Kasper Harpsøe
Research consultant
Biopharmaceuticals
Jagtvej 162, 2100 København Ø
- 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
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Unraveling the high- and low-sensitivity agonist responses of nicotinic acetylcholine receptors
Harpsøe, Kasper, Ahring, P. K., Christensen, J. K., Jensen, M. L., Peters, D. & Balle, T., 27 Jul 2011, In: Journal of Neuroscience. 31, 30, p. 10759-10766Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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. 891-901Research output: Contribution to journal › Journal article › Research › peer-review
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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. 847-860Research output: Contribution to journal › Journal article › Research › peer-review
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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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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
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Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites
Kaae, B. H., Harpsøe, Kasper, Kastrup, Jette Sandholm Jensen, Sanz, A. C., Pickering, Darryl S, Metzler, B., Clausen, Rasmus Prætorius, Gajhede, Michael, Sauerberg, P., Liljefors, T. & Madsen, Ulf, 2007, In: Chemistry & Biology. 14, 11, p. 1294-303 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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, Icaro 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. 469-473Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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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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
- Published
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
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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-conotoxin analogues targeting a7 nicotinic acetylcholine receptors: Improved antagonistic activity by incorporation of proline derivatives
Armishaw, C., Jensen, Anders A., Balle, T., Clark, R. J., Harpsøe, Kasper, Skonberg, C., Liljefors, T. & Strømgaard, Kristian, 2009, In: Journal of Biological Chemistry. 284, 14, p. 9498-9512Research 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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Prediction of the binding mode of biarylpropylsulfonamide allosteric AMPA receptor modulators based on docking, GRID molecular interaction fields and 3D-QSAR analysis
Harpsøe, Kasper, Liljefors, T. & Balle, T., 2008, In: Journal of Molecular Graphics and Modelling. 26, 5, p. 874-883Research 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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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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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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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 journal › Conference abstract in journal › Research › peer-review
- Published
Nyt bindingssted i nikotine acetylcholinreceptorer: håb om ny behandling af eksempelvis ADHD og Alzheimers sygdom
Harpsøe, Kasper & Balle, T., Feb 2012, In: BestPractice Psykiatri/Neurologi. 5, 16, p. 7-10 4 p.Research output: Contribution to journal › Journal article › Communication
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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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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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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. 210-213Research output: Contribution to journal › Letter › 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
Published -
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
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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