 2200 Copenhagen N, Denmark
Virology 325:241-51. 2004..As ORF74 is a known inducer of neoplasia, these findings may have important implications for cytomegalovirus-associated pathogenicity... - The role of transmembrane segment II in 7TM receptor activationT Benned-Jensen
Institute for Neuroscience and Pharmacology, The Panum Institute, Copenhagen University, Copenhagen N, Denmark
Curr Mol Pharmacol 2:140-8. 2009.... - Agonists and inverse agonists for the herpesvirus 8-encoded constitutively active seven-transmembrane oncogene product, ORF-74M M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, Panum Institute, University of Copenhagen, DK 2200 Copenhagen, Denmark
J Biol Chem 274:956-61. 1999..ORF-74 could serve as a target for the development of non-peptide inverse agonist drugs as demonstrated by the effect of Zn2+ on the metal ion site-engineered receptor... - Molecular interaction of a potent nonpeptide agonist with the chemokine receptor CCR8Pia C Jensen
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, Copenhagen University, Blegdamsvej 2, 2200 Copenhagen, Denmark
Mol Pharmacol 72:327-40. 2007.... - The CXC chemokine receptor encoded by herpesvirus saimiri, ECRF3, shows ligand-regulated signaling through Gi, Gq, and G12/13 proteins but constitutive signaling only through Gi and G12/13 proteinsMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, Panum Institute, University of Copenhagen, 2200 Copenhagen N, Denmark
J Biol Chem 279:32524-33. 2004..The results suggest that the unique ligand selectivity of ECRF3 among ORF74 receptors could reflect differences in the cellular tropism of the gamma(2)-herpesviruses... - Chapter 8. Activation mechanisms of chemokine receptorsPia C Jensen
Department of Neuroscience and Pharmacology, Laboratory for Molecular Pharmacology, The PanumInstitute, University of Copenhagen, Copenhagen, Denmark
Methods Enzymol 461:171-90. 2009..This also brings up the interesting discussion of allosterism, because small molecules in the chemokine field often interact with allosteric receptor sites... - Molecular mechanism of 7TM receptor activation--a global toggle switch modelThue W Schwartz
Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, and 7TM Pharma A S, Hørsholm, Denmark
Annu Rev Pharmacol Toxicol 46:481-519. 2006.... - Ligand binding and micro-switches in 7TM receptor structuresRie Nygaard
Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen, DK 2200, Denmark
Trends Pharmacol Sci 30:249-59. 2009..e. especially TM-VI), which performs the large, global toggle switch movements connecting ligand binding with intracellular signaling... - Prohormone convertase 1/3 is essential for processing of the glucose-dependent insulinotropic polypeptide precursorRandi Ugleholdt
Department of Medical Physiology, The Panum Institute, University of Copenhagen, Blegdamsvej 3, DK 2200 Copenhagen N, Denmark
J Biol Chem 281:11050-7. 2006.... - Kaposi sarcoma-associated herpes virus targets the lymphotactin receptor with both a broad spectrum antagonist vCCL2 and a highly selective and potent agonist vCCL3Hans R Lüttichau
Laboratory for Molecular Pharmacology, Panum Institute, 18 6, Blegdamsvej 3, DK 2200 Copenhagen N, Denmark
J Biol Chem 282:17794-805. 2007.... - Positive versus negative modulation of different endogenous chemokines for CC-chemokine receptor 1 by small molecule agonists through allosteric versus orthosteric bindingPia C Jensen
Department of Neuroscience and Pharmacology, Copenhagen University, Blegdamsvej 3, DK 2200, Copenhagen, Denmark
J Biol Chem 283:23121-8. 2008.... - Exendin-4, but not dipeptidyl peptidase IV inhibition, increases small intestinal mass in GK ratsLotte Simonsen
Department of Biomedical Sciences, Panum Institute, University of Copenhagen, Blegdamsvej 3, DK 2200 Copenhagen N, Denmark
Am J Physiol Gastrointest Liver Physiol 293:G288-95. 2007..In conclusion, the continued presence of Ex-4 is necessary to maintain weight loss in GK rats. Effective antihyperglycemic treatment with Ex-4 increases intestinal mass reversibly, whereas DPPIV-I lacks intestinal effects... - Activation of the CXCR3 chemokine receptor through anchoring of a small molecule chelator ligand between TM-III, -IV, and -VIMette M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, University of Copenhagen, Blegdamsvej 3b, DK 2200, Copenhagen, Denmark
Mol Pharmacol 71:930-41. 2007..It is proposed that in rhodopsin-like 7TM receptors, small-molecule compounds in general act as agonists in a similar manner as here demonstrated with the artificial, metal ion site anchored chelators, by holding TM-VI bent inward... - GIP-(3-42) does not antagonize insulinotropic effects of GIP at physiological concentrationsCarolyn F Deacon
Dept of Medical Physiology, The Panum Institute, Blegdamsvej 3, DK 2200 Copenhagen N, Denmark
Am J Physiol Endocrinol Metab 291:E468-75. 2006..We conclude that, although GIP-(3-42) can weakly antagonize cAMP accumulation and insulin output in vitro, it does not behave as a physiological antagonist in vivo... - Microbiological exploitation of the chemokine systemPeter J Holst
Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, Denmark
Microbes Infect 5:179-87. 2003.... - Virally encoded chemokines and chemokine receptors in the role of viral infectionsPeter J Holst
Laboratory for Molecular Pharmacology, Department of Pharmacology, Panum Institute, Copenhagen, Denmark
Contrib Microbiol 10:232-52. 2003..These have already had their potential demonstrated in animal models and may in their native or modified forms represent useful therapies in humans... - High content screening for G protein-coupled receptors using cell-based protein translocation assaysCharlotta Granas
BioImage A S, Copenhagen, Denmark
Comb Chem High Throughput Screen 8:301-9. 2005.... - Molecular requirements for inhibition of the chemokine receptor CCR8--probe-dependent allosteric interactionsP C Rummel
Department of Neuroscience and Pharmacology, Faculty of Health Sciences, Copenhagen University, Copenhagen, Denmark
Br J Pharmacol 167:1206-17. 2012..This structure differs from the predominant pharmacophore for most small-molecule CC-chemokine receptor antagonists, which in fact activate CCR8, suggesting that CCR8 inhibition requires alternative structural probes... - The CCR5 receptor acts as an alloantigen in CCR5Delta32 homozygous individuals: identification of chemokineand HIV-1-blocking human antibodiesH J Ditzel
Department of Clinical Immunology, Copenhagen University Hospital, Rigshospitalet, DK 2200 Copenhagen, Denmark
Proc Natl Acad Sci U S A 95:5241-5. 1998..The identified human antibodies to CCR5 define an alloantigen that may cause allograft rejection in a mismatch situation even in individuals with no history of blood transfusions or i.v. drug abuse... - Structure, function and physiological consequences of virally encoded chemokine seven transmembrane receptorsM M Rosenkilde
Laboratory for Molecular Pharmacology, Department of Pharmacology, University of Copenhagen, Copenhagen, Denmark
Br J Pharmacol 153:S154-66. 2008..Finally, we highlight the emerging impact of these receptor on virus-mediated diseases... - Porcine glucagon-like peptide-2: structure, signaling, metabolism and effectsNis B Pedersen
Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark
Regul Pept 146:310-20. 2008..In conclusion, pGLP-2 and hGLP-2 have similar effects in vivo and in vitro in spite of the structural differences. However, pGLP-2 is cleared more rapidly in pigs than hGLP-2... - Mutations at the CXCR4 interaction sites for AMD3100 influence anti-CXCR4 antibody binding and HIV-1 entrySigrid Hatse
Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
FEBS Lett 546:300-6. 2003..3. Thus, resistance of HIV-1 NL4.3 to AMD3100 is associated with a decreased dependence of the viral gp120 on Asp(262) of CXCR4, pointing to a different mode of interaction of wild-type versus AMD3100-resistant virus with CXCR4... - Epstein-Barr virus-encoded BILF1 is a constitutively active G protein-coupled receptorSarah J Paulsen
Clinical Research Unit, Copenhagen University Hospital, Hvidovre, Denmark
J Virol 79:536-46. 2005..We suggest that EBV may use BILF1 to regulate Galphai-activated pathways during viral lytic replication, thereby affecting disease progression... - 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 specificityEvi Kostenis
7TM Pharma, Fremtidsvej 3, 2970 Hoersholm, Denmark
J Pharmacol Exp Ther 313:78-87. 2005.... - AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitorSigrid Hatse
Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
Biochem Pharmacol 70:752-61. 2005.... - Functional analysis of the murine cytomegalovirus chemokine receptor homologue M33: ablation of constitutive signaling is associated with an attenuated phenotype in vivoRuth Case
Clinical Medical Virology Centre, University of Queensland, Sir Albert Sakzewski Virus Research Centre, Royal Children s Hospital, Herston 4029, Queensland, Australia
J Virol 82:1884-98. 2008..In addition, HCMV UL33 was found to partially compensate for the lack of M33 in vivo, suggesting conserved biological roles of the UL33 gene family... - Modest human immunodeficiency virus coreceptor function of CXCR3 is strongly enhanced by mimicking the CXCR4 ligand binding pocket in the CXCR3 receptorSigrid Hatse
Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
J Virol 81:3632-9. 2007..Moreover, the CXCR4 antagonist AMD3100 exhibited antagonistic and anti-HIV activities in U87.CD4.CXCR3[K300A, S304E] cells but not in U87.CD4.CXCR3[WT] cells...