Kasper Harpsøe

Search results

• 2023

  A community Biased Signaling Atlas

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

  Research output: Contribution to journal › Journal article › Research › peer-review
  13 Citations (Scopus)

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

  Bartling, C. R. O., Alexopoulou, F., Kuschert, S., Chin, Y. K. Y., Jia, X., Sereikaite, V., Özcelik, D., Jensen, T. M., Jain, P., Nygaard, M. M., Harpsøe, K., Gloriam, D. E., Mobli, M. & Strømgaard, K., 2023, In: Journal of Medicinal Chemistry. 66, 4, p. 3045-3057

  Research output: Contribution to journal › Journal article › Research › peer-review
  3 Citations (Scopus)

• Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT_2A Receptor Agonist

  Marcher-Rørsted, E., Nykodemová, J., Harpsøe, K., Jensen, A. A. & Kristensen, J. L., 2023, In: ACS Medicinal Chemistry Letters. 14, 3, p. 319–325

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• Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139

  Pallareti, L., Rath, T. F., Trapkov, B., Tsonkov, T., Nielsen, A. T., Harpsøe, K., Gentry, P. R., Bräuner-Osborne, H., Gloriam, D. E. & Foster, S. R., 2023, In: European Journal of Pharmacology. 943, 175553.

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  3 Citations (Scopus)

  33 Downloads (Pure)

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

  Pottie, E., Poulie, C. B. M., Simon, I. A., Harpsøe, K., D’Andrea, L., Komarov, I. V., Gloriam, D. E., Jensen, A. A., Kristensen, J. L. & Stove, C. P., 2023, In: ACS Chemical Neuroscience. 14, 15, p. 2727–2742

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  6 Citations (Scopus)

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• 2022

  Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT_2A Receptor Agonists

  Poulie, C. B. M., Pottie, E., Simon, I. A., Harpsøe, K., D'Andrea, L., Komarov, I. V., Gloriam, D. E., Jensen, A. A., Stove, C. P. & Kristensen, J. L., 2022, In: Journal of Medicinal Chemistry. 65, 18, p. 12031–12043

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  11 Citations (Scopus)

  51 Downloads (Pure)

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

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

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  63 Citations (Scopus)

  13 Downloads (Pure)

• Ligand-directed bias of G protein signaling at the dopamine D₂ receptor

  Von Moo, E., Harpsøe, K., Hauser, A. S., Masuho, I., Bräuner-Osborne, H., Gloriam, D. E. & Martemyanov, K. A., 2022, In: Cell Chemical Biology. 29, 2, p. 226-238

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  20 Citations (Scopus)
• 2021

  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, K., Gloriam, D. E., Aoki, K. & Takeuchi, T., 2021, In: Molecular Brain. 14, 1, 14 p., 173.

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  17 Citations (Scopus)

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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, K., Gloriam, D. E., Frølund, B. & Wellendorph, P., 2021, In: Molecular Pharmacology. 100, 1, p. 46-56

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  3 Citations (Scopus)

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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, K., Buchleithner, S., Conforti, I., Jung, S., Gloriam, D. E., Schirmeister, T., Wellendorph, P. & Frølund, B., 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
  7 Citations (Scopus)

• 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-D., Yen, H-Y., Robinson, C. V., Harpsøe, K., Svensson, B., Guo, J., Jiang, H., Gloriam, D. E., Melcher, K., Jiang, Y., Zhang, Y. & Xu, H. E., 2021, In: Nature. 592, p. 469-473

  Research output: Contribution to journal › Journal article › Research › peer-review
  166 Citations (Scopus)

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

  Bartling, C. R. O., Jensen, T. M. T., Henry, S. M., Colliander, A. L., Sereikaite, V., Wenzler, M., Jain, P., Maric, H. M., Harpsøe, K., Pedersen, S. W., Clemmensen, L. S., Haugaard-Kedström, L. M., Gloriam, D. E., Ho, A. & Strømgaard, K., 2021, In: Journal of the American Chemical Society. 143, 2, p. 891-901

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  17 Citations (Scopus)

  40 Downloads (Pure)
• 2020

  Delineation of molecular determinants for FR900359 inhibition of G_q/11 unlocks inhibition of Gα_s

  Boesgaard, M. W., Harpsøe, K., Malmberg, M., Underwood, C. R., Inoue, A., Mathiesen, J. M., König, G. M., Kostenis, E., Gloriam, D. E. & Bräuner-Osborne, H., 2020, In: Journal of Biological Chemistry. 295, 40, p. 13850-13861

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  14 Citations (Scopus)

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

  Falk-Petersen, C. B., Tsonkov, T. M., Nielsen, M. S., Harpsøe, K., Bundgaard, C., Frølund, B., Kristiansen, U., Gloriam, D. E. & Wellendorph, P., 22 Jun 2020, In: Scientific Reports. 10, 1, 12 p., 10078.

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  11 Citations (Scopus)

  206 Downloads (Pure)
• 2019

  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, F., Falk-Petersen, C. B., Jensen, C. H., Nielsen, J. O., Tian, Y., Anglani, V., Kongstad, K. T., Piilgaard, L., Nielsen, B., Gloriam, D. E., Kehler, J., Jensen, A. A., Harpsøe, K., Wellendorph, P. & Frølund, B., 14 Mar 2019, In: Journal of Medicinal Chemistry. 62, 5, p. 2798-2813

  Research output: Contribution to journal › Journal article › Research › peer-review
  14 Citations (Scopus)

• 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, F., Nielsen, B., Kongstad, K. T., Rolando, B., De Blasio, R., Gloriam, D. E., Löffler, R., Thiesen, L., Harpsøe, K., Frydenvang, K., Boschi, D., Wellendorph, P., Lolli, M. L., Jensen, A. A. & Frølund, B., 27 Jun 2019, In: Journal of Medicinal Chemistry. 62, 12, p. 5797-5809

  Research output: Contribution to journal › Journal article › Research › peer-review
  20 Citations (Scopus)

• Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

  Malfacini, D., Patt, J., Annala, S., Harpsøe, K., Eryilmaz, F., Reher, R., Crüsemann, M., Hanke, W., Zhang, H., Tietze, D., Gloriam, D. E., Bräuner-Osborne, H., Strømgaard, K., König, G. M., Inoue, A., Gomeza, J. & Kostenis, E., 12 Apr 2019, In: The Journal of Biological Chemistry. 294, 15, p. 5747-5758

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  31 Citations (Scopus)

  137 Downloads (Pure)
• 2018

  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, D. E., Roth, B. L., Stevens, R. C. & Liu, Z., 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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  177 Citations (Scopus)

• GPCRdb in 2018: adding GPCR structure models and ligands

  Pándy-Szekeres, G., Munk, C., Tsonkov, T. M., Mordalski, S., Harpsøe, K., Hauser, A. S., Bojarski, A. J. & Gloriam, D. E., 2018, In: Nucleic Acids Research. 46, D1, 7 p., gkx1109.

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  386 Citations (Scopus)

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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, K., Daly, N. L., Xiong, X., Underwood, C. R., Haugaard-kedström, L. M., Bräuner-osborne, H., Gloriam, D. E. & Strømgaard, K., 2018, In: European Journal of Medicinal Chemistry. 156, p. 847-860

  Research output: Contribution to journal › Journal article › Research › peer-review
  27 Citations (Scopus)
• 2017

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

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

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  34 Citations (Scopus)

  975 Downloads (Pure)

• 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, K. T., Gloriam, D. E., Clausen, R. P., Harpsøe, K., Wellendorph, P. & Frølund, B., 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 9022-9039 18 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  22 Citations (Scopus)

• Structural insight to mutation effects uncover a common allosteric site in class C GPCRs

  Harpsøe, K., Boesgaard, M. W., Munk, C., Bräuner-Osborne, H. & Gloriam, D. E., 2017, In: Bioinformatics (Oxford, England). 33, 8, p. 1116-1120 5 p., btw784.

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  11 Citations (Scopus)

  222 Downloads (Pure)
• 2016

  GPCRdb: an information system for G protein-coupled receptors

  Isberg, V., Mordalski, S., Munk, C., Rataj, K., Harpsøe, K., Hauser, A. S., Vroling, B., Bojarski, A. J., Vriend, G. & Gloriam, D. E., 4 Jan 2016, In: Nucleic Acids Research. 44, D1, p. D356-64

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  232 Citations (Scopus)

  436 Downloads (Pure)

• GPCRdb: The G protein-coupled receptor database - an introduction

  Munk, C., Isberg, V., Mordalski, S., Harpsøe, K., Rataj, K., Hauser, A. S., Kolb, P., Bojarski, A. J., Vriend, G. & Gloriam, D. 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
  155 Citations (Scopus)

• Integrating structural and mutagenesis data to elucidate GPCR ligand binding

  Munk, C., Harpsøe, K., Hauser, A. S., Isberg, V. & Gloriam, D. E., Oct 2016, In: Current Opinion in Pharmacology. 30, p. 51-58 8 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  46 Citations (Scopus)

• 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, K., Björkling, F., Bräuner-Osborne, H. & Gloriam, D. E., 10 Nov 2016, In: Scientific Reports. 6, p. 1-13 13 p., 36681.

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  20 Citations (Scopus)

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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, K., Gardella, T. J., Wöldike, M. F., Mannstadt, M., Gloriam, D. E., Bräuner-osborne, H. & Strømgaard, K., 2016, In: Nature Chemistry. 8, 11, p. 1035-1041 7 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  63 Citations (Scopus)
• 2015

  Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors - A Structural Perspective of Ligands and Mutants

  Harpsøe, K., Isberg, V., Tehan, B. G., Weiss, D., Arsova, A., Marshall, F. H., Bräuner-Osborne, H. & Gloriam, D. 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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  37 Citations (Scopus)
• 2014

  mGluR5: Exploration of Orthosteric and Allosteric Ligand Binding Pockets and Their Applications to Drug Discovery

  Mølck, C., Harpsøe, K., Gloriam, D. E., Mathiesen, J. M., Nielsen, S. M. & Bräuner-Osborne, H., Oct 2014, In: Neurochemical Research. 39, 10, p. 1862-1875 14 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  28 Citations (Scopus)

• Revision of the Classical Dopamine D2 Agonist Pharmacophore Based on an Integrated Medicinal Chemistry, Homology Modelling and Computational Docking Approach

  Krogsgaard-Larsen, N., Harpsøe, K., 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
  2 Citations (Scopus)
• 2013

  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, K., 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
  15 Citations (Scopus)

• Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors

  Harpsøe, K., Hald, H., Timmermann, D. B., Jensen, M. L., Dyhring, T., Nielsen, E. Ø., Peters, D., Balle, T., Gajhede, M., Kastrup, J. S. J. & 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
  26 Citations (Scopus)

• Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain

  Krintel, C., Harpsøe, K., Zachariassen, L. G., Peters, D., Frydenvang, K., Pickering, D. S., Gajhede, M. & Kastrup, J. S., 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
  15 Citations (Scopus)
• 2012

  A robust force field based method for calculating conformational energies of charged drug-like molecules

  Pøhlsgaard, J., Harpsøe, K., Jørgensen, F. S. & Olsen, L., 2012, In: Journal of Chemical Information and Modeling. 52, 2, p. 409-419

  Research output: Contribution to journal › Journal article › Research › peer-review
  5 Citations (Scopus)

• 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, K., 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
  11 Citations (Scopus)

• 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, K., Thygesen, S. B., Rahr, L. M., Ahring, P. K., Balle, T. & Jensen, A. A., 2012, In: Journal of Biological Chemistry. 287, 30, p. 25241-25254

  Research output: Contribution to journal › Journal article › Research › peer-review
  28 Citations (Scopus)

• 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, K., Gajhede, M., Kastrup, J. S. & Balle, T., 3 Feb 2012, In: The Journal of Biological Chemistry. 287, 6, p. 4248-4259

  Research output: Contribution to journal › Journal article › Research › peer-review
  41 Citations (Scopus)

• Nyt bindingssted i nikotine acetylcholinreceptorer: håb om ny behandling af eksempelvis ADHD og Alzheimers sygdom

  Translated title of the contribution: New binding site in the nicotinic acetylcholine receptors: hope for new treatment of e.g. ADHD and Alzheimer's diseaseHarpsøe, K. & 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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• 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, K., Gloriam, D. E., Clausen, R. P., Madsen, U., Pedersen, L., Jimenez, H. N., Nielsen, S. M., Mathiesen, J. M. & Bräuner-Osborne, H., 2012, In: Molecular Pharmacology. 82, 5, p. 929-37 9 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  32 Citations (Scopus)

• Structure-activity relationships for negative allosteric mGluR5 modulators

  Kaae, B. H., Harpsøe, K., Kvist, T., Mathiesen, J. M., Mølck, C., Gloriam, D. E., Jimenez, H. N., Uberti, M. A., Nielsen, S. M., Nielsen, B., Bräuner-Osborne, H., Sauerberg, P., Clausen, R. P. & Madsen, U., 2012, In: ChemMedChem. 7, 3, p. 440-451

  Research output: Contribution to journal › Journal article › Research › peer-review
  15 Citations (Scopus)
• 2011

  Unraveling the high- and low-sensitivity agonist responses of nicotinic acetylcholine receptors

  Harpsøe, K., Ahring, P. K., Christensen, J. K., Jensen, M. L., Peters, D. & Balle, T., 27 Jul 2011, In: Journal of Neuroscience. 31, 30, p. 10759-10766

  Research output: Contribution to journal › Journal article › Research › peer-review
  119 Citations (Scopus)
• 2009

  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, K., Liljefors, T. & Balle, T., 2009, In: Journal of Medicinal Chemistry. 52, 8, p. 2311-2316

  Research output: Contribution to journal › Journal article › Research › peer-review
  14 Citations (Scopus)

• Rational design of a-conotoxin analogues targeting a7 nicotinic acetylcholine receptors: Improved antagonistic activity by incorporation of proline derivatives

  Armishaw, C., Jensen, A. A., Balle, T., Clark, R. J., Harpsøe, K., Skonberg, C., Liljefors, T. & Strømgaard, K., 2009, In: Journal of Biological Chemistry. 284, 14, p. 9498-9512

  Research output: Contribution to journal › Journal article › Research › peer-review
  52 Citations (Scopus)
• 2008

  Computeren viser vejen til et nyt potentielt lægemiddel

  Harpsøe, K., Kaae, B. H., Balle, T., Pickering, D. S. & Kastrup, J. S. J., 2008, In: Lægemiddelforskning. p. 28-30

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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, K., Liljefors, T. & Balle, T., 2008, In: Journal of Molecular Graphics and Modelling. 26, 5, p. 874-883

  Research output: Contribution to journal › Journal article › Research › peer-review
  14 Citations (Scopus)
• 2007

  Identification of a putative binding site for 5-alkyl-benzothiadiazides in the AMPA receptor dimer interface

  Harpsøe, K., 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
  12 Citations (Scopus)

• Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites

  Kaae, B. H., Harpsøe, K., Kastrup, J. S. J., Sanz, A. C., Pickering, D. S., Metzler, B., Clausen, R. P., Gajhede, M., Sauerberg, P., Liljefors, T. & Madsen, U., 2007, In: Chemistry & Biology. 14, 11, p. 1294-303 10 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  55 Citations (Scopus)