Kasper Harpsøe
Senior Advisor
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
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
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 : The Journal of Biological Chemistry. 295, p. 13850-13861Research 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
GPCRdb in 2018: adding GPCR structure models and ligands
Pándy-Szekeres, G., Munk, Christian, Tsonkov, T. M., Mordalski, S., Harpsøe, Kasper, Hauser, Alexander Sebastian, Bojarski, A. J. & Gloriam, David E., 2018, In : Nucleic Acids Research. 46, D1, 7 p., gkx1109.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, Christian, Bräuner-Osborne, 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
- Published
GPCRdb: an information system for G protein-coupled receptors
Isberg, V., Mordalski, S., Munk, Christian, 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
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
-
242
downloads
GPCRdb: an information system for G protein-coupled receptors
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
216
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 -
151
downloads
GPCRdb in 2018: adding GPCR structure models and ligands
Research output: Contribution to journal › Journal article › Research › peer-review
Published