Kasper Harpsøe

Kasper Harpsøe

Research consultant


  1. 2023
  2. Published

    A community Biased Signaling Atlas

    Caroli, J., Mamyrbekov, A., Harpsøe, Kasper, Gardizi, S., Dörries, L., Ghosh, E., Hauser, Alexander Sebastian, Kooistra, Albert J. & Gloriam, David E., 2023, In: Nature Chemical Biology. 19, p. 531–535

    Research output: Contribution to journalComment/debateResearchpeer-review

  3. Published

    Comprehensive Peptide Cyclization Examination Yields Optimized APP Scaffolds with Improved Affinity toward Mint2

    Bartling, Christian Reinhard Otto, Alexopoulou, Flora, Kuschert, S., Chin, Y. K. Y., Jia, X., Sereikaité, Vita, Özcelik, D., Jensen, T. M., Jain, P., Nygaard, M. M., Harpsøe, Kasper, Gloriam, David E., Mobli, M. & Strømgaard, Kristian, 2023, In: Journal of Medicinal Chemistry. 66, 4, p. 3045-3057

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Published

    Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT2A Receptor Agonist

    Marcher, Emil, Nykodemová, J., Harpsøe, Kasper, Jensen, Anders A. & Kristensen, Jesper Langgaard, 2023, In: ACS Medicinal Chemistry Letters. 14, 3, p. 319–325

    Research output: Contribution to journalJournal articleResearchpeer-review

  5. Published

    Ligand selectivity hotspots in serotonin GPCRs

    Simon, Ícaro Ariel, Bjørn-Yoshimoto, Walden, Harpsøe, Kasper, Iliadis, S., Svensson, B., Jensen, Anders A. & Gloriam, David E., 2023, In: Trends in Pharmacological Sciences. 44, 12, p. 978-990

    Research output: Contribution to journalReviewResearchpeer-review

  6. Published

    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 journalJournal articleResearchpeer-review

  7. Published

    Structure–Activity Assessment and In-Depth Analysis of Biased Agonism in a Set of Phenylalkylamine 5-HT2A Receptor Agonists

    Pottie, E., Poulie, Christian Bernard Matthijs, Simon, Ícaro Ariel, Harpsøe, Kasper, D’Andrea, L., Komarov, I. V., Gloriam, David E., Jensen, Anders A., Kristensen, Jesper Langgaard & Stove, C. P., 2023, In: ACS Chemical Neuroscience. 14, 15, p. 2727–2742

    Research output: Contribution to journalJournal articleResearchpeer-review

  8. 2022
  9. Published

    Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT2A Receptor Agonists

    Poulie, Christian Bernard Matthijs, Pottie, E., Simon, I. A., Harpsøe, Kasper, D’andrea, L., Komarov, I. V., Gloriam, David E., Jensen, Anders A., Stove, C. P. & Kristensen, Jesper Langgaard, 2022, In: Journal of Medicinal Chemistry. 65, 18, p. 12031–12043

    Research output: Contribution to journalJournal articleResearchpeer-review

  10. Published

    GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors

    Huang, S., Xu, P., Shen, D., Simon, I. A., Mao, C., Tan, Y., Zhang, H., Harpsøe, Kasper, Li, H., Zhang, Y., You, C., Yu, X., Jiang, Y., Zhang, Y., Gloriam, David E. & Xu, H. E., 2022, In: Molecular Cell. 82, 14, p. 2681-2695.e6 15 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  11. Published

    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 journalJournal articleResearchpeer-review

  12. Published

    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 journalLetterResearchpeer-review

  13. 2021
  14. Published

    Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors

    Rostrup, F., Falk-petersen, C. B., Harpsøe, Kasper, Buchleithner, S., Conforti, I., Jung, S., Gloriam, David E., Schirmeister, T., Wellendorph, Petrine & Frølund, Bente, 22 Apr 2021, In: Journal of Medicinal Chemistry. 64, 8, p. 4730-4743 14 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  15. Published

    A novel red fluorescence dopamine biosensor selectively detects dopamine in the presence of norepinephrine in vitro

    Nakamoto, C., Goto, Y., Tomizawa, Y., Fukata, Y., Fukata, M., Harpsøe, Kasper, Gloriam, David E., Aoki, K. & Takeuchi, T., 2021, In: Molecular Brain. 14, 1, 14 p., 173.

    Research output: Contribution to journalJournal articleResearchpeer-review

  16. Published

    Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors

    Falk-Petersen, C. B., Rostrup, F., Löffler, R., Buchleihtner, S., Harpsøe, Kasper, Gloriam, David E., Frølund, Bente & Wellendorph, Petrine, 2021, In: Molecular Pharmacology. 100, 1, p. 46-56

    Research output: Contribution to journalJournal articleResearchpeer-review

  17. Published

    Peptide inhibitors as tool compounds targeting GPCR signaling

    Daver, H., Harpsøe, Kasper & Gloriam, David E., 2021, In: European Biophysics Journal. 50, SUPPL 1, p. 161-161 238.

    Research output: Contribution to journalConference abstract in journalResearchpeer-review

  18. Published

    Structural insights into the lipid and ligand regulation of serotonin receptors

    Xu, P., Huang, S., Zhang, H., Mao, C., Zhou, X. E., Cheng, X., Simon, I. A., Shen, D., Yen, H., Robinson, C. V., Harpsøe, Kasper, Svensson, B., Guo, J., Jiang, H., Gloriam, David E., Melcher, K., Jiang, Y., Zhang, Y. & Xu, H. E., 2021, In: Nature. 592, p. 469-473

    Research output: Contribution to journalJournal articleResearchpeer-review

  19. Published

    Targeting the APP-Mint2 Protein-Protein Interaction with a Peptide-Based Inhibitor Reduces Amyloid-β Formation

    Bartling, Christian Reinhard Otto, Jensen, T. M. T., Henry, S. M., Colliander, A. L., Sereikaité, Vita, Wenzler, M., Jain, P., Maric, H. M., Harpsøe, Kasper, Pedersen, S. W., Clemmensen, L. S., Haugaard-Kedström, L. M., Gloriam, David E., Ho, A. & Strømgaard, Kristian, 2021, In: Journal of the American Chemical Society. 143, 2, p. 891-901

    Research output: Contribution to journalJournal articleResearchpeer-review

  20. 2020
  21. Published

    Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors

    Falk-Petersen, C. B., Tsonkov, T. M., Nielsen, M. S., Harpsøe, Kasper, Bundgaard, C., Frølund, Bente, Kristiansen, Uffe, Gloriam, David E. & Wellendorph, Petrine, 22 Jun 2020, In: Scientific Reports. 10, 1, 12 p., 10078.

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. 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

  23. 2019
  24. Published

    Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at gamma-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters

    Giraudo, A., Krall, J., Bavo, Francesco, Nielsen, Birgitte, Kongstad, Kenneth Thermann, Rolando, B., De Blasio, R., Gloriam, David E., Löffler, R., Thiesen, L., Harpsøe, Kasper, Frydenvang, Karla Andrea, Boschi, D., Wellendorph, Petrine, Lolli, M. L., Jensen, Anders A. & Frølund, Bente, 27 Jun 2019, In: Journal of Medicinal Chemistry. 62, 12, p. 5797-5809

    Research output: Contribution to journalJournal articleResearchpeer-review

  25. Published

    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 journalJournal articleResearchpeer-review

  26. Published

    Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites

    Krall, J., Bavo, Francesco, Falk-Petersen, C. B., Jensen, C. H., Nielsen, J. O., Tian, Yongsong, Anglani, V., Kongstad, Kenneth Thermann, Petersen, Louise Piilgaard, Nielsen, Birgitte, Gloriam, David E., Kehler, J., Jensen, Anders A., Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 14 Mar 2019, In: Journal of Medicinal Chemistry. 62, 5, p. 2798-2813

    Research output: Contribution to journalJournal articleResearchpeer-review

  27. 2018
  28. Published

    5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology

    Peng, Y., McCorvy, J. D., Harpsøe, K., Lansu, K., Yuan, S., Popov, P., Qu, L., Pu, M., Che, T., Nikolajsen, L. F., Huang, X., Wu, Y., Shen, L., Bjørn-Yoshimoto, W. E., Ding, K., Wacker, D., Han, G. W., Cheng, J., Katritch, V., Jensen, A. A. & 6 others, Hanson, M. A., Zhao, S., Gloriam, David E., Roth, B. L., Stevens, R. C. & Liu, Z., 2018, In: Cell. 172, 4, p. 719-730 P719-730.E14.

    Research output: Contribution to journalJournal articleResearchpeer-review

  29. Published

    GPCRdb in 2018: adding GPCR structure models and ligands

    Pándy-Szekeres, Gáspár, Munk, C., Tsonkov, T. M., Mordalski, S., Harpsøe, Kasper, Hauser, Alexander Sebastian, Bojarski, A. J. & Gloriam, David E., 2018, In: Nucleic Acids Research. 46, D1, 7 p., gkx1109.

    Research output: Contribution to journalJournal articleResearchpeer-review

  30. Published

    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 journalJournal articleResearchpeer-review

  31. 2017
  32. Published

    Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide

    Di Giglio, M. G., Muttenthaler, M., Harpsøe, Kasper, Liutkeviciute, Z., Keov, P., Eder, T., Rattei, T., Arrowsmith, S., Wray, S., Marek, A., Elbert, T., Alewood, P. F., Gloriam, David E. & Gruber, C. W., 1 Feb 2017, In: Scientific Reports. 7, 15 p., 41002.

    Research output: Contribution to journalJournal articleResearchpeer-review

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