Birgitte Holst

Birgitte Holst

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Birgitte Holst

Publications by authors named "Birgitte Holst"

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Translating biased signaling in the ghrelin receptor system into differential in vivo functions.

Proc Natl Acad Sci U S A 2018 10 9;115(43):E10255-E10264. Epub 2018 Oct 9.

Laboratory for Molecular Pharmacology, Department of Biomedical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark;

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http://dx.doi.org/10.1073/pnas.1804003115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6205473PMC
October 2018

Hepatic NAD levels and NAMPT abundance are unaffected during prolonged high-fat diet consumption in C57BL/6JBomTac mice.

Mol Cell Endocrinol 2018 09 2;473:245-256. Epub 2018 Feb 2.

Novo Nordisk Foundation Center for Basic Metabolic Research, Section of Integrative Physiology, University of Copenhagen, Copenhagen, Denmark. Electronic address:

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http://dx.doi.org/10.1016/j.mce.2018.01.025DOI Listing
September 2018

Synthesis and Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists.

ACS Med Chem Lett 2018 May 23;9(5):496-501. Epub 2018 Apr 23.

Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium.

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http://dx.doi.org/10.1021/acsmedchemlett.8b00105DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5949835PMC
May 2018

The Apolipoprotein M/S1P Axis Controls Triglyceride Metabolism and Brown Fat Activity.

Cell Rep 2018 01;22(1):175-188

Department of Clinical Biochemistry, Rigshospitalet, 2100 Copenhagen, Denmark; Department of Biomedical Sciences, University of Copenhagen, 2200 Copenhagen, Denmark; Department of Clinical Medicine, University of Copenhagen, 2200 Copenhagen, Denmark. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2017.12.029DOI Listing
January 2018

Development of potent and proteolytically stable human neuromedin U receptor agonists.

Eur J Med Chem 2018 Jan 14;144:887-897. Epub 2017 Dec 14.

Research Group of Organic Chemistry, Departments of Chemistry and Bioengineering Sciences, Vrije Universiteit Brussel, Pleinlaan 2, 1050, Brussels, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.12.035DOI Listing
January 2018

Exploring the Behavioral and Metabolic Phenotype Generated by Re-Introduction of the Ghrelin Receptor in the Ventral Tegmental Area.

Int J Mol Sci 2017 Apr 26;18(5). Epub 2017 Apr 26.

Section for Metabolic Receptology, The Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, 2200 Copenhagen, Denmark.

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http://dx.doi.org/10.3390/ijms18050914DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5454827PMC
April 2017

Model-Based Discovery of Synthetic Agonists for the Zn-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions.

J Med Chem 2017 02 23;60(3):886-898. Epub 2017 Jan 23.

Novo Nordisk Foundation Center for Protein Research, University of Copenhagen , Blegdamsvej 3, DK-2200, Copenhagen, Denmark.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.6b00648
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http://dx.doi.org/10.1021/acs.jmedchem.6b00648DOI Listing
February 2017

GPR119, a Major Enteroendocrine Sensor of Dietary Triglyceride Metabolites Coacting in Synergy With FFA1 (GPR40).

Endocrinology 2016 Dec 25;157(12):4561-4569. Epub 2016 Oct 25.

NNF Center for Basic Metabolic Research (J.H.E., M.H., L.V.K., A.N.M., M.S.E., A.-S.H., R.S., K.L.E., B.H., T.W.S.), Section for Metabolic Receptology; Laboratory for Molecular Pharmacology (J.H.E., M.H., L.V.K., M.S.E., A.-S.H., R.S., K.L.E., B.H., T.W.S.), Department of Neuroscience and Pharmacology; and Danish Diabetes Academy (M.S.E.), 5000 Odense, Denmark; Novo Nordisk Foundation Center for Basic Metabolic Research (P.T.), Section for Metabolic Genetics, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark; Merck Research Laboratories (T.J.K., A.D.H.), Kenilworth, New Jersey 07033; Cambridge Institute for Medical Research and MRC Metabolic Diseases Unit (F.M.G., F.R.), University of Cambridge, Cambridge, CB20QQ United Kingdom; Department of Drug Design and Pharmacology (H.S.H.), University of Copenhagen, DK-2100 Copenhagen, Denmark.

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http://dx.doi.org/10.1210/en.2016-1334DOI Listing
December 2016

Functional and genetic epidemiological characterisation of the FFAR4 (GPR120) p.R270H variant in the Danish population.

J Med Genet 2016 09 11;53(9):616-23. Epub 2016 Apr 11.

Section of Metabolic Genetics, The Novo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark Faculty of Health Sciences, University of Southern Denmark, Odense, Denmark.

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http://dx.doi.org/10.1136/jmedgenet-2015-103728DOI Listing
September 2016

Effects of Peripheral Neurotensin on Appetite Regulation and Its Role in Gastric Bypass Surgery.

Endocrinology 2016 09 20;157(9):3482-92. Epub 2016 Jul 20.

Laboratory for Molecular Pharmacology (C.R., L.J.S., Z.R., B.S., A.N.M., B.Ho.), Department of Neuroscience and Pharmacology, and Department of Biomedical Sciences (B.Ha., J.J.H.), Faculty of Health Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark; Section for Metabolic Receptology (C.R., L.J.S., Z.R., B.S., A.N.M., B.Ho.) and Section for Translational Metabolic Physiology (B.Ha., J.J.H.), the Novo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark; Institute of Veterinary Physiology (T.B., C.L.F., T.A.L.), Vetsuisse Faculty, and Center for Integrative Human Physiology (T.A.L.), University of Zurich, CH-8057 Zurich, Switzerland; Institute of Biochemistry (K.B.-S., A.G.B.-S.), University of Leipzig, D-04103 Leipzig, Germany; Gubra ApS (L.S.D., J.J.), Hørsholm, DK-2970 Denmark; and Biomedicine Discovery Institute (Z.B.A.), Metabolic Disease and Obesity Program, Monash University, Melbourne, Victoria 3800, Australia.

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http://dx.doi.org/10.1210/en.2016-1329DOI Listing
September 2016

Anxiolytic-Like Effects of Increased Ghrelin Receptor Signaling in the Amygdala.

Int J Neuropsychopharmacol 2016 05 29;19(5). Epub 2016 Apr 29.

Laboratory of Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen, Denmark, and The Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, Copenhagen, Denmark (Mr Jensen, Ms Ratner, Dr Rudenko, Ms Skov, Ms Hundahl, and Dr Holst); Laboratory of Neural Plasticity, Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen, Denmark (Drs Christiansen and Woldbye).

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http://dx.doi.org/10.1093/ijnp/pyv123DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4886665PMC
May 2016

Acute disruption of glucagon secretion or action does not improve glucose tolerance in an insulin-deficient mouse model of diabetes.

Diabetologia 2016 Feb 5;59(2):363-70. Epub 2015 Nov 5.

Section for Translational Metabolic Physiology, Novo Nordisk Foundation Center for Basic Metabolic Research and Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, building 12.2, DK-2200, Copenhagen, Denmark.

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http://link.springer.com/10.1007/s00125-015-3794-2
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http://dx.doi.org/10.1007/s00125-015-3794-2DOI Listing
February 2016

Short-term effects of dietary advanced glycation end products in rats.

Br J Nutr 2016 Feb;115(4):629-36

1Department of Nutrition, Exercise and Sports,University of Copenhagen,Rolighedsvej 30,1958 Frederiksberg C,Denmark.

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http://dx.doi.org/10.1017/S0007114515004833DOI Listing
February 2016

Immune malfunction in the GPR39 zinc receptor of knockout mice: Its relationship to depressive disorder.

J Neuroimmunol 2016 Feb 2;291:11-7. Epub 2015 Dec 2.

Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, PL 30-688 Kraków, Poland; Institute of Pharmacology, Polish Academy of Sciences, Smętna 12, PeL 31-343 Kraków, Poland.

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http://dx.doi.org/10.1016/j.jneuroim.2015.12.001DOI Listing
February 2016

Neurotensin Is Coexpressed, Coreleased, and Acts Together With GLP-1 and PYY in Enteroendocrine Control of Metabolism.

Endocrinology 2016 Jan 15;157(1):176-94. Epub 2015 Oct 15.

Novo Nordisk Foundation Center for Basic Metabolic Research (K.V.G., C.F.R., B.S., M.S.E., A.N.M., J.P., M.K.N., K.L.E., F.B., J.J.H., B.H., T.W.S.), Section for Metabolic Receptology and Enteroendocrinology; Laboratory for Molecular Pharmacology (K.V.G., C.F.R., M.S.E., A.N.M., M.K.N., K.L.E., B.H., T.W.S.), Department of Neuroscience and Pharmacology; and Department of Biomedical Sciences (B.S., J.P., S.S.P., J.J.H.), Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen DK-2200, Denmark; Department of Molecular and Clinical Medicine (F.S., F.B.), Sahlgrenska Center for Cardiovascular and Metabolic Research/Wallenberg Laboratory, University of Gothenburg, 413 45 Gothenburg, Sweden; Danish Diabetes Academy (M.S.E.), 5000 Odense, Denmark; Merck Research Laboratories (A.R.N., T.K., A.D.H.), Kenilworth, NJ 07033; and Department of Pharmacology (S.O.), Max-Planck-Institute for Heart and Lung Research, 61231 Bad Nauheim, Germany.

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https://academic.oup.com/endo/article-lookup/doi/10.1210/en.
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http://dx.doi.org/10.1210/en.2015-1600DOI Listing
January 2016

In Silico Investigation of the Neurotensin Receptor 1 Binding Site: Overlapping Binding Modes for Small Molecule Antagonists and the Endogenous Peptide Agonist.

Mol Inform 2016 01 16;35(1):19-24. Epub 2015 Sep 16.

M Lückmann, B Holst, TW Schwartz, TM Frimurer, Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, Blegdamsvej 3B, 2200 Copenhagen. Denmark.

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http://dx.doi.org/10.1002/minf.201500080DOI Listing
January 2016

Bioorthogonal Labeling of Ghrelin Receptor to Facilitate Studies of Ligand-Dependent Conformational Dynamics.

Chem Biol 2015 Nov 5;22(11):1431-1436. Epub 2015 Nov 5.

Laboratory of Chemical Biology and Signal Transduction, The Rockefeller University, 1230 York Avenue, New York, NY 10065, USA; Department of Neurobiology, Care Sciences and Society, Division for Neurogeriatrics, Center for Alzheimer Research, Karolinska Institutet, 141 57 Huddinge, Sweden. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2015.09.014DOI Listing
November 2015

Neuromedin U inhibits food intake partly by inhibiting gastric emptying.

Peptides 2015 Jul 18;69:56-65. Epub 2015 Apr 18.

Gubra ApS, Agern Alle 1, 2970 Hørsholm, Denmark. Electronic address:

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http://dx.doi.org/10.1016/j.peptides.2015.04.010DOI Listing
July 2015

Impaired oxidative capacity due to decreased CPT1b levels as a contributing factor to fat accumulation in obesity.

Am J Physiol Regul Integr Comp Physiol 2015 Jun 8;308(11):R973-82. Epub 2015 Apr 8.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen, Denmark; Section for Metabolic Receptology and Enteroendocrinology, The Novo Nordisk Foundation Center for basic Metabolic Research, University of Copenhagen, Copenhagen, Denmark;

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http://www.physiology.org/doi/10.1152/ajpregu.00219.2014
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http://dx.doi.org/10.1152/ajpregu.00219.2014DOI Listing
June 2015

Investigation of the GPR39 zinc receptor following inhibition of monoaminergic neurotransmission and potentialization of glutamatergic neurotransmission.

Brain Res Bull 2015 Jun 24;115:23-9. Epub 2015 Apr 24.

Department of Neuroscience and Pharmacology University of Copenhagen, Blegdamsvej 3, DK-2200, Copenhagen, Denmark.

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http://dx.doi.org/10.1016/j.brainresbull.2015.04.005DOI Listing
June 2015

Dietary non-esterified oleic Acid decreases the jejunal levels of anorectic N-acylethanolamines.

PLoS One 2014 24;9(6):e100365. Epub 2014 Jun 24.

Department of Drug Design & Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0100365PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4068999PMC
March 2015

GPR39 Zn(2+)-sensing receptor: a new target in antidepressant development?

J Affect Disord 2015 Mar 26;174:89-100. Epub 2014 Nov 26.

Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, PL 30-688 Kraków, Poland; Department of Neurobiology, Institute of Pharmacology, Polish Academy of Sciences, Smętna 12, PL 31-343 Kraków, Poland.

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http://dx.doi.org/10.1016/j.jad.2014.11.033DOI Listing
March 2015

Synthesis and evaluation of novel lipidated neuromedin U analogs with increased stability and effects on food intake.

J Pept Sci 2015 Feb 17;21(2):85-94. Epub 2014 Dec 17.

Gubra ApS, Agern Alle 1, 2970, Hørsholm, Denmark; The Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, Blegdamsvej 3B, 2200, Copenhagen N, Denmark.

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http://dx.doi.org/10.1002/psc.2727DOI Listing
February 2015

GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo.

Mol Metab 2015 Jan 24;4(1):3-14. Epub 2014 Oct 24.

Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, 2200 Copenhagen N, Denmark ; Department of Neuroscience and Pharmacology, University of Copenhagen, DK-2200, Copenhagen, Denmark.

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http://dx.doi.org/10.1016/j.molmet.2014.10.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4314522PMC
January 2015

GPR39 (zinc receptor) knockout mice exhibit depression-like behavior and CREB/BDNF down-regulation in the hippocampus.

Int J Neuropsychopharmacol 2014 Oct 31;18(3). Epub 2014 Oct 31.

Department of Biochemical Toxicology, Jagiellonian University Medical College, Medyczna 9, PL 30-688 Kraków, Poland (Dr. K. Młyniec, Prof. B. Budziszewska); Institute of Pharmacology, Polish Academy of Sciences, Smętna 12, PL 31-343 Kraków, Poland (Profs. B. Budziszewska, G. Nowak); Department of Neuroscience and Pharmacology University of Copenhagen, Blegdamsvej 3, DK-2200, Copenhagen, Denmark (Prof. B. Holst); Faculty of Physics and Applied Computer Science, AGH University of Science and Technology, Kraków, Poland (Dr. B. Ostachowicz); Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, PL 30-688 Kraków, Poland (Prof. G. Nowak).

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http://dx.doi.org/10.1093/ijnp/pyu002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4360246PMC
October 2014

PICK1 deficiency impairs secretory vesicle biogenesis and leads to growth retardation and decreased glucose tolerance.

PLoS Biol 2013 23;11(4):e1001542. Epub 2013 Apr 23.

Laboratory for Molecular Pharmacology, Novo Nordisk Foundation Center for Basic Metabolic Research, The Faculty of Health Sciences, Panum Institute, University of Copenhagen, Copenhagen, Denmark.

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http://dx.doi.org/10.1371/journal.pbio.1001542DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3635866PMC
October 2013

Increased susceptibility to diet-induced obesity in GPRC6A receptor knockout mice.

J Endocrinol 2013 May 15;217(2):151-60. Epub 2013 Apr 15.

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.

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http://dx.doi.org/10.1530/JOE-12-0550DOI Listing
May 2013

PheVI:09 (Phe6.44) as a sliding microswitch in seven-transmembrane (7TM) G protein-coupled receptor activation.

J Biol Chem 2012 Dec 7;287(52):43516-26. Epub 2012 Nov 7.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, the Panum Institute, Copenhagen, Denmark.

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http://www.jbc.org/lookup/doi/10.1074/jbc.M112.395137
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http://dx.doi.org/10.1074/jbc.M112.395137DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3527938PMC
December 2012

L-Arginine improves multiple physiological parameters in mice exposed to diet-induced metabolic disturbances.

Amino Acids 2012 Sep 27;43(3):1265-75. Epub 2011 Dec 27.

Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen, Denmark.

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http://dx.doi.org/10.1007/s00726-011-1199-1DOI Listing
September 2012

Improving membrane binding as a design strategy for amphipathic peptide hormones: 2-helix variants of PYY3-36.

J Pept Sci 2012 Sep 1;18(9):579-87. Epub 2012 Aug 1.

Department of Chemistry, Faculty of Science, University of Copenhagen, Thorvaldsensvej 40, 1871, Frederiksberg C, Denmark.

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http://dx.doi.org/10.1002/psc.2436DOI Listing
September 2012

An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.

J Med Chem 2012 Sep 5;55(17):7437-49. Epub 2012 Sep 5.

Institute of Biochemistry, Universität Leipzig, Brüderstraße 34, 04103 Leipzig, Germany.

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http://dx.doi.org/10.1021/jm300414bDOI Listing
September 2012

β-Cell Specific Overexpression of GPR39 Protects against Streptozotocin-Induced Hyperglycemia.

Int J Endocrinol 2011 17;2011:401258. Epub 2011 Nov 17.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark.

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http://www.hindawi.com/journals/ije/2011/401258/
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http://dx.doi.org/10.1155/2011/401258DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3227460PMC
August 2012

Deficiency of the GPR39 receptor is associated with obesity and altered adipocyte metabolism.

FASEB J 2011 Nov 22;25(11):3803-14. Epub 2011 Jul 22.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark.

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http://dx.doi.org/10.1096/fj.11-184531DOI Listing
November 2011

Studies on the anorectic effect of N-acylphosphatidylethanolamine and phosphatidylethanolamine in mice.

Biochim Biophys Acta 2011 Sep 23;1811(9):508-12. Epub 2011 Jun 23.

Department of Pharmacology & Pharmacotherapy, Faculty of Pharmaceutical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.

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http://dx.doi.org/10.1016/j.bbalip.2011.06.020DOI Listing
September 2011

Characterization of murine melanocortin receptors mediating adipocyte lipolysis and examination of signalling pathways involved.

Mol Cell Endocrinol 2011 Jul 17;341(1-2):9-17. Epub 2011 May 17.

Diabetes Biology and Pharmacology, Novo Nordisk A/S, Novo Nordisk Park, 2760 Maaloev, Denmark.

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http://dx.doi.org/10.1016/j.mce.2011.03.010DOI Listing
July 2011

Unique interaction pattern for a functionally biased ghrelin receptor agonist.

J Biol Chem 2011 Jun 14;286(23):20845-60. Epub 2011 Mar 14.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Blegdamsvej 3b, DK-2200, Copenhagen, Denmark.

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http://dx.doi.org/10.1074/jbc.M110.173237DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3121491PMC
June 2011

Long-acting lipidated analogue of human pancreatic polypeptide is slowly released into circulation.

J Med Chem 2011 Apr 31;54(8):2658-67. Epub 2011 Mar 31.

Institute of Biochemistry, Faculty of Biosciences, Pharmacy and Psychology, Leipzig University, Leipzig, Germany.

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http://dx.doi.org/10.1021/jm101357eDOI Listing
April 2011

Dietary fat decreases intestinal levels of the anorectic lipids through a fat sensor.

FASEB J 2011 Feb 19;25(2):765-74. Epub 2010 Oct 19.

Department of Pharmacology and Pharmacotheraphy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark.

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http://dx.doi.org/10.1096/fj.10-166595DOI Listing
February 2011

Modulation of the constitutive activity of the ghrelin receptor by use of pharmacological tools and mutagenesis.

Methods Enzymol 2010 ;484:53-73

Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen N, Denmark.

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http://dx.doi.org/10.1016/B978-0-12-381298-8.00003-4DOI Listing
February 2011

Risperidone treatment increases CB1 receptor binding in rat brain.

Neuroendocrinology 2010 3;91(2):155-68. Epub 2009 Oct 3.

Laboratory of Neuropsychiatry, Rigshospitalet, Copenhagen, Denmark.

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http://dx.doi.org/10.1159/000245220DOI Listing
June 2010

An enteroendocrine full package solution.

Cell Metab 2010 Jun;11(6):445-7

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, The University of Copenhagen, The Panum Institute, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1016/j.cmet.2010.05.008DOI Listing
June 2010

Stability, liposome interaction, and in vivo pharmacology of ghrelin in liposomal suspensions.

Int J Pharm 2010 May 6;390(1):13-8. Epub 2009 Jun 6.

Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark.

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http://linkinghub.elsevier.com/retrieve/pii/S037851730900372
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http://dx.doi.org/10.1016/j.ijpharm.2009.05.067DOI Listing
May 2010

A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors.

J Biol Chem 2010 Feb 17;285(6):3973-85. Epub 2009 Nov 17.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Blegdamsvej 3, DK2200 Copenhagen, Denmark.

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http://www.jbc.org/lookup/doi/10.1074/jbc.M109.064725
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http://dx.doi.org/10.1074/jbc.M109.064725DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2823539PMC
February 2010

Modifying the conserved C-terminal tyrosine of the peptide hormone PYY3-36 to improve Y2 receptor selectivity.

J Pept Sci 2009 Nov;15(11):753-9

University of Copenhagen, Faculty of Life Sciences, IGM-Bioorganic Chemistry, Thorvaldsensvej 40, 1871 Frederiksberg C, Denmark.

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http://dx.doi.org/10.1002/psc.1170DOI Listing
November 2009

In vivo characterization of high Basal signaling from the ghrelin receptor.

Endocrinology 2009 Nov 9;150(11):4920-30. Epub 2009 Oct 9.

Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1210/en.2008-1638DOI Listing
November 2009

Ligand binding and micro-switches in 7TM receptor structures.

Trends Pharmacol Sci 2009 May 16;30(5):249-59. Epub 2009 Apr 16.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen, DK-2200, Denmark.

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http://dx.doi.org/10.1016/j.tips.2009.02.006DOI Listing
May 2009

Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor.

Mol Pharmacol 2009 Jan 15;75(1):44-59. Epub 2008 Oct 15.

Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1124/mol.108.049189DOI Listing
January 2009

A gut feeling for obesity: 7TM sensors on enteroendocrine cells.

Cell Metab 2008 Dec;8(6):447-9

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, Copenhagen, Denmark.

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http://dx.doi.org/10.1016/j.cmet.2008.11.004DOI Listing
December 2008

A second disulfide bridge from the N-terminal domain to extracellular loop 2 dampens receptor activity in GPR39.

Biochemistry 2008 Sep 12;47(35):9198-207. Epub 2008 Aug 12.

Department of Neuroscience and Pharmacology, Faculty of Health Sciences, University of Copenhagen, Blegdamsvej 3b, DK-2200 Copenhagen N, Denmark.

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http://dx.doi.org/10.1021/bi8005016DOI Listing
September 2008

Molecular mechanism of Zn2+ agonism in the extracellular domain of GPR39.

FEBS Lett 2008 Jul 25;582(17):2583-8. Epub 2008 Jun 25.

University of Copenhagen, Faculty of Health Sciences, Department of Neuroscience and Pharmacology, Laboratory for Molecular Pharmacology, Blegdamsvej 3b, Copenhagen N, Denmark.

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July 2008

Importance of constitutive activity and arrestin-independent mechanisms for intracellular trafficking of the ghrelin receptor.

Mol Endocrinol 2007 Dec 23;21(12):3100-12. Epub 2007 Aug 23.

Institute of Cell Signalling, Queen's Medical Centre, Nottingham NG7 2UH, United Kingdom.

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http://dx.doi.org/10.1210/me.2007-0254DOI Listing
December 2007

Melanocortin 4 receptor mutations in obese Czech children: studies of prevalence, phenotype development, weight reduction response, and functional analysis.

J Clin Endocrinol Metab 2007 Sep 19;92(9):3689-96. Epub 2007 Jun 19.

Department of Pediatrics and Center for Research of Diabetes, Metabolism, and Nutrition, Third Faculty of Medicine, Charles University, 100 34 Prague 10, Czech Republic.

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http://dx.doi.org/10.1210/jc.2007-0352DOI Listing
September 2007

Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act?

Trends Pharmacol Sci 2007 Aug 13;28(8):366-73. Epub 2007 Jul 13.

Laboratory for Molecular Pharmacology, Institute of Neuroscience and Pharmacology, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1016/j.tips.2007.06.008DOI Listing
August 2007

GPR39 splice variants versus antisense gene LYPD1: expression and regulation in gastrointestinal tract, endocrine pancreas, liver, and white adipose tissue.

Mol Endocrinol 2007 Jul 8;21(7):1685-98. Epub 2007 May 8.

Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, University of Copenhagen, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1210/me.2007-0055DOI Listing
July 2007

Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism.

J Biol Chem 2007 May 19;282(21):15799-811. Epub 2007 Mar 19.

Laboratory for Molecular Pharmacology, The Panum Institute, Blegdamsvej 3, University of Copenhagen, 2200 Copenhagen N, Denmark.

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http://www.jbc.org/lookup/doi/10.1074/jbc.M609796200
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May 2007

GPR39 signaling is stimulated by zinc ions but not by obestatin.

Endocrinology 2007 Jan 7;148(1):13-20. Epub 2006 Sep 7.

Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1210/en.2006-0933DOI Listing
January 2007

Ghrelin receptor inverse agonists: identification of an active peptide core and its interaction epitopes on the receptor.

Mol Pharmacol 2006 Sep 23;70(3):936-46. Epub 2006 Jun 23.

Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1124/mol.106.024422DOI Listing
September 2006

Metal ion site engineering indicates a global toggle switch model for seven-transmembrane receptor activation.

J Biol Chem 2006 Jun 27;281(25):17337-46. Epub 2006 Mar 27.

Laboratory for Molecular Pharmacology, Panum Institute, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1074/jbc.M512510200DOI Listing
June 2006

Ago-allosteric modulation and other types of allostery in dimeric 7TM receptors.

J Recept Signal Transduct Res 2006 ;26(1-2):107-28

Laboratory for Molecular Pharmacology, Department of Pharmacology, University of Copenhagen and 7TM Pharma A/S, Hørsholm, Denmark.

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http://dx.doi.org/10.1080/10799890600567570 DOI Listing
May 2006

Molecular mechanism of 7TM receptor activation--a global toggle switch model.

Annu Rev Pharmacol Toxicol 2006 ;46:481-519

Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, and 7TM Pharma A/S, Hørsholm, Denmark.

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http://dx.doi.org/10.1146/annurev.pharmtox.46.120604.141218DOI Listing
April 2006

Ghrelin receptor mutations--too little height and too much hunger.

J Clin Invest 2006 Mar;116(3):637-41

Laboratory for Molecular Pharmacology, Panum Institute, University of Copenhagen, Copenhagen, Denmark.

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http://dx.doi.org/10.1172/JCI27999DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1386123PMC
March 2006

Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.

Mol Endocrinol 2005 Sep 19;19(9):2400-11. Epub 2005 May 19.

Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, Blegdamsvej 3, DK-2200, Copenhagen, Denmark.

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http://dx.doi.org/10.1210/me.2005-0059DOI Listing
September 2005

Common structural basis for constitutive activity of the ghrelin receptor family.

J Biol Chem 2004 Dec 21;279(51):53806-17. Epub 2004 Sep 21.

Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, Blegdamsvej 3, DK-2200, Copenhagen, Denmark.

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http://dx.doi.org/10.1074/jbc.M407676200DOI Listing
December 2004

Constitutive ghrelin receptor activity as a signaling set-point in appetite regulation.

Trends Pharmacol Sci 2004 Mar;25(3):113-7

Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, 7TM Pharma A/S, Denmark.

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March 2004

Distinct in vitro interaction pattern of dopamine receptor subtypes with adaptor proteins involved in post-endocytotic receptor targeting.

FEBS Lett 2004 Jan;556(1-3):276-80

Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, Building 18, 6, Blegdamsvej 3, DK-2200, Copenhagen, Denmark.

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January 2004

High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.

Mol Endocrinol 2003 Nov 7;17(11):2201-10. Epub 2003 Aug 7.

Laboratory for Molecular Pharmacology, Institute of Pharmacology, The Panum Institute, University of Copenhagen, DK-2200 Copenhagen, Denmark.

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http://dx.doi.org/10.1210/me.2003-0069DOI Listing
November 2003

Molecular mechanism of agonism and inverse agonism in the melanocortin receptors: Zn(2+) as a structural and functional probe.

Ann N Y Acad Sci 2003 Jun;994:1-11

Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Denmark.

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June 2003

Metal ion-mediated agonism and agonist enhancement in melanocortin MC1 and MC4 receptors.

J Biol Chem 2002 Dec 18;277(49):47662-70. Epub 2002 Sep 18.

Laboratory for Molecular Pharmacology, Institute of Pharmacology, University of Copenhagen, The Panum Institute, Blegdamsvej 3, Copenhagen DK-2200, Denmark.

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http://dx.doi.org/10.1074/jbc.M202103200DOI Listing
December 2002

NK1 receptor fused to beta-arrestin displays a single-component, high-affinity molecular phenotype.

Mol Pharmacol 2002 Jul;62(1):30-7

Laboratory for Molecular Pharmacology, Department of Pharmacology, The Panum Institute, University of Copenhagen, Denmark.

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July 2002