Thomas Michael Frimurer
Associate Professor
Platforms
Blegdamsvej 3B, Mærsk Tårnet, 6-7-8. sal, 2200 København N.
Member of:
Introductory remarks on publicationslist
Publications: Author or co-author on > 40 papers in peer-reviewed, medium to high profile scientific journals. Involved in innovation and commercialization activities. Patents: Author or co-author on > 15 patents on chemical leads and drug candidates for the treatment of obesity, type-2 diabetes, asthma inflammation and pain. Most recently (Mar. 2014) we patented a strong chemical package on oral available small molecule GPR39 agonists – a potential obesity and type-2 diabetes target. Invited talks: Participated in multiple oral presentations at international and national scientific meetings.
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Human substance P receptor binding mode of the antagonist drug aprepitant by NMR and crystallography
Chen, S., Lu, M., Liu, D., Yang, L., Yi, C., Ma, L., Zhang, H., Liu, Q., Frimurer, Thomas Michael, Wang, M., Schwartz, Thue W., Stevens, R. C., Wu, B., Wuthrich, K. & Zhao, Q., 2019, In: Nature Communications. 10, 8 p., 638.Research output: Contribution to journal › Journal article › Research › peer-review
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In Silico Investigation of the Neurotensin Receptor 1 Binding Site: Overlapping Binding Modes for Small Molecule Antagonists and the Endogenous Peptide Agonist
Lückmann, Michael, Holst, Birgitte, Schwartz, Thue W. & Frimurer, Thomas Michael, 2016, In: Molecular Informatics. 35, p. 19-24 6 p.Research output: Contribution to journal › Letter › Research › peer-review
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Inhibiting RHOA Signaling in Mice Increases Glucose Tolerance and Numbers of Enteroendocrine and Other Secretory Cells in the Intestine
Petersen, N., Frimurer, Thomas Michael, Pedersen, M. T., Egerod, Kristoffer Lihme, Albrechtsen, Nicolai Jacob Wewer, Holst, Jens Juul, Grapin-Botton, A., Jensen, Kim Bak & Schwartz, Thue W., 2018, In: Gastroenterology. 155, 4, p. 1164-1176 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Investigating GIPR (ant)agonism: A structural analysis of GIP and its receptor
Smit, F. X., van der Velden, W. J. C., Kizilkaya, Hüsün Sheyma, Nørskov, A., Lückmann, Michael, Hansen, T. N., wbf943, wbf943, Qvotrup, K., Frimurer, Thomas Michael & Rosenkilde, Mette, 2021, In: Structure. 29, 7, p. 679-693.e6 21 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Ligand-selective small molecule modulators of the constitutively active vGPCR US28
Amarandi, R., Lückmann, Michael, Melynis, M., Jakobsen, M. H., Fallah, Z., Spiess, Katja, Hjortø, Gertrud Malene, Pui, A., Frimurer, Thomas Michael & Rosenkilde, Mette, 2018, In: European Journal of Medicinal Chemistry. 155, p. 244-254Research output: Contribution to journal › Journal article › Research › peer-review
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Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
Madsen, J. J., Ye, L., Frimurer, Thomas Michael & Olsen, O. H., 2022, In: Protein Science. 31, 11, 16 p., e4456.Research output: Contribution to journal › Journal article › Research › peer-review
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Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?
Högberg, T., Frimurer, Thomas Michael & Sasmal, P. K., 1 Oct 2012, In: Bioorganic & Medicinal Chemistry Letters. 22, 19, p. 6039-6047 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions.
Frimurer, Thomas Michael, Mende, F., Graae, A., Engelstoft, M. S., Egerod, Kristoffer Lihme, Nygaard, R., Gerlach, L., Hansen, J. B., Schwartz, Thue W. & Holst, Birgitte, 2017, In: Journal of Medicinal Chemistry. 60, 3, p. 886-898 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors
Thiele, S., Malmgaard-Clausen, M., Engel-Andreasen, J., Steen, A., Rummel, P. C., Nielsen, M. C., Gloriam, David E., Frimurer, Thomas Michael, Ulven, Trond & Rosenkilde, Mette, 27 Sep 2012, In: Journal of Medicinal Chemistry. 55, 18, p. 8164-77 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Modulation of constitutive activity and signaling bias of the ghrelin receptor by conformational constraint in the second extracellular loop
Mokrosinski, J., Frimurer, Thomas Michael, Sivertsen, B., Schwartz, Thue W. & Holst, Birgitte, Sep 2012, In: Journal of Biological Chemistry. 287, p. 33488-33502 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular Mechanism of Action for Allosteric Modulators and Agonists in CC-chemokine Receptor 5 (CCR5)
Karlshøj, S., Amarandi, R. M., Larsen, Olav, Daugvilaite, V., Steen, A., Brvar, M., Pui, A., Frimurer, Thomas Michael, Ulven, Trond & Rosenkilde, Mette, 23 Dec 2016, In: Journal of Biological Chemistry. 291, 52, p. 26860-26874Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183)
Benned-Jensen, T., Norn, C., Laurent, S., Madsen, C. M., Larsen, H. M., Arfelt, K. N., Wolf, R. M., Frimurer, Thomas Michael, Sailer, A. W. & Rosenkilde, Mette, 12 Oct 2012, In: The Journal of Biological Chemistry. 287, 42, p. 35470-83 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular dynamics-based identification of binding pathways and two distinct high-affinity sites for succinate in succinate receptor 1/GPR91
Iliyaz, Aslihan Shenol, Lückmann, Michael, Trauelsen, Mette, Lambrughi, M., Tiberti, M., Papaleo, E., Frimurer, Thomas Michael & Schwartz, Thue W., 2024, In: Molecular Cell. 84, 5, p. 955-966.e4 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1
Lückmann, Michael, Trauelsen, Mette, Bentsen, M. A., Nissen, T. A. D., Martins, J., Fallah, Z., Nygaard, M. M., Papaleo, E., Lindorff-Larsen, Kresten, Schwartz, Thue W. & Frimurer, Thomas Michael, 2 Apr 2019, In: Proceedings of the National Academy of Sciences of the United States of America. 116, 14, p. 7123-7128Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular mechanism of ligand binding pathways and activation of the succinate receptor
Iliyaz, Aslihan Shenol, Lückmann, Michael, Trauelsen, Mette, Frimurer, Thomas Michael & Schwartz, Thue W., 2021, In: European Biophysics Journal. 50, Suppl. 1, p. 160 1 p., P-234.Research output: Contribution to journal › Conference abstract in journal › Research
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Mutation-Guided Unbiased Modeling of the Fat Sensor GPR119 for High-Yield Agonist Screening.
Norn, C., Pedersen, M. H., Engelstoft, M. S., Kim, S. H., Lehmann, J., Jones, R. M., Schwartz, Thue W. & Frimurer, Thomas Michael, 2015, In: Structure. 23, 12, p. 2377-2386 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits
Ulven, Trond, Receveur, J., Grimstrup, M., Rist, Ø., Frimurer, Thomas Michael, Gerlach, L., Mathiesen, Jesper M., Kostenis, E., Uller, L. & Högberg, T., 2006, In: Journal of Medicinal Chemistry. 49, 23, p. 6638-6641 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1
Rist, O., Grimstrup, M., Receveur, J., Frimurer, Thomas Michael, Ulven, Trond, Kostenis, E. & Högberg, T., 4 Dec 2009, In: Bioorganic & Medicinal Chemistry Letters. 20, 3, p. 1177-1180 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2
Grimstrup, M., Rist, Ø., Receveur, J., Frimurer, Thomas Michael, Ulven, Trond, Mathiesen, Jesper M., Kostenis, E. & Högberg, T., 1 Feb 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 3, p. 1181-1185 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists
Sasmal, P. K., Krishna, C. V., Sudheerkumar Adabala, S., Rawoof, K. A., Thadi, A., Sukumar, K. P., Cheera, S., Abbineni, C., Rao, K. V. L. N., Prasanthi, A., Nijhawan, K., Jaleel, M., Ramachandran Iyer, L., Chaitanya, T. K., Tiwari, N. K., Krishna, N. L., Potluri, V., Khanna, I., Frimurer, T. M., Lückmann, M. & 3 others, , 15 Feb 2015, In: Bioorganic & Medicinal Chemistry Letters. 25, 4, p. 887-92 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Optimization of First-in-Class Dual-Acting FFAR1/FFAR4 Allosteric Modulators with Novel Mode of Action
Lückmann, Michael, Iliyaz, Aslihan Shenol, Nissen, T. A. D., Petersen, Jacob Emil, Kouvchinov, David, Schwartz, Thue W. & Frimurer, Thomas Michael, 2022, In: ACS Medicinal Chemistry Letters. 13, 12, p. 1839-1847Research output: Contribution to journal › Journal article › Research › peer-review
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PheVI:09 (Phe6.44) as a sliding microswitch in seven-transmembrane (7TM) G protein-coupled receptor activation
Valentin-Hansen, L., Holst, Birgitte, Frimurer, Thomas Michael, Schwartz, Thue W. & Hansen, L. V., 21 Dec 2012, In: Journal of Biological Chemistry. 287, 52, p. 43516-43526 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Phenoxyacetic acid derivatives as CRTH2 receptor ligands, their preparation, pharmaceutical compositions, and use in therapy
Ulven, Trond, Frimurer, Thomas Michael, Rist, Ø., Kostenis, E., Högberg, T., Receveur, J. & Grimstrup, M., 2007, Patent No. WO 2007/062678 A1Research output: Patent
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Preassociation between the 5-HT7 serotonin receptor and G protein Gs: molecular determinants and association with low potency activation of adenylyl cyclase
Ulsund, A. H., Dahl, M., Frimurer, Thomas Michael, Manfra, O., Schwartz, Thue W., Levy, F. O. & Andressen, K. W., 2019, In: FASEB Journal. 33, 3, p. 3870-3886Research output: Contribution to journal › Journal article › Research › peer-review
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Preparation of phenyl benzoyl pyrazoles as CRTH2 receptor ligands
Ulven, Trond, Frimurer, Thomas Michael, Rist, O., Kostenis, E., Hoegberg, T., Receveur, J. & Grimstrup, M., 2005, Patent No. WO 2005/115382 A1Research output: Patent
ID: 34520257
Most downloads
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610
downloads
Receptor structure-based discovery of non-metabolite agonists for the succinate receptor GPR91
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
143
downloads
Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
132
downloads
Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1
Research output: Contribution to journal › Journal article › Research › peer-review
Published