Kasper Harpsøe
Research consultant
Peptides and Proteins
Jagtvej 162, 2100 København Ø
I have worked within computational medicinal chemistry since I started my PhD in 2003 and have extensive experience with most molecular modeling techniques. Since 2014, I have been part of the Gloriam Group (gloriamgroup.org), which has G Protein-Coupled Receptors (GPCRs) as the main research focus. My role in the group is project manager for our activities within computatoional drug design of small molecule and peptide ligands. Most of our work are in multidisciplinary drug discovery projects in close collaboration with medicinal chemists, molecular pharmacologist, structural biologists and data scientists from both academia and industry. Our focus is mainly on biased signalling (fuctional selectivity) of GPCRs, design of inhibitors of protein-protein interactions in intracellular signalling and orthosteric GPCR ligands. In recent years, our focus has changed from traditional small molecule ligands to peptides.
Additionally, we host the GPCRdb (gpcrdb.org), which contains reference data, interactive visualisation and experiment design tools for GPCRs. GPCRdb curates sequence alignments, structures and receptor mutations from literature and we provide, among other things, interactive diagrams that visualise receptor residues (e.g. snakeplot and helix box plot) and relationships (e.g phylogenetic trees).
Selected publications
- Published
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, Patrick Ryan, Liu, K., Larionova, M., Liu, J., Chen, N., Bräuner-Osborne, 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
- Published
Ligand-directed bias of G protein signaling at the dopamine D2 receptor
Moo, Ee Von, Harpsøe, Kasper, Hauser, Alexander Sebastian, Masuho, I., Bräuner-Osborne, Hans, Gloriam, David E. & Martemyanov, K. A., 2022, In: Cell Chemical Biology. 29, 2, p. 226-238Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors
Falk-Petersen, C. B., Rostrup, Frederik, 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
- Published
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 Ariel, 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
- Published
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-Osborne, Hans, 2020, In: Journal of Biological Chemistry. 295, 40, p. 13850-13861Research output: Contribution to journal › Journal article › Research › peer-review
- Published
5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology
Peng, Y., McCorvy, J. D., Harpsøe, Kasper, Lansu, K., Yuan, S., Popov, P., Qu, L., Pu, M., Che, T., Nikolajsen, L. F., Huang, X., Wu, Y., Shen, L., Bjørn-Yoshimoto, Walden, Ding, K., Wacker, D., Han, G. W., Cheng, J., Katritch, V., Jensen, Anders A., Hanson, M. A., Zhao, S., Gloriam, David 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
- 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-Osborne, Hans & Strømgaard, Kristian, 2016, In: Nature Chemistry. 8, 11, p. 1035-1041 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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-Osborne, 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
- 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
ID: 1428429
Most downloads
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186
downloads
GPCRdb: an information system for G protein-coupled receptors
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
182
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 -
132
downloads
GPCRdb in 2018: adding GPCR structure models and ligands
Research output: Contribution to journal › Journal article › Research › peer-review
Published