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Calcium-sensing receptor internalization is β-arrestin-dependent and modulated by allosteric ligands.

Mos I, Jacobsen SE, Foster S, Brauner-Osborne H.

Mol Pharmacol. 2019 Aug 9. pii: mol.119.116772. doi: 10.1124/mol.119.116772. [Epub ahead of print]


Biased agonism of clinically approved μ-opioid receptor agonists and TRV130 is not controlled by binding and signaling kinetics.

Pedersen MF, Wróbel TM, Märcher-Rørsted E, Pedersen DS, Møller TC, Gabriele F, Pedersen H, Matosiuk D, Foster SR, Bouvier M, Bräuner-Osborne H.

Neuropharmacology. 2019 Jul 24:107718. doi: 10.1016/j.neuropharm.2019.107718. [Epub ahead of print]


G protein-coupled receptor pharmacology-The next generation.

Bräuner-Osborne H, Rosenkilde MM, Gether U, Gloriam DE.

Basic Clin Pharmacol Toxicol. 2019 Jul 13. doi: 10.1111/bcpt.13291. [Epub ahead of print] No abstract available.


Enhanced agonist residence time, internalization rate and signalling of the GIP receptor variant [E354Q] facilitate receptor desensitization and long-term impairment of the GIP system.

Gabe MBN, van der Velden WJC, Gadgaard S, Smit FX, Hartmann B, Bräuner-Osborne H, Rosenkilde MM.

Basic Clin Pharmacol Toxicol. 2019 Jul 12. doi: 10.1111/bcpt.13289. [Epub ahead of print]


Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands.

Gaiser BI, Danielsen M, Marcher-Rørsted E, Røpke Jørgensen K, Wróbel TM, Frykman M, Johansson H, Bräuner-Osborne H, Gloriam DE, Mathiesen JM, Sejer Pedersen D.

J Med Chem. 2019 Aug 15. doi: 10.1021/acs.jmedchem.9b00595. [Epub ahead of print]


Pharmacology and function of the orphan GPR139 G protein-coupled receptor.

Vedel L, Nøhr AC, Gloriam DE, Bräuner-Osborne H.

Basic Clin Pharmacol Toxicol. 2019 May 27. doi: 10.1111/bcpt.13263. [Epub ahead of print] Review.


Metabolic and skeletal homeostasis are maintained in full locus GPRC6A knockout mice.

Jørgensen CV, Gasparini SJ, Tu J, Zhou H, Seibel MJ, Bräuner-Osborne H.

Sci Rep. 2019 Apr 12;9(1):5995. doi: 10.1038/s41598-019-41921-8.


Label-free dynamic mass redistribution analysis of endogenous adrenergic receptor signaling in primary preadipocytes and differentiated adipocytes.

Jørgensen CV, Zhou H, Seibel MJ, Bräuner-Osborne H.

J Pharmacol Toxicol Methods. 2019 May - Jun;97:59-66. doi: 10.1016/j.vascn.2019.03.005. Epub 2019 Apr 1.


Identification of a novel scaffold for a small molecule GPR139 receptor agonist.

Nøhr AC, Shehata MA, Palmer D, Pokhrel R, Vallianou M, Foster SR, Gentry PR, Gloriam DE, Bräuner-Osborne H.

Sci Rep. 2019 Mar 7;9(1):3802. doi: 10.1038/s41598-019-40085-9.


Structure-Activity Relationship Studies of the Natural Product Gq/11 Protein Inhibitor YM-254890.

Xiong XF, Zhang H, Boesgaard MW, Underwood CR, Bräuner-Osborne H, Strømgaard K.

ChemMedChem. 2019 Apr 17;14(8):865-870. doi: 10.1002/cmdc.201900018. Epub 2019 Mar 21.


Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity.

Malfacini D, Patt J, Annala S, Harpsøe K, Eryilmaz F, Reher R, Crüsemann M, Hanke W, Zhang H, Tietze D, Gloriam DE, Bräuner-Osborne H, Strømgaard K, König GM, Inoue A, Gomeza J, Kostenis E.

J Biol Chem. 2019 Apr 12;294(15):5747-5758. doi: 10.1074/jbc.RA118.007250. Epub 2019 Feb 11.


Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359.

Zhang H, Nielsen AL, Boesgaard MW, Harpsøe K, Daly NL, Xiong XF, Underwood CR, Haugaard-Kedström LM, Bräuner-Osborne H, Gloriam DE, Strømgaard K.

Eur J Med Chem. 2018 Aug 5;156:847-860. doi: 10.1016/j.ejmech.2018.07.023. Epub 2018 Jul 12.


Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors.

Gabe MBN, Sparre-Ulrich AH, Pedersen MF, Gasbjerg LS, Inoue A, Bräuner-Osborne H, Hartmann B, Rosenkilde MM.

Biochem Pharmacol. 2018 Apr;150:97-107. doi: 10.1016/j.bcp.2018.01.040. Epub 2018 Feb 3.


Investigating Internalization and Intracellular Trafficking of GPCRs: New Techniques and Real-Time Experimental Approaches.

Foster SR, Bräuner-Osborne H.

Handb Exp Pharmacol. 2018;245:41-61. doi: 10.1007/164_2017_57. Review.


Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).

Jørgensen L, Al-Khawaja A, Kickinger S, Vogensen SB, Skovgaard-Petersen J, Rosenthal E, Borkar N, Löffler R, Madsen KK, Bräuner-Osborne H, Schousboe A, Ecker GF, Wellendorph P, Clausen RP.

J Med Chem. 2017 Nov 9;60(21):8834-8846. doi: 10.1021/acs.jmedchem.7b00924. Epub 2017 Oct 19.


Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils.

Christensen HB, Gloriam DE, Pedersen DS, Cowland JB, Borregaard N, Bräuner-Osborne H.

J Pharmacol Toxicol Methods. 2017 Nov;88(Pt 1):72-78. doi: 10.1016/j.vascn.2017.07.003. Epub 2017 Jul 15.


Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method.

Frandsen IO, Boesgaard MW, Fidom K, Hauser AS, Isberg V, Bräuner-Osborne H, Wellendorph P, Gloriam DE.

Sci Rep. 2017 Jul 6;7(1):4829. doi: 10.1038/s41598-017-05058-w.


Identification of AICP as a GluN2C-Selective N-Methyl-d-Aspartate Receptor Superagonist at the GluN1 Glycine Site.

Jessen M, Frederiksen K, Yi F, Clausen RP, Hansen KB, Bräuner-Osborne H, Kilburn P, Damholt A.

Mol Pharmacol. 2017 Aug;92(2):151-161. doi: 10.1124/mol.117.108944. Epub 2017 Jun 6. Erratum in: Mol Pharmacol. 2018 Oct;94(4):1101-1102.


Structure-Activity Relationship Studies of the Cyclic Depsipeptide Natural Product YM-254890, Targeting the Gq Protein.

Zhang H, Xiong XF, Boesgaard MW, Underwood CR, Bräuner-Osborne H, Strømgaard K.

ChemMedChem. 2017 Jun 7;12(11):830-834. doi: 10.1002/cmdc.201700155. Epub 2017 May 16.


The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site.

Nøhr AC, Jespers W, Shehata MA, Floryan L, Isberg V, Andersen KB, Åqvist J, Gutiérrez-de-Terán H, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2017 Apr 25;7(1):1128. doi: 10.1038/s41598-017-01049-z.


Investigating the molecular mechanism of positive and negative allosteric modulators in the calcium-sensing receptor dimer.

Jacobsen SE, Gether U, Bräuner-Osborne H.

Sci Rep. 2017 Apr 18;7:46355. doi: 10.1038/srep46355.


Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of N-(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT2A Receptor Agonist.

Jensen AA, McCorvy JD, Leth-Petersen S, Bundgaard C, Liebscher G, Kenakin TP, Bräuner-Osborne H, Kehler J, Kristensen JL.

J Pharmacol Exp Ther. 2017 Jun;361(3):441-453. doi: 10.1124/jpet.117.239905. Epub 2017 Mar 30.


The GPRC6A receptor displays constitutive internalization and sorting to the slow recycling pathway.

Jacobsen SE, Ammendrup-Johnsen I, Jansen AM, Gether U, Madsen KL, Bräuner-Osborne H.

J Biol Chem. 2017 Apr 28;292(17):6910-6926. doi: 10.1074/jbc.M116.762385. Epub 2017 Mar 9.


Knockin mouse with mutant Gα11 mimics human inherited hypocalcemia and is rescued by pharmacologic inhibitors.

Roszko KL, Bi R, Gorvin CM, Bräuner-Osborne H, Xiong XF, Inoue A, Thakker RV, Strømgaard K, Gardella T, Mannstadt M.

JCI Insight. 2017 Feb 9;2(3):e91079. doi: 10.1172/jci.insight.91079.


Structural insight to mutation effects uncover a common allosteric site in class C GPCRs.

Harpsøe K, Boesgaard MW, Munk C, Bräuner-Osborne H, Gloriam DE.

Bioinformatics. 2017 Apr 15;33(8):1116-1120. doi: 10.1093/bioinformatics/btw784.


Genetic Variations in the Human G Protein-coupled Receptor Class C, Group 6, Member A (GPRC6A) Control Cell Surface Expression and Function.

Jørgensen S, Have CT, Underwood CR, Johansen LD, Wellendorph P, Gjesing AP, Jørgensen CV, Quan S, Rui G, Inoue A, Linneberg A, Grarup N, Jun W, Pedersen O, Hansen T, Bräuner-Osborne H.

J Biol Chem. 2017 Jan 27;292(4):1524-1534. doi: 10.1074/jbc.M116.756577. Epub 2016 Dec 16.


Robust GLP-1 secretion by basic L-amino acids does not require the GPRC6A receptor.

Clemmensen C, Jørgensen CV, Smajilovic S, Bräuner-Osborne H.

Diabetes Obes Metab. 2017 Apr;19(4):599-603. doi: 10.1111/dom.12845. Epub 2017 Jan 19.


The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW.

Nøhr AC, Shehata MA, Hauser AS, Isberg V, Mokrosinski J, Andersen KB, Farooqi IS, Pedersen DS, Gloriam DE, Bräuner-Osborne H.

Neurochem Int. 2017 Jan;102:105-113. doi: 10.1016/j.neuint.2016.11.012. Epub 2016 Dec 1.


Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139.

Shehata MA, Nøhr AC, Lissa D, Bisig C, Isberg V, Andersen KB, Harpsøe K, Björkling F, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2016 Nov 10;6:36681. doi: 10.1038/srep36681.


Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors.

Xiong XF, Zhang H, Underwood CR, Harpsøe K, Gardella TJ, Wöldike MF, Mannstadt M, Gloriam DE, Bräuner-Osborne H, Strømgaard K.

Nat Chem. 2016 Nov;8(11):1035-1041. doi: 10.1038/nchem.2577. Epub 2016 Jul 25.


Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.

Johansson H, Boesgaard MW, Nørskov-Lauritsen L, Larsen I, Kuhne S, Gloriam DE, Bräuner-Osborne H, Sejer Pedersen D.

J Med Chem. 2015 Nov 25;58(22):8938-51. doi: 10.1021/acs.jmedchem.5b01254. Epub 2015 Nov 16.


Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

Harpsøe K, Isberg V, Tehan BG, Weiss D, Arsova A, Marshall FH, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2015 Sep 11;5:13869. doi: 10.1038/srep13869.


Role of post-translational modifications on structure, function and pharmacology of class C G protein-coupled receptors.

Nørskov-Lauritsen L, Bräuner-Osborne H.

Eur J Pharmacol. 2015 Sep 15;763(Pt B):233-40. doi: 10.1016/j.ejphar.2015.05.015. Epub 2015 May 14. Review.


A cAMP Biosensor-Based High-Throughput Screening Assay for Identification of Gs-Coupled GPCR Ligands and Phosphodiesterase Inhibitors.

Vedel L, Bräuner-Osborne H, Mathiesen JM.

J Biomol Screen. 2015 Aug;20(7):849-57. doi: 10.1177/1087057115580019. Epub 2015 Apr 7.


N-glycosylation and disulfide bonding affects GPRC6A receptor expression, function, and dimerization.

Nørskov-Lauritsen L, Jørgensen S, Bräuner-Osborne H.

FEBS Lett. 2015 Feb 27;589(5):588-97. doi: 10.1016/j.febslet.2015.01.019. Epub 2015 Jan 21.


Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists.

Hansen M, Jacobsen SE, Plunkett S, Liebscher GE, McCorvy JD, Bräuner-Osborne H, Kristensen JL.

Bioorg Med Chem. 2015 Jul 15;23(14):3933-7. doi: 10.1016/j.bmc.2014.12.011. Epub 2014 Dec 17.


Functional consequences of glucagon-like peptide-1 receptor cross-talk and trafficking.

Roed SN, Nøhr AC, Wismann P, Iversen H, Bräuner-Osborne H, Knudsen SM, Waldhoer M.

J Biol Chem. 2015 Jan 9;290(2):1233-43. doi: 10.1074/jbc.M114.592436. Epub 2014 Dec 1.


Introduction to special issue in honor of Professor Povl Krogsgaard-Larsen.

Bräuner-Osborne H, Schousboe A.

Neurochem Res. 2014 Oct;39(10):1845-6. No abstract available.


Pharmacological identification of a guanidine-containing β-alanine analogue with low micromolar potency and selectivity for the betaine/GABA transporter 1 (BGT1).

Al-Khawaja A, Petersen JG, Damgaard M, Jensen MH, Vogensen SB, Lie ME, Kragholm B, Bräuner-Osborne H, Clausen RP, Frølund B, Wellendorph P.

Neurochem Res. 2014 Oct;39(10):1988-96. doi: 10.1007/s11064-014-1336-9. Epub 2014 May 23.


Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139.

Isberg V, Andersen KB, Bisig C, Dietz GP, Bräuner-Osborne H, Gloriam DE.

J Chem Inf Model. 2014 Jun 23;54(6):1553-7. doi: 10.1021/ci500197a. Epub 2014 May 30.


G protein-coupled receptor signaling analysis using homogenous time-resolved Förster resonance energy transfer (HTRF®) technology.

Nørskov-Lauritsen L, Thomsen AR, Bräuner-Osborne H.

Int J Mol Sci. 2014 Feb 13;15(2):2554-72. doi: 10.3390/ijms15022554.


mGluR5: exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery.

Mølck C, Harpsøe K, Gloriam DE, Mathiesen JM, Nielsen SM, Bräuner-Osborne H.

Neurochem Res. 2014 Oct;39(10):1862-75. doi: 10.1007/s11064-014-1248-8. Epub 2014 Feb 4.


Synthesis and structure-activity relationships of N-benzyl phenethylamines as 5-HT2A/2C agonists.

Hansen M, Phonekeo K, Paine JS, Leth-Petersen S, Begtrup M, Bräuner-Osborne H, Kristensen JL.

ACS Chem Neurosci. 2014 Mar 19;5(3):243-9. doi: 10.1021/cn400216u. Epub 2014 Jan 15.


Real-time trafficking and signaling of the glucagon-like peptide-1 receptor.

Roed SN, Wismann P, Underwood CR, Kulahin N, Iversen H, Cappelen KA, Schäffer L, Lehtonen J, Hecksher-Soerensen J, Secher A, Mathiesen JM, Bräuner-Osborne H, Whistler JL, Knudsen SM, Waldhoer M.

Mol Cell Endocrinol. 2014 Feb 15;382(2):938-49. doi: 10.1016/j.mce.2013.11.010. Epub 2013 Nov 22.


Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site.

Kvist T, Steffensen TB, Greenwood JR, Mehrzad Tabrizi F, Hansen KB, Gajhede M, Pickering DS, Traynelis SF, Kastrup JS, Bräuner-Osborne H.

J Biol Chem. 2013 Nov 15;288(46):33124-35. doi: 10.1074/jbc.M113.480210. Epub 2013 Sep 26.


The GPCR, class C, group 6, subtype A (GPRC6A) receptor: from cloning to physiological function.

Clemmensen C, Smajilovic S, Wellendorph P, Bräuner-Osborne H.

Br J Pharmacol. 2014 Mar;171(5):1129-41. doi: 10.1111/bph.12365. Review.


Delineation of the GPRC6A receptor signaling pathways using a mammalian cell line stably expressing the receptor.

Jacobsen SE, Nørskov-Lauritsen L, Thomsen AR, Smajilovic S, Wellendorph P, Larsson NH, Lehmann A, Bhatia VK, Bräuner-Osborne H.

J Pharmacol Exp Ther. 2013 Nov;347(2):298-309. doi: 10.1124/jpet.113.206276. Epub 2013 Sep 5.


GABA(B)-agonistic activity of certain baclofen homologues.

Attia MI, Herdeis C, Bräuner-Osborne H.

Molecules. 2013 Aug 22;18(9):10266-84. doi: 10.3390/molecules180910266.


Structure-based discovery of antagonists for GluN3-containing N-methyl-D-aspartate receptors.

Kvist T, Greenwood JR, Hansen KB, Traynelis SF, Bräuner-Osborne H.

Neuropharmacology. 2013 Dec;75:324-36. doi: 10.1016/j.neuropharm.2013.08.003. Epub 2013 Aug 22.


Oral L-arginine stimulates GLP-1 secretion to improve glucose tolerance in male mice.

Clemmensen C, Smajilovic S, Smith EP, Woods SC, Bräuner-Osborne H, Seeley RJ, D'Alessio DA, Ryan KK.

Endocrinology. 2013 Nov;154(11):3978-83. doi: 10.1210/en.2013-1529. Epub 2013 Aug 19.

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