Kasper Harpsøe
Research consultant
Biopharmaceuticals
Jagtvej 162, 2100 København Ø
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Covalent Trapping of Methyllycaconitine at the α4-α4 Interface of the α4β2 Nicotinic Acetylcholine Receptor: ANTAGONIST BINDING SITE AND MODE OF RECEPTOR INHIBITION REVEALED
Absalom, N. L., Quek, G., Lewis, T. M., Qudah, T., von Arenstorff, I., Ambrus, J. I., Harpsøe, Kasper, Karim, N., Balle, T., McLeod, M. D. & Chebib, M., 13 Sep 2013, In: The Journal of Biological Chemistry. 288, 37, p. 26521-32 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Covalent attachment of antagonists to the a7 nicotinic acetylcholine receptor: synthesis and reactivity of substituted maleimides
Ambrus, J. I., Halliday, J. I., Kanizaj, N., Absalom, N., Harpsøe, Kasper, Balle, T., Chebib, M. & McLeod, M. D., 7 Jul 2012, In: Chemical Communications. 48, 53, p. 6699-6701 3 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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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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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. 3045-3057Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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. 531–535Research output: Contribution to journal › Comment/debate › Research › peer-review
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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
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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 journal › Journal article › Research › peer-review
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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. 46-56Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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. 5797-5809Research 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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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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Identification of a putative binding site for 5-alkyl-benzothiadiazides in the AMPA receptor dimer interface
Harpsøe, Kasper, Varming, T., Gouliaev, A. H., Peters, D. & Liljefors, T., 2007, In: Journal of Molecular Graphics and Modelling. 26, 1, p. 213-225 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors
Harpsøe, Kasper, Hald, H., Timmermann, D. B., Jensen, M. L., Dyhring, T., Nielsen, E. Ø., Peters, D., Balle, T., Gajhede, Michael, Kastrup, Jette Sandholm Jensen & Ahring, P. K., 25 Jan 2013, In: Journal of Biological Chemistry. 288, 4, p. 2559-2570 12 p.Research 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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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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GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors
Huang, S., Xu, P., Shen, D., Simon, Icaro 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 journal › Journal article › Research › peer-review
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GPCRdb: an information system for G protein-coupled receptors
Isberg, V., Mordalski, S., Munk, C., Rataj, K., Harpsøe, Kasper, Hauser, Alexander Sebastian, Vroling, B., Bojarski, A. J., Vriend, G. & Gloriam, David E., 4 Jan 2016, In: Nucleic Acids Research. 44, D1, p. D356-64Research 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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Design and characterization of dimeric ligands cross-linking two identical modulatory AMPA receptor sites
Kaae, B. H., Harpsøe, Kasper, Sanz, A. C., Pickering, Darryl S, Sauerberg, P., Clausen, Rasmus Prætorius, Kastrup, Jette Sandholm Jensen, Liljefors, T. & Madsen, Ulf, 19 Aug 2007, In: American Chemical Society. Abstracts of Papers (at the National Meeting). 234Research output: Contribution to journal › Conference abstract in journal › Research
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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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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
- Published
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
ID: 1428429
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465
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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 -
319
downloads
GPCRdb: an information system for G protein-coupled receptors
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
280
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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