Jesper M. Mathiesen

Jesper M. Mathiesen

Associate Professor


  1. 2024
  2. 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. 1141–1148

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. 2023
  4. Published

    Glycine: a long-sought novel ligand for GPR158

    Rosenkilde, Mette & Mathiesen, Jesper M., 2023, In: Trends in Pharmacological Sciences. 44, 8, p. 489-491

    Research output: Contribution to journalLetterResearchpeer-review

  5. 2022
  6. 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. 104-113

    Research output: Contribution to journalJournal articleResearchpeer-review

  7. 2021
  8. 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. 455-459

    Research output: Contribution to journalJournal articleResearchpeer-review

  9. 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. 450-454

    Research output: Contribution to journalJournal articleResearchpeer-review

  10. 2020
  11. 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. 13850-13861

    Research output: Contribution to journalJournal articleResearchpeer-review

  12. 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 journalJournal articleResearchpeer-review

  13. 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, 6503

    Research output: Contribution to journalComment/debateResearchpeer-review

  14. 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 journalJournal articleResearchpeer-review

  15. 2019
  16. Published

    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 journalJournal articleResearchpeer-review

  17. 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. P1243-1251

    Research output: Contribution to journalJournal articleResearchpeer-review

  18. 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. 79-84

    Research output: Contribution to journalJournal articleResearchpeer-review

  19. 2018
  20. Published

    Gs protein peptidomimetics as allosteric modulators of the β2-adrenergic receptor

    Boyhus, L. E., Danielsen, M., 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 journalJournal articleResearchpeer-review

  21. 2016
  22. 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 proceedingBook chapterResearchpeer-review

  23. 2015
  24. 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 journalJournal articleResearchpeer-review

  25. 2014
  26. 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 journalJournal articleResearchpeer-review

  27. 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 journalJournal articleResearchpeer-review

  28. 2013
  29. 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 journalJournal articleResearch

  30. 2012
  31. 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 journalJournal articleResearchpeer-review

  32. 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 journalJournal articleResearchpeer-review

  33. 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. 440-451

    Research output: Contribution to journalJournal articleResearchpeer-review

  34. 2011
  35. 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 journalJournal articleResearchpeer-review

  36. 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. 43-43

    Research output: Contribution to journalConference abstract in journalResearch

  37. 2010
  38. 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. 7512-7515

    Research output: Contribution to journalJournal articleResearchpeer-review

  39. 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 journalJournal articleResearchpeer-review

  40. 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 journalJournal articleResearchpeer-review

  41. 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. 6089-6098

    Research output: Contribution to journalJournal articleResearchpeer-review

  42. 2009
  43. 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 journalJournal articleResearchpeer-review

  44. 2007
  45. 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, 16

    Research output: Contribution to journalJournal articleResearchpeer-review

  46. 2006
  47. 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 journalJournal articleResearchpeer-review

  48. 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 journalJournal articleResearchpeer-review

  49. 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 journalJournal articleResearchpeer-review

  50. 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 journalJournal articleResearchpeer-review

  51. 2005
  52. 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 journalJournal articleResearchpeer-review

  53. 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 journalJournal articleResearchpeer-review

  54. 2003
  55. 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. 1026-30

    Research output: Contribution to journalJournal articleResearchpeer-review

ID: 4873159