Thomas Michael Frimurer

Thomas Michael Frimurer

Associate Professor

Member of:

    ORCID: 0000-0002-9682-8245

    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.

     


    Publication year:
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    1 - 50 out of 73Page size: 50
    1. 2004
    2. Published

      A pseudo-sequence method for comparing 7TM receptors with respect to the physicochemical properties of their binding sites

      Frimurer, Thomas Michael, Ulven, Trond, Högberg, T. & Elling, C. E., 2004, Patent No. WO 2004/079625

      Research output: Patent

    3. Published

      Cyclic Quinoline compounds for use in MCH receptor related disorders

      Frimurer, Thomas Michael, Ulven, Trond, Högberg, T., Nørregaard, P. K., Little, P. B. & Receveur, J., 2004, Patent No. WO 2004/052371

      Research output: Patent

    4. Published

      Quinoline compounds for use in MCH receptor related disorders

      Frimurer, Thomas Michael, Ulven, Trond, Högberg, T., Nørregaard, P. K., Little, P. B. & Receveur, J., 2004, Patent No. WO 2004/052370

      Research output: Patent

    5. 2005
    6. Published

      6-Acylamino-2-aminoquinolines as Potent Melanin-Concentrating Hormone 1 Receptor Antagonists

      Ulven, Trond, Frimurer, Thomas Michael, Receveur, J., Little, P. B., Rist, Ø., Nørregaard, P. K. & Högberg, T., 2005, In: Journal of Medicinal Chemistry. 48, 18, p. 5684-5697 14 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    7. Published

      A physicogenetic method to assign ligand-binding relationships between 7TM receptors

      Frimurer, Thomas Michael, Ulven, Trond, Elling, T. C. E., Gerlach, L. O., Kostenis, E. & Högberg, T., 2005, In: Bioorganic & Medicinal Chemistry Letters. 15, 16, p. 3707-3712 6 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    8. Published

      CRTH2 receptor ligands for therapeutic use

      Ulven, Trond, Frimurer, Thomas Michael, Rist, Ø., Kostenis, E., Högberg, T., Receveur, J. & Grimstrup, M., 2005, Patent No. WO 2005/115382 A1

      Research output: Patent

    9. Published

      CRTH2 receptor ligands for therapeutic use - B-series

      Ulven, Trond, Frimurer, Thomas Michael, Rist, Ø., Kostenis, E. & Högberg, T., 2005, Patent No. WO 2005/115374 A1

      Research output: Patent

    10. Published

      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 A1

      Research output: Patent

    11. Published

      Preparation of substituted thiazoleacetic acids as CRTH2 receptor ligands

      Ulven, Trond, Frimurer, Thomas Michael, Rist, O., Kostenis, E., Hoegberg, T., Receveur, J. & Grimstrup, M., 2005, Patent No. WO 2005/116001 A1

      Research output: Patent

    12. Published

      Quinazoline compounds and their use in MCH-related disease

      Frimurer, Thomas Michael, Ulven, Trond, Högberg, T., Nørregaard, P. K., Little, P. B., Receveur, J. & Grimstrup, M., 2005, Patent No. WO 2005/123714

      Research output: Patent

    13. Published

      Substituted thiazoleacetic acids as CRTH2 receptor ligands

      Ulven, Trond, Frimurer, Thomas Michael, Rist, Ø., Kostenis, E., Högberg, T., Receveur, J. & Grimstrup, M., 2005, Patent No. WO 2005/116001 A1

      Research output: Patent

    14. 2006
    15. Published

      6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists

      Ulven, Trond, Little, P. B., Receveur, J., Frimurer, Thomas Michael, Rist, Ø., Nørregaard, P. K., Mathiesen, Jesper M. & Högberg, T., 2006, In: Bioorganic & Medicinal Chemistry Letters. 16, 4, p. 1070-1075 6 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    16. Published

      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

    17. 2007
    18. Published

      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 A1

      Research output: Patent

    19. Published

      Thiazole- and pyrimidineacetic 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 2007/062677 A1

      Research output: Patent

    20. 2009
    21. Published

      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

    22. 2010
    23. Published

      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

    24. Published

      Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists

      Grimstrup, M., Receveur, J. M., Rist, Ø., Frimurer, Thomas Michael, Nielsen, P. A., Mathiesen, Jesper M. & Högberg, T., 1 Mar 2010, In: Bioorganic and Medicinal Chemistry Letters. 20, 5, p. 1638-1641 4 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    25. 2011
    26. Published

      Allosteric and orthosteric sites in CC chemokine receptor (CCR5), a chimeric receptor approach

      Thiele, S., Steen, A., Jensen, P. C., Mokrosinski, J., Frimurer, Thomas Michael & Rosenkilde, Mette, 2011, In: Journal of Biological Chemistry. 286, 43, p. 37543-54 12 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    27. Published

      Reversed binding of a small molecule ligand in homologous chemokine receptors – differential role of extracellular loop 2.

      Rummel, P. C., Thiele, S., Steen, A. M. F., Elder, A., Kolbech, R., Ghosh, S., Frimurer, Thomas Michael & Rosenkilde, Mette, 2011, In: British Journal of Pharmacology. 166

      Research output: Contribution to journal › Journal article › Research › peer-review

    28. 2012
    29. Published

      Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2

      Jensen, P. C., Thiele, S., Steen, A., Elder, A., Kolbeck, R., Ghosh, S., Frimurer, Thomas Michael & Rosenkilde, Mette, May 2012, In: British Journal of Pharmacology. 166, 1, p. 258-75 18 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    30. Published

      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

    31. Published

      An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor

      Els, S., Schild, E., Petersen, P. S., Kilian, T., Mokrosinski, J., Frimurer, Thomas Michael, Chollet, C., Schwartz, Thue W., Holst, Birgitte & Beck-Sickinger, A. G., 13 Sep 2012, In: Journal of Medicinal Chemistry. 55, 17, p. 7437-49 13 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    32. Published

      The arginine of the DRY motif in transmembrane segment III functions as a balancing micro-switch in the activation of the β2-adrenergic receptor

      Hansen, L. V., Groenen, M., Nygaard, R., Frimurer, Thomas Michael, Holliday, N. D. & Schwartz, Thue W., 14 Sep 2012, In: Journal of Biological Chemistry. 287, 38, p. 31973-82 10 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    33. Published

      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

    34. Published

      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

    35. Published

      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

    36. Published

      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

    37. 2013
    38. Published

      Biased and Constitutive Signaling in the CC-Chemokine Receptor CCR5 by manipulating the Interface between Transmembrane Helix 6 and 7

      Steen, A., Thiele, S., Guo, D., Gasbjerg, Lærke Smidt, Frimurer, Thomas Michael & Rosenkilde, Mette, 3 May 2013, In: Journal of Biological Chemistry. 288, 18, p. 12511-12521 11 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    39. Published

      Assessment and Challenges of Ligand Docking into Comparative Models of G-Protein Coupled Receptors

      Nguyen, E. D., Meiler, J., Norn, C. & Frimurer, Thomas Michael, 2 Jul 2013, In: PLOS ONE. 8, 7, p. e67302 19 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    40. Published

      Structure-Activity Relationships and Identification of Optmized CC-Chemokine Receptor CCR1, 5, and 8 Metal-Ion Chelators

      Chalikiopoulos, A., Thiele, S., Malmgaard-Clausen, M., Rydberg, P., Isberg, V., Ulven, Trond, Frimurer, Thomas Michael, Rosenkilde, Mette & Gloriam, David E., 25 Nov 2013, In: Journal of Chemical Information and Modeling. 53, 11, p. 2863-73 11 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    41. 2014
    42. Published

      Gating function of isoleucine-116 in TM-3 (position III:16/3.40) for the activity state of the CC-chemokine receptor 5 (CCR5)

      Steen, A., wbf943, wbf943, Thiele, S., Guo, D., Frimurer, Thomas Michael & Rosenkilde, Mette, Mar 2014, In: British Journal of Pharmacology. 171, 6, p. 1566-79 14 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    43. Published

      Structural basis for constitutive activity and agonist-induced activation of the enteroendocrine fat sensor GPR119

      Engelstoft, M. S., Norn, C., Pedersen, M. H., Holliday, N. D., Elster, L., Lehmann, J., Jones, R. M., Frimurer, Thomas Michael & Schwartz, Thue W., Dec 2014, In: British Journal of Pharmacology. 171, 24, p. 5774-89 16 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    44. 2015
    45. Published

      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

    46. Published

      GPR40 (FFAR1) – Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

      Pedersen, M. H., Bentsen, M. A., Husted, Anna Sofie, Ekberg, J. P., Wright, M. J., Di Salvo, J., Weinglass, A. B., Engelstoft, M. S., Madsen, A. N., Lückmann, Michael, Miller, M. W., Trujillo, M. E., Frimurer, Thomas Michael, Holst, Birgitte, Howard, A. D. & Schwartz, Thue W., Jan 2015, In: Molecular Metabolism. 4, 1, p. 3-14 12 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    47. Published

      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, Rist, Ø., Elster, L. & Högberg, T., 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

    48. Published

      Downregulation of 5-HT7 Serotonin Receptors by the Atypical Antipsychotics Clozapine and Olanzapine. Role of Motifs in the C-Terminal Domain and Interaction with GASP-1

      Manfra, O., Van Craenenbroeck, K., Skieterska, K., Frimurer, Thomas Michael, Schwartz, Thue W., Levy, F. O. & Andressen, K. W., Jul 2015, In: A C S Chemical Neuroscience. 6, 7, p. 1206–1218 13 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    49. Published

      Biased Gs Versus Gq Proteins and β-Arrestin Signaling in the NK1 Receptor Determined by Interactions in the Water Hydrogen Bond Network

      Valentin-Hansen, L., Frimurer, Thomas Michael, Mokrosinski, J., Holliday, N. D. & Schwartz, Thue W., 2 Oct 2015, In: The Journal of Biological Chemistry. 290, 40, p. 24495-508 14 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    50. 2016
    51. Published

      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

    52. Published

      Role of Conserved Disulfide Bridges and Aromatic Residues in Extracellular Loop 2 of Chemokine Receptor CCR8 for Chemokine and Small Molecule Binding

      Barington, L., Rummel, P. C., Lückmann, Michael, Pihl, H., Larsen, Olav, Daugvilaite, V., Johnsen, A. H., Frimurer, Thomas Michael, Karlshøj, S. & Rosenkilde, Mette, 19 May 2016, In: The Journal of Biological Chemistry. 291, 31, p. 16208-16220

      Research output: Contribution to journal › Journal article › Research › peer-review

    53. Published

      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. 26860-26874

      Research output: Contribution to journal › Journal article › Research › peer-review

    54. 2017
    55. Published

      Biased agonism and allosteric modulation of GPR183- a 7TM receptor also known as EBV-induced EBI2

      Daugvilaite, V., Madsen, C. M., Lückmann, Michael, Castello Echeverria, C., Sailer, A. W., Frimurer, Thomas Michael, Rosenkilde, Mette & Benned-Jensen, T., 2017, In: British Journal of Pharmacology. 174, 13, p. 2031–2042

      Research output: Contribution to journal › Journal article › Research › peer-review

    56. Published

      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

    57. Published

      Structural biology: Full monty of family B GPCRs

      Schwartz, Thue W. & Frimurer, Thomas Michael, 2017, In: Nature Chemical Biology. 13, 8, p. 819-821

      Research output: Contribution to journal › Journal article › Research › peer-review

    58. Published

      Structure-based discovery of novel US28 small molecule ligands with different modes of action

      Lückmann, Michael, Amarandi, R., Papargyri, N., Jakobsen, M. H., Ulven, Elisabeth Rexen, Jensen, Lars Juhl, Pui, A., Schwartz, Thue W., Rosenkilde, Mette & Frimurer, Thomas Michael, 2017, In: Chemical Biology & Drug Design. 89, 3, p. 289–296

      Research output: Contribution to journal › Journal article › Research › peer-review

    59. Published

      Receptor structure-based discovery of non-metabolite agonists for the succinate receptor GPR91

      Trauelsen, Mette, Ulven, Elisabeth Rexen, Hjorth, Siv Annegrethe, Brvar, M., Monaco, C., Frimurer, Thomas Michael & Schwartz, Thue W., Dec 2017, In: Molecular Metabolism. 6, 12, p. 1585-1596 12 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    60. 2018
    61. Published

      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

    62. Published

      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. 244-254

      Research output: Contribution to journal › Journal article › Research › peer-review

    63. Published

      Structural changes at the myrtenol backbone reverse its positive allosteric potential into inhibitory GABAA receptor modulation

      Milanos, S., Kuenzel, K., Gilbert, D. F., Janzen, D., Sasi, M., Buettner, A., Frimurer, Thomas Michael & Villmann, C., 2018, In: Biological Chemistry. 399, 6, p. 549-563 15 p.

      Research output: Contribution to journal › Journal article › Research › peer-review

    64. Published

      Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1

      Ulven, Elisabeth Rexen, Trauelsen, Mette, Brvar, M., Lückmann, Michael, Bielefeldt, L. Ø., Jensen, L. K. I., Schwartz, Thue W. & Frimurer, Thomas Michael, 2018, In: Scientific Reports. 8, 1, p. 1-18 10010.

      Research output: Contribution to journal › Journal article › Research › peer-review

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