Kasper Harpsøe
Research consultant
Biopharmaceuticals
Jagtvej 162, 2100 København Ø
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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. 2798-2813Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs
Krall, J., Jensen, C. H., Bavo, F., Falk-Petersen, C. B., Haugaard, A. S., Vogensen, S. B., Tian, Y., Nittegaard-Nielsen, M., Sigurdardóttir, S. B., Kehler, J., Kongstad, Kenneth Thermann, Gloriam, David E., Clausen, Rasmus Prætorius, Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 9022-9039 18 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain
Krintel, C., Harpsøe, Kasper, Zachariassen, L. G., Peters, D., Frydenvang, Karla Andrea, Pickering, Darryl S, Gajhede, Michael & Kastrup, Jette Sandholm Jensen, 2013, In: Acta Crystallographica Section D: Structural Biology. 69, Pt 9, p. 1645-1652 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Revision of the Classical Dopamine D2 Agonist Pharmacophore Based on an Integrated Medicinal Chemistry, Homology Modelling and Computational Docking Approach
Krogsgaard-Larsen, N., Harpsøe, Kasper, Kehler, J., Christoffersen, C. T., Brøsen, P. & Balle, T., 24 Jul 2014, In: Neurochemical Research. 39, 10, p. 1997-2007 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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. 5747-5758Research output: Contribution to journal › Journal article › Research › peer-review
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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. 319–325Research output: Contribution to journal › Journal article › Research › peer-review
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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
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GPCRdb: The G protein-coupled receptor database - an introduction
Munk, C., Isberg, V., Mordalski, S., Harpsøe, Kasper, Rataj, K., Hauser, Alexander Sebastian, Kolb, P., Bojarski, A. J., Vriend, G. & Gloriam, David E., Jul 2016, In: British Journal of Pharmacology. 173, 14, p. 2195-207 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Integrating structural and mutagenesis data to elucidate GPCR ligand binding
Munk, C., Harpsøe, Kasper, Hauser, Alexander Sebastian, Isberg, V. & Gloriam, David E., Oct 2016, In: Current Opinion in Pharmacology. 30, p. 51-58 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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
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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 journal › Journal article › Research › peer-review
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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
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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, , 2018, In: Cell. 172, 4, p. 719-730 P719-730.E14.Research output: Contribution to journal › Journal article › Research › peer-review
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Novel quinoxaline derivatives and their medical use
Peters, D., Christensen, J. K., Harpsøe, Kasper & Liljefors, T., 2007, Patent No. WO/2007/060144, 31 May 2007Research output: Patent
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Pharmacological characterisation of biarylisopropylalsulphonamide AMPA-R potentiators
Pickering, Darryl S, Sanz, C., Harpsøe, Kasper, Clausen, Rasmus Prætorius, Sauerberg, P., Liljefors, T., Madsen, Ulf & Kaae, B. H., 2007, In: Journal of Neurochemistry. 102 (suppl. 1), 41Research output: Contribution to journal › Conference abstract in journal › Research
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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, Icaro A, 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. 2727–2742Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT2A Receptor Agonists
Poulie, Christian Bernard Matthijs, Pottie, E., Simon, Icaro 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. 12031–12043Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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A robust force field based method for calculating conformational energies of charged drug-like molecules
Pøhlsgaard, J., Harpsøe, Kasper, Jørgensen, Flemming Steen & Olsen, L., 2012, In: Journal of Chemical Information and Modeling. 52, 2, p. 409-419Research output: Contribution to journal › Journal article › Research › peer-review
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Crystal structure of the acetylcholine binding protein (AChBP) from Lymnaea stagnalis in complex with NS3950 (1-(6-bromo-5-ethoxypyridin-3-yl)-1,4-diazepane)
Rohde, L. A. H., Ahring, P. K., Jensen, M. L., Nielsen, E. O., Peters, D., Helgstrand, C., Krintel, C., Harpsøe, Kasper, Gajhede, Michael, Kastrup, Jette Sandholm Jensen & Balle, T., 14 Dec 2011Research output: Other contribution › Research
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Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine alpha4beta2 receptors: Unique role of halogen bonding revealed
Rohde, L. A. H., Ahring, P. K., Jensen, M. L., Nielsen, E. Ø., Peters, D., Helgstrand, C., Krintel, C., Harpsøe, Kasper, Gajhede, Michael, Kastrup, Jette Sandholm Jensen & Balle, T., 3 Feb 2012, In: The Journal of Biological Chemistry. 287, 6, p. 4248-4259Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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
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Ligand selectivity hotspots in serotonin GPCRs
Simon, Icaro A, Bjørn-Yoshimoto, Walden, Harpsøe, Kasper, Iliadis, S., Svensson, B., Jensen, Anders A. & Gloriam, David E., 2023, In: Trends in Pharmacological Sciences. 44, 12, p. 978-990Research output: Contribution to journal › Review › Research › peer-review
ID: 1428429
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Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide
Research output: Contribution to journal › Journal article › Research › peer-review
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318
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GPCRdb: an information system for G protein-coupled receptors
Research output: Contribution to journal › Journal article › Research › peer-review
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279
downloads
Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139
Research output: Contribution to journal › Journal article › Research › peer-review
Published