Thomas Michael Frimurer

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• 2025

  Renal Ghrelin-Family GPR39 Receptor and Urinary Concentrating Ability

  Liu, L., Rosenbaek, L. L., Kui, M., Svendsen, S. L., Brethvad, A. O., Jakobsen, A., Sparsoe, L. V., Hamilton, A., Sørensen, M. V., Skov, M., Therkildsen, J. R., Andresen, J. K., Laitakari, A., Frimurer, T. M., Jensen, B. L., Pluznick, J., Fenton, R. A., Holst, B. & Praetorius, H., 2025, (E-pub ahead of print) In: Journal of the American Society of Nephrology.

  Research output: Contribution to journal › Journal article › Research › peer-review
• 2024

  Molecular determinants of neuropeptide-mediated activation mechanisms in tachykinin NK1 and NK2 receptors

  Petersen, J. E., Pavlovskyi, A., Madsen, J. J., Schwartz, T. W., Frimurer, T. M. & Olsen, O. H., 2024, In: The Journal of Biological Chemistry. 300, 12, 13 p., 107948.

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• Molecular dynamics-based identification of binding pathways and two distinct high-affinity sites for succinate in succinate receptor 1/GPR91

  Shenol, A., Lückmann, M., Trauelsen, M., Lambrughi, M., Tiberti, M., Papaleo, E., Frimurer, T. M. & Schwartz, T. W., 2024, In: Molecular Cell. 84, 5, p. 955-966.e4 17 p.

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  7 Citations (Scopus)

  18 Downloads (Pure)

• Multiple recent HCAR2 structures demonstrate a highly dynamic ligand binding and G protein activation mode

  Shenol, A., Tenente, R., Lückmann, M., Frimurer, T. M. & Schwartz, T. W., 2024, In: Nature Communications. 15, 10 p., 5364.

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  2 Citations (Scopus)

  7 Downloads (Pure)
• 2023

  Biosynthesis of natural and halogenated plant monoterpene indole alkaloids in yeast

  Bradley, S. A., Lehka, B. J., Hansson, F. G., Adhikari, K. B., Rago, D., Rubaszka, P., Haidar, A. K., Chen, L., Hansen, L. G., Gudich, O., Giannakou, K., Lengger, B., Gill, R. T., Nakamura, Y., de Bernonville, T. D., Koudounas, K., Romero-Suarez, D., Ding, L., Qiao, Y. & Frimurer, T. M. & 12 others, Petersen, A. A., Besseau, S., Kumar, S., Gautron, N., Melin, C., Marc, J., Jeanneau, R., O’Connor, S. E., Courdavault, V., Keasling, J. D., Zhang, J. & Jensen, M. K., 2023, In: Nature Chemical Biology. 19, 12, p. 1551-1560 10 p.

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

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  23 Citations (Scopus)

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• Deciphering specificity and cross-reactivity in tachykinin NK1 and NK2 receptors

  Madsen, J. J., Petersen, J. E., Christensen, D. P., Hansen, J. B., Schwartz, T. W., Frimurer, T. M. & Olsen, O. H., 2023, In: Journal of Biological Chemistry. 299, 12, 11 p., 105438.

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  2 Citations (Scopus)

  24 Downloads (Pure)
• 2022

  Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures

  Madsen, J. J., Ye, L., Frimurer, T. M. & 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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  6 Citations (Scopus)

  28 Downloads (Pure)

• Optimization of First-in-Class Dual-Acting FFAR1/FFAR4 Allosteric Modulators with Novel Mode of Action

  Lückmann, M., Shenol, A., Nissen, T. A. D., Petersen, J. E., Kouvchinov, D., Schwartz, T. W. & Frimurer, T. M., 2022, In: ACS Medicinal Chemistry Letters. 13, 12, p. 1839-1847

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  3 Citations (Scopus)

  30 Downloads (Pure)

• Serotonin G Protein-Coupled Receptor-Based Biosensing Modalities in Yeast

  Lengger, B., Hoch-Schneider, E. E., Jensen, C. N., Jakočiū Nas, T., Petersen, A. A., Frimurer, T. M., Jensen, E. D. & Jensen, M. K., 2022, In: ACS Sensors. 7, 5, p. 1323-1335

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  19 Citations (Scopus)

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• 2021

  Discovery of GPR183 Agonists Based on an Antagonist Scaffold

  Kjær, V. M. S., Ieremias, L., Daugvilaite, V., Lückmann, M., Frimurer, T. M., Ulven, T., Rosenkilde, M. M. & Våbenø, J., 2021, In: ChemMedChem. 16, 17, p. 2623-2627

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  9 Citations (Scopus)

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• Extracellular succinate hyperpolarizes M2 macrophages through SUCNR1/GPR91-mediated Gq signaling

  Trauelsen, M., Hiron, T. K., Lin, D., Petersen, J. E., Breton, B., Husted, A. S., Hjorth, S. A., Inoue, A., Frimurer, T. M., Bouvier, M., O'Callaghan, C. A. & Schwartz, T. W., 2021, In: Cell Reports. 35, 11, 15 p., 109246.

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  82 Citations (Scopus)

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• GLP-1 Val8: A Biased GLP-1R Agonist with Altered Binding Kinetics and Impaired Release of Pancreatic Hormones in Rats

  van der Velden, W. J. C., Smit, F. X., Christiansen, C. B., Møller, T. C., Hjortø, G. M., Larsen, O., Schiellerup, S. P., Bräuner-Osborne, H., Holst, J. J., Hartmann, B., Frimurer, T. M. & Rosenkilde, M. M., 2021, In: ACS Pharmacology & Translational Science. 4, 1, p. 296-313 18 p.

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

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  29 Citations (Scopus)

• Investigating GIPR (ant)agonism: A structural analysis of GIP and its receptor

  Smit, F. X., van der Velden, W. J. C., Kizilkaya, H. S., Nørskov, A., Lückmann, M., Hansen, T. N., Sparre-Ulrich, A. H., Qvotrup, K., Frimurer, T. M. & Rosenkilde, M. M., 2021, In: Structure. 29, 7, p. 679-693.e6 21 p.

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

• Molecular mechanism of ligand binding pathways and activation of the succinate receptor

  Iliyaz, A. S., Luckmann, M., Trauelsen, M., Frimurer, T. M. & Schwartz, T. 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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• Selective release of gastrointestinal hormones induced by an orally active GPR39 agonist

  Grunddal, K. V., Diep, T. A., Petersen, N., Tough, I. R., Skov, L. J., Liu, L., Buijink, J. A., Mende, F., Jin, C., Jepsen, S. L., Sørensen, L. M. E., Achiam, M. P., Strandby, R. B., Bach, A., Hartmann, B., Frimurer, T. M., Hjorth, S. A., Bouvier, M., Cox, H. & Holst, B., 2021, In: Molecular Metabolism. 49, 14 p., 101207.

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

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  14 Citations (Scopus)

  61 Downloads (Pure)

• The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target

  Laitakari, A., Liu, L., Frimurer, T. M. & Holst, B., 2021, In: International Journal of Molecular Sciences. 22, 8, 22 p., 3872.

  Research output: Contribution to journal › Review › peer-review

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  32 Citations (Scopus)

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• 2020

  Structural basis for GPCR signaling by small polar versus large lipid metabolites-discovery of non-metabolite ligands

  Luckmann, M., Trauelsen, M., Frimurer, T. M. & Schwartz, T. W., 2020, In: Current Opinion in Cell Biology. 63, p. 38-48

  Research output: Contribution to journal › Review › peer-review
  20 Citations (Scopus)
• 2019

  Allostery in Coagulation Factor VIIa Revealed by Ensemble Refinement of Crystallographic Structures

  Sørensen, A. B., Madsen, J. J., Frimurer, T. M., Overgaard, M. T., Gandhi, P. S., Persson, E. & Olsen, O. H., 2019, In: Biophysical Journal. 116, 10, p. 1823-1835

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

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  9 Citations (Scopus)

• Biased Signaling of CCL21 and CCL19 Does Not Rely on N-Terminal Differences, but Markedly on the Chemokine Core Domains and Extracellular Loop 2 of CCR7

  Jorgensen, A. S., Larsen, O., Uetz-von Allmen, E., Lückmann, M., Legler, D. F., Frimurer, T. M., Veldkamp, C. T., Hjortø, G. M. & Rosenkilde, M. M., 2019, In: Frontiers in Immunology. 10, 14 p., 2156.

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

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  20 Citations (Scopus)

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• H4K20me0 recognition by BRCA1-BARD1 directs homologous recombination to sister chromatids

  Nakamura, K., Saredi, G., Becker, J. R., Foster, B. M., Nguyen, N. V., Beyer, T. E., Cesa, L. C., Faull, P. A., Lukauskas, S., Frimurer, T., Chapman, J. R., Bartke, T. & Groth, A., 2019, In: Nature Cell Biology. 21, 3, p. 311-318

  Research output: Contribution to journal › Letter › peer-review

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  144 Citations (Scopus)

• 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, T. M., Wang, M.-W., Schwartz, T. 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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  44 Citations (Scopus)

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• Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1

  Lückmann, M., Trauelsen, M., Bentsen, M. A., Nissen, T. A. D., Martins, J., Fallah, Z., Nygaard, M. M., Papaleo, E., Lindorff-Larsen, K., Schwartz, T. W. & Frimurer, T. M., 2 Apr 2019, In: Proceedings of the National Academy of Sciences of the United States of America. 116, 14, p. 7123-7128

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  42 Citations (Scopus)

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• Preassociation between the 5-HT₇ serotonin receptor and G protein G_s: molecular determinants and association with low potency activation of adenylyl cyclase

  Ulsund, A. H., Dahl, M., Frimurer, T. M., Manfra, O., Schwartz, T. W., Levy, F. O. & Andressen, K. W., 2019, In: FASEB Journal. 33, 3, p. 3870-3886

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

• Selective Allosteric Modulation of N-Terminally Cleaved, but Not Full Length CCL3 in CCR1

  Larsen, O., Lückmann, M., van der Velden, W. J. C., Oliva-Santiago, M., Brvar, M., Ulven, T., Frimurer, T. M., Karlshøj, S. & Rosenkilde, M. M., 2019, In: ACS Pharmacology & Translational Science. 2, 6, p. 429-441 13 p.

  Research output: Contribution to journal › Letter › peer-review

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  3 Citations (Scopus)

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• 2018

  Inhibiting RHOA Signaling in Mice Increases Glucose Tolerance and Numbers of Enteroendocrine and Other Secretory Cells in the Intestine

  Petersen, N., Frimurer, T. M., Pedersen, M. T., Egerod, K. L., Wewer, A. N. J., Holst, J. J., Grapin-Botton, A., Jensen, K. B. & Schwartz, T. W., 2018, In: Gastroenterology. 155, 4, p. 1164-1176 4 p.

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

• Ligand-selective small molecule modulators of the constitutively active vGPCR US28

  Amarandi, R.-M., Luckmann, M., Melynis, M., Jakobsen, M. H., Fallah, Z., Spiess, K., Hjorto, G. M., Pui, A., Frimurer, T. M. & Rosenkilde, M. M., 2018, In: European Journal of Medicinal Chemistry. 155, p. 244-254

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

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

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

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

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

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

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

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  16 Citations (Scopus)

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• The HETE Is on FFAR1 and Pancreatic Islet Cells

  Trauelsen, M., Lückmann, M., Frimurer, T. M. & Schwartz, T. W., 2018, In: Cell Metabolism. 27, 2, p. 273-275 3 p.

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

• Translating biased signaling in the ghrelin receptor system into differential in vivo functions

  Mende, F., Hundahl, C., Plouffe, B., Skov, L. J., Sivertsen, B., Madsen, A. N., Lückmann, M., Diep, T. A., Offermanns, S., Frimurer, T. M., Bouvier, M. & Holst, B., 2018, In: Proceedings of the National Academy of Sciences of the United States of America. 115, 43, p. E10255-E10264 10 p.

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

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  48 Citations (Scopus)
• 2017

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

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

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

• Model-Based Discovery of Synthetic Agonists for the Zn²⁺-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions.

  Frimurer, T. M., Mende, F., Graae, A.-S., Engelstoft, M. S., Egerod, K. L., Nygaard, R., Gerlach, L.-O., Hansen, J. B., Schwartz, T. W. & Holst, B., 2017, In: Journal of Medicinal Chemistry. 60, 3, p. 886-898 13 p.

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

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

  Trauelsen, M., Rexen Ulven, E., Hjorth, S. A., Brvar, M., Monaco, C., Frimurer, T. M. & Schwartz, T. W., Dec 2017, In: Molecular Metabolism. 6, 12, p. 1585-1596 12 p.

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

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  44 Citations (Scopus)

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• Structural biology: Full monty of family B GPCRs

  Schwartz, T. W. & Frimurer, T. M., 2017, In: Nature Chemical Biology. 13, 8, p. 819-821

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

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

  Lückmann, M., Amarandi, R.-M., Papargyri, N., Jakobsen, M. H., Christiansen, E., Jensen, L. J., Pui, A., Schwartz, T. W., Rosenkilde, M. M. & Frimurer, T. M., 2017, In: Chemical Biology & Drug Design. 89, 3, p. 289–296

  Research output: Contribution to journal › Journal article › Research › peer-review
  13 Citations (Scopus)
• 2016

  In Silico Investigation of the Neurotensin Receptor 1 Binding Site: Overlapping Binding Modes for Small Molecule Antagonists and the Endogenous Peptide Agonist

  Lückmann, M., Holst, B., Schwartz, T. W. & Frimurer, T. M., 2016, In: Molecular Informatics. 35, p. 19-24 6 p.

  Research output: Contribution to journal › Letter › peer-review

  Open Access
  9 Citations (Scopus)

• Molecular Mechanism of Action for Allosteric Modulators and Agonists in CC-chemokine Receptor 5 (CCR5)

  Karlshøj, S., Amarandi, R. M., Larsen, O., Daugvilaite, V., Steen, A., Brvar, M., Pui, A., Frimurer, T. M., Ulven, T. & Rosenkilde, M. M., 23 Dec 2016, In: Journal of Biological Chemistry. 291, 52, p. 26860-26874

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

  Open Access
  11 Citations (Scopus)

• 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, M., Pihl, H., Larsen, O., Daugvilaite, V., Johnsen, A. H., Frimurer, T. M., Karlshøj, S. & Rosenkilde, M. M., 19 May 2016, In: The Journal of Biological Chemistry. 291, 31, p. 16208-16220

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

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

  Valentin-Hansen, L., Frimurer, T. M., Mokrosinski, J., Holliday, N. D. & Schwartz, T. 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
  36 Citations (Scopus)

• 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, T., Schwartz, T. 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
  13 Citations (Scopus)

• 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, A. S., Ekberg, J. P., Wright, M. J., Di Salvo, J., Weinglass, A. B., Engelstoft, M. S., Madsen, A. N., Lückmann, M., Miller, M. W., Trujillo, M. E., Frimurer, T. M., Holst, B., Howard, A. D. & Schwartz, T. W., Jan 2015, In: Molecular Metabolism. 4, 1, p. 3-14 12 p.

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

  Open Access
  195 Citations (Scopus)

• 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, T. W. & Frimurer, T. M., 2015, In: Structure. 23, 12, p. 2377-2386 10 p.

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

• 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
  8 Citations (Scopus)
• 2014

  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., Sparre-Ulrich, A. H., Thiele, S., Guo, D., Frimurer, T. M. & Rosenkilde, M. M., Mar 2014, In: British Journal of Pharmacology. 171, 6, p. 1566-79 14 p.

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

• 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, T. M. & Schwartz, T. 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
  25 Citations (Scopus)
• 2013

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

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

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

• 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., Hansen, L. S., Frimurer, T. M. & Rosenkilde, M. M., 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

  Open Access
  62 Citations (Scopus)

• 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, T., Frimurer, T. M., Rosenkilde, M. M. & Gloriam, D. 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
  3 Citations (Scopus)
• 2012

  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.-M., Mokrosinski, J., Frimurer, T. M., Chollet, C., Schwartz, T. W., Holst, B. & Beck-Sickinger, A. G., 13 Sept 2012, In: Journal of Medicinal Chemistry. 55, 17, p. 7437-49 13 p.

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

• Melanin concentrating hormone receptor 1 (MCHR1) antagonists - Still a viable approach for obesity treatment?

  Högberg, T., Frimurer, T. M. & 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
  37 Citations (Scopus)