Kasper Harpsøe
Research consultant
Biopharmaceuticals
Jagtvej 162, 2100 København Ø
- 2017
- 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
- Published
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
- 2016
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2015
- 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
- 2014
- 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
- Published
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
- 2013
- Published
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
- Published
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
- Published
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
- 2012
- Published
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
- Published
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
- 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
- Published
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
- Published
Discovery of a novel allosteric modulator of 5-HT3 receptor: Inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site
Trattnig, S. M., Harpsøe, Kasper, Thygesen, S. B., Rahr, L. M., Ahring, P. K., Balle, T. & Jensen, Anders A., 2012, In: Journal of Biological Chemistry. 287, 30, p. 25241-25254Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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. 440-451Research output: Contribution to journal › Journal article › Research › peer-review
- 2011
- Published
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
- 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. 43-43Research output: Contribution to journal › Conference abstract in journal › Research
- Published
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
- 2009
- Published
Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4ß2 nicotinic ligands
Tosco, P., Ahring, P. K., Dyhring, T., Peters, D., Harpsøe, Kasper, Liljefors, T. & Balle, T., 2009, In: Journal of Medicinal Chemistry. 52, 8, p. 2311-2316Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
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
Published -
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