Hans Bräuner

Characterization of the real-time internalization of nine GPCRs reveals distinct dependence on arrestins and G proteins

Møller, T. C., Moo, Ee Von, Inoue, A., Pedersen, M. F. & Bräuner, Hans, 2024, In: Biochimica et Biophysica Acta - Molecular Cell Research. 1871, 1, 12 p., 119584.

Research output: Contribution to journal › Journal article › Research › peer-review

Structure-Activity Relationship Studies and Optimization of 4-Hydroxypyridones as GPR84 Agonists

Ieremias, L., Kaspersen, M. H., Manandhar, Asmita, Schultz-Knudsen, Katrine, Vrettou, C. I., Pokhrel, R., Heidtmann, C. V., Jenkins, L., Kanellou, C., Marsango, S., Li, Y., Bräuner, Hans, Ulven, Elisabeth Rexen, Milligan, G. & Ulven, Trond, 2024, In: Journal of Medicinal Chemistry. 67, 5, p. 3542-3570

Research output: Contribution to journal › Journal article › Research › peer-review

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors

Alexander, S. P. H., Christopoulos, A., Davenport, A. P., Kelly, E., Mathie, A. A., Peters, J. A., Veale, E. L., Armstrong, J. F., Faccenda, E., Harding, S. D., Davies, J. A., Abbracchio, M. P., Abraham, G., Agoulnik, A., Alexander, W., Al-Hosaini, K., Bäck, M., Baker, J. G., Barnes, N. M., Bathgate, R. & 146 others, Beaulieu, J., Beck-Sickinger, A. G., Behrens, M., Bernstein, K. E., Bettler, B., Birdsall, N. J. M., Blaho, V., Boulay, F., Bousquet, C., Bräuner, Hans, Burnstock, G., Caló, G., Castaño, J. P., Catt, K. J., Ceruti, S., Chazot, P., Chiang, N., Chini, B., Chun, J., Cianciulli, A., Civelli, O., Clapp, L. H., Couture, R., Cox, H. M., Csaba, Z., Dahlgren, C., Dent, G., Douglas, S. D., Dournaud, P., Eguchi, S., Escher, E., Filardo, E. J., Fong, T., Fumagalli, M., Gainetdinov, R. R., Garelja, M. L., de Gasparo, M., Gerard, C., Gershengorn, M., Gobeil, F., Goodfriend, T. L., Goudet, C., Grätz, L., Gregory, K. J., Gundlach, A. L., Hamann, J., Hanson, J., Hauger, R. L., Hay, D. L., Heinemann, A., Herr, D., Hollenberg, M. D., Holliday, N. D., Horiuchi, M., Hoyer, D., Hunyady, L., Husain, A., IJzerman, A. P., Inagami, T., Jacobson, K. A., Jensen, R. T., Jockers, R., Jonnalagadda, D., Karnik, S., Kaupmann, K., Kemp, J., Kennedy, C., Kihara, Y., Kitazawa, T., Kozielewicz, P., Kreienkamp, H., Kukkonen, J. P., Langenhan, T., Larhammar, D., Leach, K., Lecca, D., Lee, J. D., Leeman, S. E., Leprince, J., Li, X. X., Lolait, S. J., Lupp, A., Macrae, R., Maguire, J., Malfacini, D., Mazella, J., McArdle, C. A., Melmed, S., Michel, M. C., Miller, L. J., Mitolo, V., Mouillac, B., Müller, C. E., Murphy, P. M., Nahon, J., Ngo, T., Norel, X., Nyimanu, D., O'Carroll, A., Offermanns, S., Panaro, M. A., Parmentier, M., Pertwee, R. G., Pin, J., Prossnitz, E. R., Quinn, M., Ramachandran, R., Ray, M., Reinscheid, R. K., Rondard, P., Rovati, G. E., Ruzza, C., Sanger, G. J., Schöneberg, T., Schulte, G., Schulz, S., Segaloff, D. L., Serhan, C. N., Singh, K. D., Smith, C. M., Stoddart, L. A., Sugimoto, Y., Summers, R., Tan, V. P., Thal, D., Thomas, W. W., Timmermans, P. B. M. W. M., Tirupula, K., Toll, L., Tulipano, G., Unal, H., Unger, T., Valant, C., Vanderheyden, P., Vaudry, D., Vaudry, H., Vilardaga, J., Walker, C. S., Wang, J. M., Ward, D. T., Wester, H., Willars, G. B., Williams, T. L., Woodruff, T. M., Yao, C. & Ye, R. D., Oct 2023, In: British Journal of Pharmacology. 180 Suppl 2, p. S23-S144

Research output: Contribution to journal › Journal article › Research › peer-review

Endocytic proteins mediating GPR15 receptor internalization provide insight into the underlying mechanisms

Deng, Y., Moo, Ee Von, Inoue, A. & Bräuner, Hans, 2023, In: FEBS Letters. 597, 11, p. 1528-1540

Research output: Contribution to journal › Journal article › Research › peer-review

Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139

Pallareti, L., Rath, T. F., Trapkov, Boris, Tsonkov, T., Nielsen, A. T., Harpsøe, Kasper, Gentry, P. R., Bräuner, Hans, Gloriam, David E. & Foster, S. R., 2023, In: European Journal of Pharmacology. 943, 175553.

Research output: Contribution to journal › Journal article › Research › peer-review

Structure–activity relationship of GPR15L peptide analogues and investigation of their interaction with the GPR15 receptor

Deng, Y., Perez Almeria, C. V., van Gijzel, L., Schaller, Kay, Vedel, L., Gloriam, David E., Ulven, Trond & Bräuner, Hans, 2023, In: Basic and Clinical Pharmacology and Toxicology. 132, 6, p. 459-471

Research output: Contribution to journal › Journal article › Research › peer-review

Delineation of the GPR15 receptor-mediated Gα protein signalling profile in recombinant mammalian cells

Deng, Y., Moo, Ee Von, Almería, C. V. P., Gentry, P. R., Vedel, L., Mathiesen, Jesper M. & Bräuner, Hans, 2022, In: Basic and Clinical Pharmacology and Toxicology. 131, 2, p. 104-113

Research output: Contribution to journal › Journal article › Research › peer-review

Development of a medium throughput whole-cell microtiter plate Thr286 autophosphorylation assay for CaMKIIα using ELISA

Palmelund, L. B., van Woerden, G. M., Bräuner, Hans & Wellendorph, Petrine, 2022, In: Journal of Pharmacological and Toxicological Methods. 118, 8 p., 107226.

Research output: Contribution to journal › Journal article › Research › peer-review

Ligand-directed bias of G protein signaling at the dopamine D₂ receptor

Moo, Ee Von, Harpsøe, Kasper, Hauser, Alexander Sebastian, Masuho, I., Bräuner, Hans, Gloriam, David E. & Martemyanov, K. A., 2022, In: Cell Chemical Biology. 29, 2, p. 226-238

Research output: Contribution to journal › Journal article › Research › peer-review

Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139

Zhou, Y., Daver, H., Trapkov, B., Wu, L., Wu, M., Harpsøe, Kasper, Gentry, P. R., Liu, K., Larionova, M., Liu, J., Chen, N., Bräuner, Hans, Gloriam, David E., Hua, T. & Liu, Z. J., 2022, In: Cell Research. 32, 2, p. 210-213

Research output: Contribution to journal › Letter › Research › peer-review

Somatostatin venom analogs evolved by fish-hunting cone snails: From prey capture behavior to identifying drug leads

Ramiro, Iris Bea L. , Bjørn-Yoshimoto, Walden, Imperial, J. S., Gajewiak, J., Salcedo, P. F., Watkins, M., Taylor, D., Resager, W., Ueberheide, B., Bräuner, Hans, Whitby, F. G., Hill, C. P., Martin, L. F., Patwardhan, A., Concepcion, G. P., Olivera, B. M. & Safavi-Hemami, H., 2022, In: Science Advances. 8, 12, 16 p., eabk1410.

Research output: Contribution to journal › Journal article › Research › peer-review

Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu_5a receptor internalization

van Senten, Jeffrey Roy, Møller, T. C., Moo, Ee Von, Seiersen, S. D. & Bräuner, Hans, 2022, In: Journal of Biological Chemistry. 298, 10, 16 p., 102466.

Research output: Contribution to journal › Journal article › Research › peer-review

Positive allosteric modulators of metabotropic glutamate receptor 5 as tool compounds to study signaling bias

Arsova, A., Møller, T. C., Hellyer, S. D., Vedel, L., Foster, S. R., Hansen, J. L., Bräuner, Hans & Gregory, K. J., 1 May 2021, In: Molecular Pharmacology. 99, 5, p. 328-241

Research output: Contribution to journal › Journal article › Research › peer-review

Arrestin-Dependent and -Independent Internalization of G Protein–Coupled Receptors: Methods, Mechanisms, and Implications on Cell Signaling

Moo, Ee Von, van Senten, Jeffrey Roy, Bräuner, Hans & Møller, T. C., 2021, In: Molecular Pharmacology. 99, 4, p. 242-255

Research output: Contribution to journal › Journal article › Research › peer-review

Asymmetric activation of the calcium-sensing receptor homodimer

Gao, Y., Robertson, M. J., Rahman, Sabrina Nalini, Seven, A. B., Zhang, C., Meyerowitz, J. G., Panova, O., Hannan, F. M., Thakker, R. V., Bräuner, Hans, Mathiesen, Jesper M. & Skiniotis, G., 2021, In: Nature. 595, p. 455-459

Research output: Contribution to journal › Journal article › Research › peer-review

GLP-1 Val8: A Biased GLP-1R Agonist with Altered Binding Kinetics and Impaired Release of Pancreatic Hormones in Rats

van der Velden, W. J. C., Smit, F. X., Christiansen, Charlotte Bayer, Møller, T. C., Hjortø, Gertrud Malene, Larsen, Olav, Schiellerup, S. P., Bräuner, Hans, Holst, Jens Juul, Hartmann, Bolette, Frimurer, Thomas Michael & Rosenkilde, Mette, 2021, In: ACS Pharmacology & Translational Science. 4, 1, p. 296-313 18 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Mutational Landscape of the Proglucagon-Derived Peptides

Lindquist, Peter, Madsen, Jakob Sture, Bräuner, Hans, Rosenkilde, Mette & Hauser, Alexander Sebastian, 2021, In: Frontiers in Endocrinology. 12, 14 p., 698511.

Research output: Contribution to journal › Journal article › Research › peer-review

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors

Alexander, S. P., Christopoulos, A., Davenport, A. P., Kelly, E., Mathie, A., Peters, J. A., Veale, E. L., Armstrong, J. F., Faccenda, E., Harding, S. D., Pawson, A. J., Southan, C., Davies, J. A., Abbracchio, M. P., Alexander, W., Al-Hosaini, K., Bäck, M., Barnes, N. M., Bathgate, R., Beaulieu, J-M. & 135 others, Bernstein, K. E., Bettler, B., Birdsall, N. J. M., Blaho, V., Boulay, F., Bousquet, C., Bräuner, Hans, Burnstock, G., Caló, G., Castaño, J. P., Catt, K. J., Ceruti, S., Chazot, P., Chiang, N., Chini, B., Chun, J., Cianciulli, A., Civelli, O., Clapp, L. H., Couture, R., Csaba, Z., Dahlgren, C., Dent, G., Singh, K. D., Douglas, S. D., Dournaud, P., Eguchi, S., Escher, E., Filardo, E. J., Fong, T., Fumagalli, M., Gainetdinov, R. R., Gasparo, M. D., Gerard, C., Gershengorn, M., Gobeil, F., Goodfriend, T. L., Goudet, C., Gregory, K. J., Gundlach, A. L., Hamann, J., Hanson, J., Hauger, R. L., Hay, D. L., Heinemann, A., Hollenberg, M. D., Holliday, N. D., Horiuchi, M., Hoyer, D., Hunyady, L., Husain, A., IJzerman, A. P., Inagami, T., Jacobson, K. A., Jensen, R. T., Jockers, R., Jonnalagadda, D., Karnik, S., Kaupmann, K., Kemp, J., Kennedy, C., Kihara, Y., Kitazawa, T., Kozielewicz, P., Kreienkamp, H., Kukkonen, J. P., Langenhan, T., Leach, K., Lecca, D., Lee, J. D., Leeman, S. E., Leprince, J., Li, X. X., Williams, T. L., Lolait, S. J., Lupp, A., Macrae, R., Maguire, J., Mazella, J., McArdle, C. A., Melmed, S., Michel, M. C., Miller, L. J., Mitolo, V., Mouillac, B., Müller, C. E., Murphy, P., Nahon, J., Ngo, T., Norel, X., Nyimanu, D., O'Carroll, A., Offermanns, S., Panaro, M. A., Parmentier, M., Pertwee, R. G., Pin, J., Prossnitz, E. R., Quinn, M., Ramachandran, R., Ray, M., Reinscheid, R. K., Rondard, P., Rovati, G. E., Ruzza, C., Sanger, G. J., Schöneberg, T., Schulte, G., Schulz, S., Segaloff, D. L., Serhan, C. N., Stoddart, L. A., Sugimoto, Y., Summers, R., Tan, V. P., Thal, D., Thomas, W. W., Timmermans, P. B. M. W. M., Tirupula, K., Tulipano, G., Unal, H., Unger, T., Valant, C., Vanderheyden, P., Vaudry, D., Vaudry, H., Vilardaga, J., Walker, C. S., Wang, J. M., Ward, D. T., Wester, H., Willars, G. B., Woodruff, T. M., Yao, C. & Ye, R. D., 2021, In: British Journal of Pharmacology. 178 , S1, p. S27-S156

Research output: Contribution to journal › Journal article › Research › peer-review

The Calcium-Sensing Receptor Is Essential for Calcium and Bicarbonate Sensitivity in Human Spermatozoa

Boisen, I. M., Rehfeld, Anders Aagaard, Mos, I., Poulsen, N. N., Nielsen, J. E., Schwarz, Peter, Rejnmark, L., Dissing, Steen, Bach-Mortensen, P., Juul, Anders, Bräuner, Hans, Lanske, B. & Blomberg Jensen, M., 2021, In: The Journal of clinical endocrinology and metabolism. 106, 4, p. e1775-e1792

Research output: Contribution to journal › Journal article › Research › peer-review

International Union of Basic and Clinical Pharmacology. CVIII. Calcium-Sensing Receptor Nomenclature, Pharmacology, and Function

Leach, K., Hannan, F. M., Josephs, T. M., Keller, A. N., Møller, T. C., Ward, D. T., Kallay, E., Mason, R. S., Thakker, R. V., Riccardi, D., Conigrave, A. D. & Bräuner, Hans, Jul 2020, In: Pharmacological Reviews. 72, 3, p. 558-604 47 p.

Research output: Contribution to journal › Review › Research › peer-review

Heterozygous Mutation (Q459R) in the Calcium-Sensing Receptor Gene Causes Familial Hypocalciuric Hypercalcemia 1 (FHH1)

Boisen, I. M., Mos, I., Lerche-Black, E. M., Juul, Anders, Bräuner, Hans & Blomberg Jensen, M., 1 Apr 2020, In: The Journal of clinical endocrinology and metabolism. 105, 4, p. e1322-e1330

Research output: Contribution to journal › Journal article › Research › peer-review

Novel approaches leading towards peptide GPCR de-orphanisation

Hauser, Alexander Sebastian, Gloriam, David E., Bräuner, Hans & Foster, S. R., 1 Mar 2020, In: British Journal of Pharmacology. 177, 5, p. 961-968 8 p.

Research output: Contribution to journal › Review › Research › peer-review

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

Pedersen, M. F., Wrobel, T. M., Marcher, Emil, Pedersen, D. S., Møller, T. C., Gabriele, F., Pedersen, H., Matosiuk, D., Foster, S. R., Bouvier, M. & Bräuner, Hans, 2020, In: Neuropharmacology. 166, 13 p., 107718.

Research output: Contribution to journal › Journal article › Research › peer-review

Delineation of molecular determinants for FR900359 inhibition of G_q/11 unlocks inhibition of Gα_s

Boesgaard, M. W., Harpsøe, Kasper, Malmberg, M., Underwood, C. R., Inoue, A., Mathiesen, Jesper M., König, G. M., Kostenis, E., Gloriam, David E. & Bräuner, Hans, 2020, In: Journal of Biological Chemistry. 295, 40, p. 13850-13861

Research output: Contribution to journal › Journal article › Research › peer-review

Detailed in vitro pharmacological characterization of clinically tested negative allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)

Arsova, A., Møller, T. C., Vedel, L., Hansen, J. L., Foster, S. R., Gregory, K. J. & Bräuner, Hans, 2020, In: Molecular Pharmacology. 98, 1, p. 49-60

Research output: Contribution to journal › Journal article › Research › peer-review

Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells

Møller, T. C., Pedersen, M. F., van Senten, Jeffrey Roy, Seiersen, S. D., Mathiesen, Jesper M., Bouvier, M. & Bräuner, Hans, 2020, In: Scientific Reports. 10, 1, 13 p., 17395.

Research output: Contribution to journal › Journal article › Research › peer-review

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, M. B. N., van der Velden, W. J. C., Gadgaard, S., Smit, F. X., Hartmann, Bolette, Bräuner, Hans & Rosenkilde, Mette, 2020, In: Basic & Clinical Pharmacology & Toxicology. 126, p. 122-132

Research output: Contribution to journal › Journal article › Research › peer-review

G protein-coupled receptor pharmacology-The next generation

Bräuner, Hans, Rosenkilde, Mette, Gether, Ulrik & Gloriam, David E., 2020, In: Basic & Clinical Pharmacology & Toxicology. 126, Supplement 6, p. 3-4 2 p.

Research output: Contribution to journal › Editorial › Research

Pharmacology and physiological function of the orphan GPRC6A receptor

Jorgensen, C. V. & Bräuner, Hans, 2020, In: Basic & Clinical Pharmacology & Toxicology. 126, p. 77-87 11 p.

Research output: Contribution to journal › Review › Research › peer-review

The selective 5-HT2A receptor agonist 25CN-NBOH: structure-activity relationship, in vivo pharmacology, and in vitro and ex vivo binding characteristics of [3H]25CN-NBOH

Jensen, Anders A., Halberstadt, A. L., Marcher, Emil, Odland, Anna Ulstein, Chatha, M., Speth, N., Liebscher, G., Hansen, M., Bräuner, Hans, Palner, M., Andreasen T., Jesper & Kristensen, Jesper Langgaard, 2020, In: Biochemical Pharmacology. 177, 16 p., 113979.

Research output: Contribution to journal › Journal article › Research › peer-review

Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors

Foster, S. R., Hauser, Alexander Sebastian, Vedel, L., Strachan, R. T., Huang, X., Gavin, A. C., Shah, S. D., Nayak, A. P., Haugaard-Kedström, L. M., Penn, R. B., Roth, B. L., Bräuner, Hans & Gloriam, David E., 31 Oct 2019, In: Cell. 179, 4, p. 895-908

Research output: Contribution to journal › Journal article › Research › peer-review

Calcium-Sensing Receptor Internalization Is β-Arrestin-Dependent and Modulated by Allosteric Ligands

Mos, I., Jacobsen, S. E., Foster, S. R. & Bräuner, Hans, Oct 2019, In: Molecular Pharmacology. 96, 4, p. 463-474 12 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Gaiser, B. I., Danielsen, M., Marcher, Emil, Røpke Jørgensen, K., Wróbel, T. M., Frykman, M., Johansson, H., Bräuner, Hans, Gloriam, David E., Mathiesen, Jesper M. & Sejer Pedersen, D., 12 Sep 2019, In: Journal of Medicinal Chemistry. 62, 17, p. 7806-7839 34 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Vedel, L., Nøhr, A. C., Gloriam, David E. & Bräuner, Hans, 27 May 2019, In: Basic & Clinical Pharmacology & Toxicology. 126, p. 35-46

Research output: Contribution to journal › Review › Research › peer-review

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

Jørgensen, C. V., Gasparini, S. J., Tu, J., Zhou, H., Seibel, M. J. & Bräuner, Hans, 12 Apr 2019, In: Scientific Reports. 9, 1, 8 p., 5995.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Malfacini, D., Patt, J., Annala, S., Harpsøe, Kasper, Eryilmaz, F., Reher, R., Crüsemann, M., Hanke, W., Zhang, H., Tietze, D., Gloriam, David E., Bräuner, Hans, Strømgaard, Kristian, König, G. M., Inoue, A., Gomeza, J. & Kostenis, E., 12 Apr 2019, In: The Journal of Biological Chemistry. 294, 15, p. 5747-5758

Research output: Contribution to journal › Journal article › Research › peer-review

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

Jørgensen, C. V., Zhou, H., Seibel, M. J. & Bräuner, Hans, 1 Apr 2019, In: Journal of Pharmacological and Toxicological Methods. 97, p. 59-66 8 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Structure–Activity Relationship Studies of the Natural Product G _q/11 Protein Inhibitor YM-254890

Xiong, X. F., Zhang, H., Boesgaard, M. W., Underwood, C. R., Bräuner, Hans & Strømgaard, Kristian, Apr 2019, In: ChemMedChem. 14, 8, p. 865-870

Research output: Contribution to journal › Journal article › Research › peer-review

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

Nøhr, A. C., Shehata, M. A., Palmer, D., Pokhrel, R., Vallianou, M., Foster, S. R., Gentry, P. R., Gloriam, David E. & Bräuner, Hans, 7 Mar 2019, In: Scientific Reports. 9, 1, 10 p., 3802.

Research output: Contribution to journal › Journal article › Research › peer-review

Human GIP(3-30)NH 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, M. B. N., Sparre-Ulrich, A. H., Pedersen, M. F., Gasbjerg, Lærke Smidt, Inoue, A., Bräuner, Hans, Hartmann, Bolette & Rosenkilde, M. M., 31 Jan 2018, In: Biochemical Pharmacology. 150, p. 97-107 11 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Zhang, H., Nielsen, A. L., Boesgaard, M. W., Harpsøe, Kasper, Daly, N. L., Xiong, X., Underwood, C. R., Haugaard-kedström, L. M., Bräuner, Hans, Gloriam, David E. & Strømgaard, Kristian, 2018, In: European Journal of Medicinal Chemistry. 156, p. 847-860

Research output: Contribution to journal › Journal article › Research › peer-review

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview

CGTP Collaborators, C. C., Dec 2017, In: British Journal of Pharmacology. 174, p. S1-S16

Research output: Contribution to journal › Journal article › Research › peer-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, S. B., Skovgaard-Petersen, J., Rosenthal, E., Borkar, N., Löffler, R., Madsen, K. K., Bräuner, Hans, Schousboe, Arne, Ecker, G. F., Wellendorph, Petrine & Clausen, Rasmus Prætorius, 9 Oct 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 8834-8846

Research output: Contribution to journal › Journal article › Research › peer-review

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, Rasmus Prætorius, Hansen, K. B., Bräuner, Hans, Kilburn, J. P. & Damholt, A., Aug 2017, In: Molecular Pharmacology. 92, 2, p. 151-161 11 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Christensen, H. B., Gloriam, David E., Pedersen, D. S., Cowland, J. B., Borregaard, N. & Bräuner, Hans, 15 Jul 2017, In: Journal of Pharmacological and Toxicological Methods. 88, Pt 1, p. 72-78 7 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Frandsen, I. O., Boesgaard, M. W., Fidom, K., Hauser, Alexander Sebastian, Isberg, V., Bräuner, Hans, Wellendorph, Petrine & Gloriam, David E., 6 Jul 2017, In: Scientific Reports. 7, 1, 10 p., 4829.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Zhang, H., Xiong, X., Boesgaard, M. W., Underwood, C. R., Bräuner, Hans & Strømgaard, Kristian, 7 Jun 2017, In: ChemMedChem. 12, 11, p. 830-834 5 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Shehata, M. A., Jensen, A. C. N., Jespers, W., Floryan, L., Isberg, V., Andersen, K. B., Åqvist, J., Gutiérrez-de-Terán, H., Bräuner, Hans & Gloriam, David E., 25 Apr 2017, In: Scientific Reports. 7, 9 p., 1128.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Roszko, K. L., Bi, R., Gorvin, C. M., Bräuner, Hans, Xiong, X., Inoue, A., Thakker, R. V., Strømgaard, Kristian, Gardella, T. & Mannstadt, M., 9 Feb 2017, In: JCI insight. 2, 3, 15 p., e91079.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Jensen, A. C. N., Shehata, M. A., Hauser, Alexander Sebastian, Isberg, V., Mokrosinski, J., Farooqi, I. S., Pedersen, D. S., Gloriam, David E. & Bräuner, Hans, 1 Jan 2017, In: Neurochemistry International. 102, p. 105-113

Research output: Contribution to journal › Journal article › Research › peer-review

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, Anders A., McCorvy, J. D., Petersen, S. L., Bundgaard, C., Liebscher, G., Kenakin, T. P., Bräuner, Hans, Kehler, J. & Kristensen, Jesper Langgaard, 2017, In: Journal of Pharmacology and Experimental Therapeutics. 361, 3, p. 441-453

Research output: Contribution to journal › Journal article › Research › peer-review

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

Jorgensen, S., Have, C. T., Underwood, C. R., Johansen, L. D., Wellendorph, Petrine, Gjesing, A. P., Jorgensen, C. V., Quan, S., Rui, G., Inoue, A., Linneberg, Allan René, Grarup, Niels, Jun, W., Pedersen, Oluf Borbye, Hansen, Torben & Bräuner, Hans, 2017, In: The Journal of Biological Chemistry. 292, 4, p. 1524-1534 11 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Jacobsen, S. E., Gether, Ulrik & Bräuner, Hans, 2017, In: Scientific Reports. 7, 14 p., 46355.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Clemmensen, Christoffer, Jørgensen, C. V., Smajilovic, S. & Bräuner, Hans, 2017, In: Diabetes, Obesity and Metabolism. 19, 4, p. 599-603

Research output: Contribution to journal › Journal article › Research › peer-review

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

Harpsøe, Kasper, Boesgaard, M. W., Munk, C., Bräuner, Hans & Gloriam, David E., 2017, In: Bioinformatics (Oxford, England). 33, 8, p. 1116-1120 5 p., btw784.

Research output: Contribution to journal › Journal article › Research › peer-review

The GPRC6A Receptor displays Constitutive Internalization and Sorting to the Slow Recycling Pathway

Jacobsen, S. E., Ammendrup-Johnsen, I., Jansen, A. M., Gether, Ulrik, Madsen, Kenneth Lindegaard & Bräuner, Hans, 2017, In: The Journal of Biological Chemistry. 292, 17, p. 6910-6926

Research output: Contribution to journal › Journal article › Research › peer-review

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

Shehata, M. A., Jensen, A. C. N., Lissa, D., Bisig, C., Isberg, V., Andersen, K. B., Harpsøe, Kasper, Björkling, Fredrik, Bräuner, Hans & Gloriam, David E., 10 Nov 2016, In: Scientific Reports. 6, p. 1-13 13 p., 36681.

Research output: Contribution to journal › Journal article › Research › peer-review

Radiosynthesis and characterisation of a potent and selective GPR139 agonist radioligand

Kuhne, S., Nøhr, A. C., Marek, A., Elbert, T., Klein, A. B., Bräuner, Hans, Wellendorph, Petrine & Pedersen, D. S., 2016, In: RSC Advances. 6, 2, p. 947-952 6 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Xiong, X., Zhang, H., Underwood, C. R., Harpsøe, Kasper, Gardella, T. J., Wöldike, M. F., Mannstadt, M., Gloriam, David E., Bräuner, Hans & Strømgaard, Kristian, 2016, In: Nature Chemistry. 8, 11, p. 1035-1041 7 p.

Research output: Contribution to journal › Journal article › Research › peer-review

The Concise Guide to PHARMACOLOGY 2015/16: Overview

CGTP Collaborators, C. C., 1 Dec 2015, In: British Journal of Pharmacology. 172, 24, p. 5729-5743 15 p.

Research output: Contribution to journal › Review › Research › peer-review

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

Johansson, H., Boesgaard, M. W., Nørskov-Lauritsen, L., Larsen, I., Kuhne, S., Gloriam, David E., Bräuner, Hans & Sejer Pedersen, D., 25 Nov 2015, In: Journal of Medicinal Chemistry. 58, 22, p. 8938-51 14 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Harpsøe, Kasper, Isberg, V., Tehan, B. G., Weiss, D., Arsova, A., Marshall, F. H., Bräuner, Hans & Gloriam, David E., 11 Sep 2015, In: Scientific Reports. 5, p. 1-11 11 p., 13869.

Research output: Contribution to journal › Journal article › Research › peer-review

L-amino acid sensing G protein-coupled receptors and their role in food intake sensing

Bräuner, Hans, Mar 2015, In: Chemical Senses. 40, 3, p. 231-231 1 p.

Research output: Contribution to journal › Conference abstract in journal › Research › peer-review

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

Nørskov-Lauritsen, L., Jørgensen, S. & Bräuner, Hans, 21 Jan 2015, In: FEBS Letters. 589, p. 588–597 10 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Functional Consequences of Glucagon-like Peptide-1 Receptor Cross-talk and Trafficking

Roed, S. N., Nøhr, A. C., Wismann, P., Iversen, H., Bräuner, Hans, Knudsen, S. M. & Waldhoer, M., 9 Jan 2015, In: The Journal of Biological Chemistry. 290, 2, p. 1233-1243 11 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Vedel, L., Bräuner, Hans & Mathiesen, Jesper M., 2015, In: Journal of Biomolecular Screening. 20, p. 849-857 9 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Identification of the first surrogate agonists for the G protein-coupled receptor GPR132

Shehata, M. A., Christensen, H. B., Isberg, V., Pedersen, D. S., Bender, A., Bräuner, Hans & Gloriam, David E., 2015, In: RSC Advances. 5, p. 48551-48557 7 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Nørskov-Lauritsen, L. & Bräuner, Hans, 2015, In: European Journal of Pharmacology. 763, p. 233-240 8 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Hansen, M., Jacobsen, S. E., Plunkett, S., Liebscher, G. E., McCorvy, J. D., Bräuner, Hans & Kristensen, Jesper Langgaard, 2015, In: Bioorganic & Medicinal Chemistry. 23, 14, p. 3933-3937 5 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Bräuner, Hans & Schousboe, Arne, Oct 2014, In: Neurochemical Research. 39, 10, p. 1845-6 2 p.

Research output: Contribution to journal › Journal article › Research

mGluR5: Exploration of Orthosteric and Allosteric Ligand Binding Pockets and Their Applications to Drug Discovery

Mølck, C., Harpsøe, Kasper, Gloriam, David E., Mathiesen, Jesper M., Nielsen, S. M. & Bräuner, Hans, Oct 2014, In: Neurochemical Research. 39, 10, p. 1862-1875 14 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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. M. A., Petersen, J. G., Damgaard, M., Jensen, M. H., Vogensen, S. B., Lie, M. E. K., Kragholm, B., Bräuner, Hans, Clausen, Rasmus Prætorius, Frølund, Bente & Wellendorph, Petrine, 23 May 2014, In: Neurochemical Research. 39, 10, p. 1988-1996 9 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Ísberg, V., Andersen, K. B., Bisig, C., Dietz, G. P., Bräuner, Hans & Gloriam, David E., 14 May 2014, In: Journal of Chemical Information and Modeling. 54, 6, p. 1553-1557 5 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Roed, S. N., Wismann, P., Underwood, C. R., Kulahin, N., Iversen, H., Cappelen, K. A., Schäffer, L., Lehtonen, J., Hecksher-Soerensen, J., Secher, A., Mathiesen, Jesper M., Bräuner, Hans, Whistler, J. L., Knudsen, S. M. & Waldhoer, M., Feb 2014, In: Molecular and Cellular Endocrinology. 382, 2, p. 938-949 12 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Hansen, M., Phonekeo, K., Paine, J. S., Leth-Petersen, S., Begtrup, M., Bräuner, Hans & Kristensen, Jesper Langgaard, 7 Jan 2014, In: A C S Chemical Neuroscience. 5, 3, p. 243-249 8 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Nørskov-Lauritsen, L., Thomsen, A. R. B. & Bräuner, Hans, 2014, In: International Journal of Molecular Sciences (Online). 15, 2, p. 2554-2572

Research output: Contribution to journal › Journal article › Research › peer-review

Promiscuous Seven Transmembrane Receptors Sensing L-α-amino Acids

Smajilovic, S., Wellendorph, Petrine & Bräuner, Hans, 2014, In: Current Pharmaceutical Design. 20, p. 2693-702 10 p.

Research output: Contribution to journal › Journal article › Research › peer-review

The G protein-coupled receptor, class C, group 6, subtype A (GPRC6A) receptor: from cloning to physiological function

Clemmensen, Christoffer, Smajilovic, S., Wellendorph, Petrine & Bräuner, Hans, 2014, In: British Journal of Pharmacology. 171, 5, p. 1129-1141

Research output: Contribution to journal › Journal article › Research › peer-review

Delineation of the GPRC6A Receptor Signaling Pathways Using a Mammalian Cell Line Stably Expressing the Receptor

Jacobsen, S. E., Nørskov-Lauritsen, L., Thomsen, A. R. B., Smajilovic, S., Wellendorph, Petrine, Larsson, N. H. P., Lehmann, A., Bhatia, V. K. & Bräuner, Hans, Nov 2013, In: Journal of Pharmacology and Experimental Therapeutics. 347, 2, p. 298-309 12 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Oral L-Arginine Stimulates GLP-1 Secretion to Improve Glucose Tolerance in Male Mice

Clemmensen, C., Smajilovic, S., Smith, E. P., Woods, S. C., Bräuner, Hans, Seeley, R. J., D'Alessio, D. A. & Ryan, K. K., Nov 2013, In: Endocrinology. 154, 11, p. 3978-83 6 p.

Research output: Contribution to journal › Journal article › Research

The orthosteric GABAA receptor ligand Thio-4-PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors

Hoestgaard-Jensen, K., O'Connor, R. M., Dalby, N. O., Simonsen, C., Finger, B. C., Golubeva, A., Hammer, H., Bergmann, M. L., Kristiansen, Uffe, Krogsgaard-Larsen, Povl, Bräuner, Hans, Ebert, B., Frølund, Bente, Cryan, J. F. & Jensen, Anders A., Oct 2013, In: British Journal of Pharmacology. 170, 4, p. 919-32 14 p.

Research output: Contribution to journal › Journal article › Research › peer-review

GABA-B-agonistic activity of certain baclofen homologues

Attia, M., Herdeis, C. & Bräuner, Hans, 22 Aug 2013, In: Molecules. 18, 9, p. 10266-10284

Research output: Contribution to journal › Journal article › Research › peer-review

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

Kvist, T., Greenwood, J. R., Hansen, K. B., Traynelis, S. F. & Bräuner, Hans, 22 Aug 2013, In: Neuropharmacology. 75, p. 324-336 13 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Interactions between calcium and phosphorus in the regulation of the production of fibroblast growth factor 23 in vivo

Quinn, S. J., Thomsen, A. R. B., Pang, J. L., Kantham, L., Brown, E. M., Bräuner, Hans, Pollak, M. & Goltzman, D., 1 Feb 2013, In: American Journal of Physiology: Endocrinology and Metabolism. 304, 3, p. E310-320

Research output: Contribution to journal › Journal article › Research › peer-review

3-Substituted 2-phenyl-indoles: Privileged structures for medicinal chemistry

Johansson, K. H., Jørgensen, T. B., Gloriam, David E., Bräuner, Hans & Pedersen, D. S., 21 Jan 2013, In: R S C Advances. 3, 3, p. 945-960

Research output: Contribution to journal › Journal article › Research › peer-review

Synthesis and pharmacological characterization of certain baclofen analogues

Attia, M. I., Herdeis, C. & Bräuner, Hans, 1 Jan 2013, In: Digest Journal of Nanomaterials and Biostructures. 8, 1, p. 139-149

Research output: Contribution to journal › Journal article › Research › peer-review

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

Kvist, T., Steffensen, T. B., Greenwood, J. R., Mehrzad Tabrizi, F., Hansen, K. B., Gajhede, Michael, Pickering, Darryl S, Traynelis, S. F., Kastrup, Jette Sandholm Jensen & Bräuner, Hans, 2013, In: The Journal of Biological Chemistry. 288, p. 33124-35 12 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Discovery of a subtype-selective of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile

Kragholm, B., Kvist, T., Madsen, K. K., Jørgensen, L., Vogensen, S. B., Schousboe, Arne, Clausen, Rasmus Prætorius, Jensen, Anders A. & Bräuner, Hans, 2013, In: Biochemical Pharmacology. 86, p. 521-528

Research output: Contribution to journal › Journal article › Research › peer-review

Enhanced voluntary wheel running in GPRC6A receptor knockout mice

Clemmensen, Christoffer, Pehmøller, C., Klein, A. B., Ratner, C., Wojtaszewski, Jørgen F P & Bräuner, Hans, 2013, In: Physiology & Behavior. 118, p. 144-151 7 p.

Research output: Contribution to journal › Journal article › Research › peer-review

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

Clemmensen, Christoffer, Smajilovic, S., Madsen, A. N., Klein, A. B., Holst, Birgitte & Bräuner, Hans, 2013, In: Journal of Endocrinology. 217, 2, p. 151-60 10 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Synthesis of the calcilytic ligand NPS2143

Johansson, K. H., Cailly, T. B. G., Thomsen, A. R. B., Bräuner, Hans & Pedersen, D. S., 2013, In: Beilstein Journal of Organic Chemistry. 9, p. 1383-1387

Research output: Contribution to journal › Journal article › Research › peer-review

The L-alpha-amino acid receptor GPRC6A is expressed in the islets of Langerhans but is not involved in L-arginine-induced insulin release

Smajilovic, S., Clemmensen, Christoffer, Johansen, L. D., Wellendorph, Petrine, Holst, Jens Juul, Thams, P. G., Ogo, E. & Bräuner, Hans, 2013, In: Amino Acids. 44, 2, p. 383-390 8 p.

Research output: Contribution to journal › Journal article › Research › peer-review

cAMP biosensors applied in molecular pharmacological studies of G protein-coupled receptors

Mathiesen, Jesper M., Vedel, L. & Bräuner, Hans, 2013, In: Methods in Enzymology. 522, p. 191-207 17 p.

Research output: Contribution to journal › Journal article › Research

Strontium is a biased agonist of the calcium-sensing receptor in rat medullary thyroid carcinoma 6-23 cells

Thomsen, A. R. B., Worm, J., Jacobsen, S. E., Stahlhut, M., Latta, M. & Bräuner, Hans, Dec 2012, In: Journal of Pharmacology and Experimental Therapeutics. 343, 3, p. 638-49 12 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Novel strategies in drug discovery of the calcium-sensing receptor based on biased signaling

Thomsen, A. R. B., Smajilovic, S. & Bräuner, Hans, 1 Sep 2012, In: Current Drug Targets. 13, 10, p. 1324-35 12 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Molecular pharmacology of human NMDA receptors

Hedegaard, M., Hansen, K. B., Andersen, K. T., Bräuner, Hans & Traynelis, S. F., Sep 2012, In: Neurochemistry International. 61, 4, p. 601-609

Research output: Contribution to journal › Journal article › Research › peer-review

α4βδ GABA receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)

Absalom, N., Karim, N., Eghorn, L. F., Villumsen, I. S., Bay, T., Bräuner, Hans, Frølund, Bente, Clausen, Rasmus Prætorius, Olsen, Jesper Velgaard, Knudsen, Gitte Moos, Chebib, M. & Wellendorph, Petrine, 14 Aug 2012, In: Proceedings of the National Academy of Sciences USA (PNAS). 109, 33, p. 13404-13409 6 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Biased agonism of the calcium-sensing receptor

Thomsen, A. R. B., Hvidtfeldt, M. & Bräuner, Hans, Feb 2012, In: Cell Calcium. 51, 2, p. 107-116

Research output: Contribution to journal › Journal article › Research › peer-review

(1S, 3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a potent gamma-aminobutyric acid aminotransferase inactivator for the treatment of cocaine addiction

Pan, Y., Gerasimov, M. R., Kvist, T., Wellendorph, Petrine, Madsen, K. K., Pera, E., Lee, H., Schousboe, Arne, Chebib, M., Bräuner, Hans, Craft, C. M., Brodie, J. D., Schiffer, W. K., Dewey, S. L., Miller, S. R. & Silverman, R. B., 1 Jan 2012, In: Journal of Medicinal Chemistry. 55, 1, p. 357-366

Research output: Contribution to journal › Journal article › Research › peer-review

Extracellular Ca2+ is a danger signal activating the NLRP3 inflammasome through G protein-coupled calcium sensing receptors

Rossol, M., Pierer, M., Raulien, N., Quandt, D., Meusch, U., Rothe, K., Schubert, K., Schöneberg, T., Schaefer, M., Krügel, U., Smajilovic, S., Bräuner, Hans, Baerwald, C. & Wagner, U., 2012, In: Nature Communications. 3, p. 1329

Research output: Contribution to journal › Journal article › Research › peer-review

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

Clemmensen, Christoffer, Madsen, A. N., Smajilovic, S., Holst, Birgitte & Bräuner, Hans, 2012, In: Amino Acids. 43, 3, p. 1265-1275

Research output: Contribution to journal › Journal article › Research › peer-review

Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

Mølck, C., Harpsøe, Kasper, Gloriam, David E., Clausen, Rasmus Prætorius, Madsen, Ulf, Pedersen, L., Jimenez, H. N., Nielsen, S. M., Mathiesen, Jesper M. & Bräuner, Hans, 2012, In: Molecular Pharmacology. 82, 5, p. 929-37 9 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Structure-activity relationships for negative allosteric mGluR5 modulators

Kaae, B. H., Harpsøe, Kasper, Kvist, T., Mathiesen, Jesper M., Mølck, C., Gloriam, David E., Jimenez, H. N., Uberti, M. A., Nielsen, S. M., Nielsen, Birgitte, Bräuner, Hans, Sauerberg, P., Clausen, Rasmus Prætorius & Madsen, Ulf, 2012, In: ChemMedChem. 7, 3, p. 440-451

Research output: Contribution to journal › Journal article › Research › peer-review

Chemogenomic discovery of allosteric antagonists at the GPRC6A receptor

Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Thomsen, A. R. B., Phonekeo, K., Pedersen, D. S. & Bräuner, Hans, 23 Nov 2011, In: Chemistry & Biology. 18, 11, p. 1489-1498

Research output: Contribution to journal › Journal article › Research › peer-review

A highly selective agonist for the metabotropic glutamate receptor mGluR2

Nielsen, S. D., Fulco, M., Serpi, M., Nielsen, Birgitte, Hansen, M. B., Hansen, K. L., Thomsen, C., Brodbeck, R., Bräuner, Hans, Pellicciari, R., Norrby, P., Greenwood, J. R. & Clausen, Rasmus Prætorius, 23 Sep 2011, In: MedChemComm. 2, 11, p. 1120-1124

Research output: Contribution to journal › Journal article › Research › peer-review

Binding Mode of a Novel MPEP-Derived Metabotropic Glutamate Receptor Subtype 5 (mGluR5) NAM, 1,3-Bis(pyridin-2-ylethynyl)Benzene

Molck, C., Harpsøe, Kasper, Gloriam, David E., Kaae, B. H., Jimenez, H. N., Uberti, M. A., Topiol, S., Clausen, Rasmus Prætorius, Madsen, Ulf, Nielsen, S. M., Mathiesen, Jesper M. & Bräuner, Hans, Sep 2011, In: Current Neuropharmacology. 9, p. 43-43

Research output: Contribution to journal › Conference abstract in journal › Research

Kemogenomik: Receptoren set fra lægemiddelstoffets synspunkt

Johansson, H., Jørgensen, T. B., Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Pedersen, D. S. & Bräuner, Hans, 2011, In: Dansk Kemi. 92, 11, p. 22-26

Research output: Contribution to journal › Journal article › Research

The use of Xenopus oocytes in drug screening

Kvist, T., Hansen, K. B. & Bräuner, Hans, 2011, In: Expert Opinion on Drug Discovery. 6, 2, p. 141-153

Research output: Contribution to journal › Review › Research › peer-review

Transmembrane a-helix 2 and 7 are important for small molecule-mediated activation of the GLP-1 receptor

Underwood, C. R., Knudsen, S. M., Wulff, B. S., Bräuner, Hans, Lau, J., Knudsen, L. B., Peters, G. H. J. & Reedtz-Runge, S., 2011, In: Pharmacology. 88, 5-6, p. 340-348 9 p.

Research output: Contribution to journal › Journal article › Research › peer-review

1,2,3-triazolyl amino acids as AMPA receptor ligands

Stanley, N. J., Pedersen, D. S., Nielsen, Birgitte, Kvist, T., Mathiesen, Jesper M., Bräuner, Hans, Taylor, D. K. & Abell, A. D., 15 Dec 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 24, p. 7512-7515

Research output: Contribution to journal › Journal article › Research › peer-review

Biologiens låsesmed

Bräuner, Hans, 2 Dec 2010, In: Universitetsavisen. 2010, 9, p. 22-23

Research output: Contribution to journal › Journal article › Communication

Kemogenomik: receptoren set fra lægemiddelstoffets synspunkt

Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Pedersen, D. S. & Bräuner, Hans, Dec 2010, In: Lægemiddelforskning. 2010, p. 28-30

Research output: Contribution to journal › Journal article › Communication

A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity

Stanley, N. J., Hutchinson, M. R., Kvist, T., Nielsen, Birgitte, Mathiesen, Jesper M., Bräuner, Hans, Avery, T. D., Tiekink, E. R. T., Pedersen, D. S., Irvine, R. J., Abell, A. D. & Taylor, D. K., 2010, In: Bioorganic & Medicinal Chemistry. 18, 16, p. 6089-6098

Research output: Contribution to journal › Journal article › Research › peer-review

Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites

Sabbatini, P., Wellendorph, Petrine, Høg, S., Pedersen, M. H. F., Bräuner, Hans, Martiny, L., Frølund, Bente & Clausen, Rasmus Prætorius, 2010, In: Journal of Medicinal Chemistry. 53, 17, p. 6506-6510

Research output: Contribution to journal › Journal article › Research › peer-review

Homology modelling of the GABA transporter and analysis of tiagabine binding

Skovstrup, S., Taboureau, O., Bräuner, Hans & Jørgensen, Flemming Steen, 2010, In: ChemMedChem. 5, 7, p. 986-1000

Research output: Contribution to journal › Journal article › Research › peer-review

Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists

Hansen, K. B., Mullasseril, P., Dawit, S., Kurtkaya, N. L., Yuan, H., Vance, K. M., Orr, A. G., Kvist, T., Ogden, K. K., Le, P., Vellano, K. M., Lewis, I., Kurtkaya, S., Du, Y., Qui, M., Murphy, T. J., Snyder, J. P., Bräuner, Hans & Traynelis, S. F., 2010, In: Journal of Pharmacology and Experimental Therapeutics. 333, 3, p. 650-662

Research output: Contribution to journal › Journal article › Research › peer-review

Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization

Conti, P., Pinto, A., Tamborini, L., Madsen, Ulf, Nielsen, Birgitte, Bräuner, Hans, Hansen, K. B., Landucci, E., Pellegrini-Giampietro, D. E., De Sarro, G., Donato Di Paola, E. & De Micheli, C., 2010, In: ChemMedChem. 5, 9, p. 1465-1475

Research output: Contribution to journal › Journal article › Research › peer-review

Novel radioiodinated γ-hydroxybutyric acid analogues for radiolabeling and photolinking of high-affinity γ-hydroxybutyric acid binding sites

Wellendorph, Petrine, Høg, S., Sabbatini, P., Pedersen, M. H. F., Martiny, L., Knudsen, Gitte Moos, Frølund, Bente, Clausen, Rasmus Prætorius & Bräuner, Hans, 2010, In: Journal of Pharmacology and Experimental Therapeutics. 335, 2, p. 458-464

Research output: Contribution to journal › Journal article › Research › peer-review

Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists

Mosley, C. A., Acker, T. M., Hansen, K. B., Mullasseril, P., Andersen, K. T., Le, P., Vellano, K. M., Bräuner, Hans, Liotta, D. C. & Traynelis, S. F., 2010, In: Journal of Medicinal Chemistry. 53, 15, p. 5476-5490

Research output: Contribution to journal › Journal article › Research › peer-review

(R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABA_B receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action

Lehmann, A., Antonsson, M., Holmberg, A. A., Blackshaw, L. A., Brändén, L., Bräuner, Hans, Christiansen, B., Dent, J., Elebring, T., Jacobson, B., Jensen, J., Mattsson, J. P., Nilsson, K., Oja, S. S., Page, A. J., Saransaari, P. & von Unge, S., 2009, In: Journal of Pharmacology and Experimental Therapeutics. 331, 2, p. 504-512

Research output: Contribution to journal › Journal article › Research › peer-review

Molecular basis for amino acid sensing by family C G-protein-coupled receptors

Wellendorph, Petrine & Bräuner, Hans, 2009, In: British Journal of Pharmacology. 156, 6, p. 869-884

Research output: Contribution to journal › Journal article › Research › peer-review

Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor

Faure, H., Gorojankina, T., Rice, N., Dauban, P., Dodd, R. H., Bräuner, Hans, Rognan, D. & Ruat, M., 2009, In: Cell Calcium. 46, 5-6, p. 323-332

Research output: Contribution to journal › Journal article › Research › peer-review

Molecular pharmacology of promiscuous seven transmembrane receptors sensing organic nutrients

Wellendorph, Petrine, Johansen, L. D. & Bräuner, Hans, 2009, In: Molecular Pharmacology. 76, 3, p. 453-465

Research output: Contribution to journal › Journal article › Research › peer-review

No evidence for a bone phenotype in GPRC6A knockout mice under normal physiological conditions

Wellendorph, Petrine, Johansen, L. D., Jensen, Anders A., Casanova, E., Gassmann, M., Deprez, P., Clément-Lacroix, P., Bettler, B. & Bräuner, Hans, 2009, In: Journal of Molecular Endocrinology. 42, 3, p. 215-223

Research output: Contribution to journal › Journal article › Research › peer-review

Phenylacetic acids and the structurally related non-steroidal anti-inflammatory drug diclofenac bind to specific gamma-hydroxybutyric acid sites in rat brain

Wellendorph, Petrine, Høg, S., Skonberg, C. & Bräuner, Hans, 2009, In: Fundamental and Clinical Pharmacology. 23, 2, p. 207-213 7 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Receptorer i historisk og nutidig belysning

Bräuner, Hans, 2009, In: Carlsbergfondet. Aarsskrift. p. 30-35

Research output: Contribution to journal › Journal article › Communication

The GABA_B1a isoform mediates heterosynaptic depression at hippocampal mossy fiber synapses

Guetg, N., Seddik, R., Vigot, R., Turecek, R., Gassmann, M., Vogt, K. E., Bräuner, Hans, Shigemoto, R., Kretz, O., Frotscher, M., Kulik, Á. & Bettler, B., 2009, In: Journal of Neuroscience. 29, 5, p. 1414-1423

Research output: Contribution to journal › Journal article › Research › peer-review

The four human ¿-aminobutyric acid (GABA) transporters: pharmacological characterization and validation of a highly efficient screening assay

Kvist, T., Christiansen, B., Jensen, Anders A. & Bräuner, Hans, 2009, In: Combinatorial Chemistry & High Throughput Screening. 12, 3, p. 241-249

Research output: Contribution to journal › Journal article › Research › peer-review

The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization

Clausen, Rasmus Prætorius, Naur, P., Kristensen, Anders Skov, Greenwood, J. R., Strange, M., Bräuner, Hans, Jensen, Anders A., Nielsen, A. S. T., Geneser, U., Ringgaard, L. M., Nielsen, Birgitte, Pickering, Darryl S, Brehm, L., Gajhede, Michael, Krogsgaard-Larsen, Povl & Kastrup, Jette Sandholm Jensen, 2009, In: Journal of Medicinal Chemistry. 52, 15, p. 4911-4922

Research output: Contribution to journal › Journal article › Research › peer-review

3B but which 3B? And that's just one of the questions: the heterogeneity of human 5-HT3 receptors

Jensen, Anders A., Davies, P. A., Bräuner, Hans & Krzywkowski, K., 2008, In: TIPS - Trends in Pharmacological Sciences. 29, 9, p. 437-444

Research output: Contribution to journal › Journal article › Research › peer-review

Characterization of GPRC6A: a 7TM receptor activated by L-alpha-amino acids and positively modulated by divalent cations

Wellendorph, Petrine, Hansen, K. B., Christiansen, B., Burhenne, N., Balsgaard, A., Greenwood, J. R., Walter, B., Schmale, H., Egebjerg, J. & Bräuner, Hans, 2008, In: Fundamental and Clinical Pharmacology. Suppl. 2, p. 19

Research output: Contribution to journal › Conference abstract in journal › Research

Characterization of the effects of four HTR3B polymorphisms on human 5-HT_3AB receptor expression and signalling

Krzywkowski, K. M., Davies, P. A., Irving, A. J., Bräuner, Hans & Jensen, Anders A., 2008, In: Pharmacogenetics and Genomics (Print Edition). 18, 12, p. 1027-1040

Research output: Contribution to journal › Journal article › Research › peer-review

En genetisk variation i en serotonin–receptor – et muligt link til depression?

Krzywkowski, K. M., Feinberg-Zadek, P., Davies, P. A., Jensen, Anders A. & Bräuner, Hans, 2008, In: Dansk Kemi 83. 89, 6/7

Research output: Contribution to journal › Journal article › Communication

High-frequency HTR3B variant associated with major depression dramatically augments the signaling of the human 5-HT_3AB receptor

Krzywkowski, K. M., Davies, P. A., Feinberg-Zadek, P. L., Bräuner, Hans & Jensen, Anders A., 2008, In: Proceedings of the National Academy of Science of the United States of America. 105, 2, p. 722-727

Research output: Contribution to journal › Journal article › Research › peer-review

N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands

Clausen, Rasmus Prætorius, Christensen, C., Hansen, K. B., Greenwood, J. R., Jørgensen, L., Micale, N., Madsen, J. C., Nielsen, Birgitte, Egebjerg, J., Bräuner, Hans, Traynelis, S. F. & Kristensen, Jesper Langgaard, 2008, In: Journal of Medicinal Chemistry. 51, 14, p. 4179-87

Research output: Contribution to journal › Journal article › Research › peer-review

Novel high-affinity and selective biaromatic 4-substituted ¿-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies

Høg, S., Wellendorph, Petrine, Nielsen, Birgitte, Frydenvang, Karla Andrea, Dahl, I. F., Bräuner, Hans, Brehm, L., Frølund, Bente & Clausen, Rasmus Prætorius, 2008, In: Journal of Medicinal Chemistry. 51, 24, p. 8088-8095

Research output: Contribution to journal › Journal article › Research › peer-review

Ny human GABA-transportør: et muligt mål for behandling af epilepsi

Christiansen, B., Kvist, T., Jensen, Anders A. & Bräuner, Hans, 2008, In: Lægemiddelforskning. p. 25-27

Research output: Contribution to journal › Journal article › Communication

Pharmacological characterization of ligands at recombinant NMDA receptor subtypes by electrophysiological recordings and intracellular calcium measurements

Hansen, K. B., Bräuner, Hans & Egebjerg, J., 2008, In: Combinatorial Chemistry & High Throughput Screening. 11, 4, p. 304-315

Research output: Contribution to journal › Journal article › Research › peer-review

Regulation of GABA_B receptors by extracellular proteins and phosphorylation

Tiao, J. Y., Bradaia, A., Jensen, A. A., Biermann, B., Bräuner, Hans, Müller, M., Kaupmann, K., Gassmann, M. & Bettler, B., 2008, In: Neuropharmacology. 4, p. 626

Research output: Contribution to journal › Conference abstract in journal › Research

Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid

Pinto, A., Conti, P., De Amici, M., Tamborini, L., Madsen, Ulf, Nielsen, Birgitte, Christesen, T., Bräuner, Hans & De Micheli, C., 2008, In: Journal of Medicinal Chemistry. 51, 7, p. 2311-2315

Research output: Contribution to journal › Journal article › Research › peer-review

The rat GPRC6A: cloning and characterization

Wellendorph, Petrine, Burhenne, N., Christiansen, B., Walter, B., Schmale, H. & Bräuner, Hans, 15 Jul 2007, In: Gene. 396, 2, p. 257-267 11 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Allosteric modulation of the calcium-sensing receptor

Jensen, Anders A. & Bräuner, Hans, 2007, In: Current Neuropharmacology. 5, 3, p. 180-186

Research output: Contribution to journal › Journal article › Research › peer-review

Cloning and characterization of a functional human ¿-aminobutyric acid (GABA) transporter, human GAT-2

Christiansen, B., Meinild, A., Jensen, Anders A. & Bräuner, Hans, 2007, In: Journal of Biological Chemistry. 282, 27, p. 19331-19341 11 p.

Research output: Contribution to journal › Journal article › Research › peer-review

En genetisk variation i en serotonin-receptor: et muligt link til depression?

Krzywkowski, K. M., Davies, P. A., Feinberg-Zadek, P. L., Jensen, Anders A. & Bräuner, Hans, 2007, In: Lægemiddelforskning. p. 30-31

Research output: Contribution to journal › Journal article › Communication

Erratum: Synthesis and pharmacology of glutamate receptor ligands: New isothiazole analogues of ibotenic acid (Organic and Biomolecular Chemistry (2007) 5 DOI:10.1039/b615162k)

Jørgensen, Charlotte Grube, Clausen, Rasmus Prætorius, Hansen, K. B., Bräuner, Hans, Nielsen, Birgitte, Metzler, B., Kehler, J., Krogsgaard-Larsen, Povl & Madsen, Ulf, 2007, In: Organic and Biomolecular Chemistry. 5, 5, p. 848 1 p.

Research output: Contribution to journal › Comment/debate › Research › peer-review

Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA

Jensen, Anders A., Christesen, T., Bølcho, U., Greenwood, J. R., Postorino, G., Vogensen, S. B., Johansen, Tommy Nørskov, Egebjerg, J., Bräuner, Hans & Clausen, Rasmus Prætorius, 2007, In: Journal of Medicinal Chemistry. 50, 17, p. 4177-4185 9 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Molekylær farmakologiske subtyper

Bräuner, Hans, 2007, In: Lundbeckfondens årsskrift 2006-2007. 2006-2007, p. 30-32

Research output: Contribution to journal › Journal article › Communication

Naturally occurring variations in the human 5-HT_3A gene profoundly impact 5-HT₃ receptor function and expression

Krzywkowski, K. M., Jensen, Anders A., Connolly, C. N. & Bräuner, Hans, 2007, In: Pharmacogenetics and Genomics (Print Edition). 17, 4, p. 255-266

Research output: Contribution to journal › Journal article › Research › peer-review

Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors

Jørgensen, Charlotte Grube, Bräuner, Hans, Nielsen, Birgitte, Kehler, J., Clausen, Rasmus Prætorius, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2007, In: Bioorganic & Medicinal Chemistry. 15, 10, p. 3524-3538

Research output: Contribution to journal › Journal article › Research › peer-review

Pharmacological characterization of mouse GPRC6A, an L-alpha-amino-acid receptor modulated by divalent cations

Christiansen, B., Hansen, K. B., Wellendorph, Petrine & Bräuner, Hans, 2007, In: British Journal of Pharmacology. 150, 6, p. 798-807

Research output: Contribution to journal › Journal article › Research › peer-review

Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors

Bräuner, Hans, Wellendorph, Petrine & Jensen, Anders A., 2007, In: Current Drug Targets. 8, 1, p. 169-184

Research output: Contribution to journal › Journal article › Research › peer-review

Synthesis and pharmacological characterization at glutamate receptors of erythro- and threo-tricholomic acid and homologues thereof

Conti, P., De Amici, M., Roda, G., Pinto, A., Tamborini, L., Madsen, Ulf, Nielsen, Birgitte, Bräuner, Hans & De Micheli, C., 2007, In: Tetrahedron. 63, 10, p. 2249-2256

Research output: Contribution to journal › Journal article › Research › peer-review

Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid

Jørgensen, Charlotte Grube, Clausen, Rasmus Prætorius, Hansen, K. B., Bräuner, Hans, Nielsen, Birgitte, Metzler, B., Kehler, J., Krogsgaard-Larsen, Povl & Madsen, Ulf, 2007, In: Organic & Biomolecular Chemistry. 5, 3, p. 463-471

Research output: Contribution to journal › Journal article › Research › peer-review

Synthesis of conformationally constrained glutamic acid homologues and investigation of their pharmacological profiles

Conti, P., Pinto, A., Tamborini, L., Grazioso, G., De Sarro, G., Bräuner, Hans, Szabo, G., Hársing, L. G. & De Micheli, C., 2007, In: ChemMedChem. 2, 11, p. 1639-1647 9 p.

Research output: Contribution to journal › Journal article › Research › peer-review

Differential compartmentalization and distinct functions of GABAB receptor variants

Vigot, R., Barbieri, S., Bräuner, Hans, Turecek, R., Shigemoto, R., Zhang, Y., Luján, R., Jacobson, L. H., Biermann, B., Fritschy, J., Vacher, C., Müller, M., Sansig, G., Guetg, N., Cryan, J. F., Kaupmann, K., Gassmann, M., Oertner, T. G. & Bettler, B., 18 May 2006, In: Neuron. 50, 4, p. 589-601

Research output: Contribution to journal › Journal article › Research › peer-review

Activity of L-alpha-amino acids at the promiscuous goldfish odorant receptor 5.24

Christiansen, B., Wellendorph, Petrine & Bräuner, Hans, 24 Apr 2006, In: European Journal of Pharmacology. 536, 1-2, p. 98-101

Research output: Contribution to journal › Journal article › Research › peer-review

Known regulators of nitric oxide synthase and arginase are agonists at the human G-protein-coupled receptor GPRC6A

Christiansen, B., Wellendorph, Petrine & Bräuner, Hans, Apr 2006, In: British Journal of Pharmacology. 147, 8, p. 855-63

Research output: Contribution to journal › Journal article › Research › peer-review