Jesper M. Mathiesen
Associate Professor
Molecular and Cellular Pharmacology
Jagtvej 160
2100 København Ø
- 2003
- Published
Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP
Mathiesen, Jesper M., Svendsen, N., Bräuner, Hans, Thomsen, C. & Ramirez, M. T., Mar 2003, In: British Journal of Pharmacology. 138, 6, p. 1026-30Research output: Contribution to journal › Journal article › Research › peer-review
- 2005
- Published
Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2
Mathiesen, Jesper M., Ulven, Trond, Martin, L., Gerlach, L., Heinemann, A. & Kostenis, E., 2005, In: Molecular Pharmacology. 68, 2, p. 393-402 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Molecular pharmacology and therapeutic prospects of metabotropic glutamate receptor allosteric modulators
Ritzén, A., Mathiesen, Jesper M. & Thomsen, C., 1 Oct 2005, In: Basic and Clinical Pharmacology and Toxicology. 97, 4, p. 202-213 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2006
- Published
6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists
Ulven, Trond, Little, P. B., Receveur, J., Frimurer, Thomas Michael, Rist, Ø., Nørregaard, P. K., Mathiesen, Jesper M. & Högberg, T., 2006, In: Bioorganic & Medicinal Chemistry Letters. 16, 4, p. 1070-1075 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits
Ulven, Trond, Receveur, J., Grimstrup, M., Rist, Ø., Frimurer, Thomas Michael, Gerlach, L., Mathiesen, Jesper M., Kostenis, E., Uller, L. & Högberg, T., 2006, In: Journal of Medicinal Chemistry. 49, 23, p. 6638-6641 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
On the mechanism of interaction of potent, surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2
Mathiesen, Jesper M., Christopoulos, A., Ulven, Trond, Royer, J. F., Campillo, M., Heinemann, A., Pardo, L. & Kostenis, E., 2006, In: Molecular Pharmacology. 69, 4, p. 1441-1453 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The metabotropic glutamate receptor 4 is internalized and desensitized upon protein kinase C activation
Mathiesen, Jesper M. & Ramirez, M. T., 1 Jun 2006, In: British Journal of Pharmacology. 148, 3, p. 279-290 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2007
- Published
Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation
Uller, L., Mathiesen, Jesper M., Alenmyr, L., Korsgren, M., Ulven, Trond, Högberg, T., Andersson, G., Persson, C. G. A. & Kostenis, E., 1 Feb 2007, In: Respiratory Research. 8, 16Research output: Contribution to journal › Journal article › Research › peer-review
- 2009
- Published
The C-terminal tail of CRTH2 is a key molecular determinant that constrains GalphaI- and downstream-signaling cascade activation
Schroeder, R., Merten, N., Mathiesen, Jesper M., Martini, L., Letunic, A. K., Krop, F., Blaukat, A., Fang, Y., Tran, E., Ulven, Trond, Drewke, C., Whistler, J., Pardo, L., Gomeza, J. & Kostenis, E., 2009, In: Journal of Biological Chemistry. 284, 2, p. 1324-1336 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2010
- Published
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. 6089-6098Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2
Grimstrup, M., Rist, Ø., Receveur, J., Frimurer, Thomas Michael, Ulven, Trond, Mathiesen, Jesper M., Kostenis, E. & Högberg, T., 1 Feb 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 3, p. 1181-1185 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
Grimstrup, M., Receveur, J. M., Rist, Ø., Frimurer, Thomas Michael, Nielsen, P. A., Mathiesen, Jesper M. & Högberg, T., 1 Mar 2010, In: Bioorganic and Medicinal Chemistry Letters. 20, 5, p. 1638-1641 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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. 7512-7515Research output: Contribution to journal › Journal article › Research › peer-review
- 2011
- Published
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. 43-43Research output: Contribution to journal › Conference abstract in journal › Research
- Published
Crystal structure of the β2 adrenergic receptor-Gs protein complex
Rasmussen, Søren Gøgsig Faarup, DeVree, B. T., Zou, Y., Kruse, A. C., Chung, K. Y., Kobilka, T. S., Thian, F. S., Chae, P. S., Pardon, E., Calinski, D., Mathiesen, Jesper M., Shah, S. T. A., Lyons, J. A., Caffrey, M., Gellman, S. H., Steyaert, J., Skiniotis, G., Weis, W. I., Sunahara, R. K. & Kobilka, B. K., 29 Sep 2011, In: Nature. 477, 7366, p. 549-55 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2012
- Published
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
- Published
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. 440-451Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Crystal structure of the μ-opioid receptor bound to a morphinan antagonist
Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Mathiesen, Jesper M., Sunahara, R. K., Pardo, L., Weis, W. I., Kobilka, B. K. & Granier, S., 17 May 2012, In: Nature. 485, 7398, p. 321-326 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2013
- Published
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
- 2014
- Published
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
- Published
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
- 2015
- Published
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
- 2016
- Published
Allosteric modulators of group III metabotropic glutamate receptors as novel therapeutics
Mathiesen, Jesper M. & Teresa Ramirez, M., 19 Apr 2016, Allosteric Receptor Modulation in Drug Targeting. CRC Press, p. 207-234 28 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
- 2018
- Published
Gs protein peptidomimetics as allosteric modulators of the β2-adrenergic receptor
Boyhus, L. E., Danielsen, Mia, Bengtson, N. S., Kunze, M. B. A., Kubiak, X., Sminia, T. J., Løper, J. H., Tran, P. T., Lindorff-Larsen, Kresten, Rasmussen, Søren Gøgsig Faarup, Mathiesen, Jesper M. & Pedersen, D. S., 2018, In: RSC Advances. 8, 4, p. 2219-2228 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2019
- Published
Structural insights into the activation of metabotropic glutamate receptors
Koehl, A., Hu, H., Feng, D., Sun, B., Zhang, Y., Robertson, M. J., Chu, M., Kobilka, T. S., Laeremans, T., Steyaert, J., Tarrasch, J., Dutta, S., Fonseca, R., Weis, W. I., Mathiesen, Jesper M., Skiniotis, G. & Kobilka, B. K., 7 Feb 2019, In: Nature. 566, 7742, p. 79-84Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structural Insights into the Process of GPCR-G Protein Complex Formation
Liu, X., Xu, X., Hilger, D., Aschauer, P., Tiemann, J. K. S., Du, Y., Liu, H., Hirata, K., Sun, X., Guixa-Gonzalez, R., Mathiesen, Jesper M., Hildebrand, P. W. & Kobilka, B. K., 16 May 2019, In: Cell. 177, 5, p. P1243-1251Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands
Gaiser, B. I., Danielsen, Mia, 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
- 2020
- Published
Delineation of molecular determinants for FR900359 inhibition of Gq/11 unlocks inhibition of Gαs
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. 13850-13861Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
- Published
Structural insights into differences in G protein activation by family A and family B GPCRs
Hilger, D., Kumar, K. K., Hu, H., Pedersen, M. F., O'Brien, E. S., Giehm, L., Jennings, C., Eskici, G., Inoue, A., Lerch, M., Mathiesen, Jesper M., Skiniotis, G. & Kobilka, B. K., 2020, In: Science. 369, 6503Research output: Contribution to journal › Comment/debate › Research › peer-review
- Published
Structures of metabotropic GABAB receptor
Papasergi-Scott, M. M., Robertson, M. J., Seven, A. B., Panova, O., Mathiesen, Jesper M. & Skiniotis, G., 2020, In: Nature. 584, 7820, p. 310-314 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2021
- Published
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. 455-459Research output: Contribution to journal › Journal article › Research › peer-review
- Published
G-protein activation by a metabotropic glutamate receptor
Seven, A. B., Barros-Álvarez, X., de Lapeyrière, M., Papasergi-Scott, M. M., Robertson, M. J., Zhang, C., Nwokonko, R. M., Gao, Y., Meyerowitz, J. G., Rocher, J. P., Schelshorn, D., Kobilka, B. K., Mathiesen, Jesper M. & Skiniotis, G., 2021, In: Nature. 595, p. 450-454Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- Published
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. 104-113Research output: Contribution to journal › Journal article › Research › peer-review
- 2023
- Published
Glycine: a long-sought novel ligand for GPR158
Rosenkilde, Mette & Mathiesen, Jesper M., 2023, In: Trends in Pharmacological Sciences. 44, 8, p. 489-491Research output: Contribution to journal › Letter › Research › peer-review
- 2024
- Published
Allosteric modulation and G-protein selectivity of the Ca2+-sensing receptor
He, F., Wu, C. G., Gao, Y., Rahman, Sabrina Nalini, Zaoralová, M., Papasergi-Scott, M. M., Gu, T. J., Robertson, M. J., Seven, A. B., Li, L., Mathiesen, Jesper M. & Skiniotis, G., 2024, In: Nature. 626, p. 1141–1148Research output: Contribution to journal › Journal article › Research › peer-review
ID: 4873159
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Gs protein peptidomimetics as allosteric modulators of the β2-adrenergic receptor
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
42
downloads
Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
25
downloads
Delineation of the GPR15 receptor-mediated Gα protein signalling profile in recombinant mammalian cells
Research output: Contribution to journal › Journal article › Research › peer-review
Published