Tommy Nørskov Johansen
Associate Professor
Medicinal Chemistry
Universitetsparken 2
2100 København Ø
- 2024
- Published
Tritium and deuterium labelling of a kainate receptor antagonist and evaluation as a radioligand
Chałupnik, P., Marek, A., Hovah, M. E. L., Pickering, Darryl S, Temperini, Piero, Donbosco, S., Szymańska, E. & Johansen, Tommy Nørskov, 2024, In: Journal of Labelled Compounds and Radiopharmaceuticals. 67, 4, p. 120-130Research output: Contribution to journal › Journal article › Research › peer-review
- 2023
- Published
Structure-Activity Relationship and Solubility Studies of Novel N1-substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists
Chałupnik, P., Vialko, A., Pickering, Darryl S, Nielsen, Birgitte, Bay, Y., Kristensen, Anders Skov, Hinkkanen, M., Szczepańska, K., Karcz, T., Latacz, G., Johansen, Tommy Nørskov & Szymanska, E. M., 2023, In: ChemMedChem. 18, 18, 15 p., e202300278.Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- Published
Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
Chałupnik, P., Vialko, A., Pickering, Darryl S, Hinkkanen, M., Donbosco, S., Møller, T. C., Jensen, Anders A., Nielsen, Birgitte, Bay, Y., Kristensen, Anders Skov, Johansen, Tommy Nørskov, Łątka, K., Bajda, M. & Szymańska, E., 2022, In: International Journal of Molecular Sciences. 23, 15, 16 p., 8797.Research output: Contribution to journal › Journal article › Research › peer-review
- 2021
- Published
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds
Pallesen, J. S., Narayanan, Dilip, Tran, K. T., Solbak, Sara Marie Øie, Marseglia, G., Sørensen, L. M. E., Høj, L. J., Munafò, F., Carmona, R. M. C., Garcia, A. D., Desu, H. L., Brambilla, R., Johansen, Tommy Nørskov, Popowicz, G. M., Sattler, M., Gajhede, Michael & Bach, Anders, 2021, In: Journal of Medicinal Chemistry. 64, 8, p. 4623–4661Research output: Contribution to journal › Journal article › Research › peer-review
- 2019
- Published
N1-Substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists: X-ray Crystallography, Structure-Affinity Relationships and in vitro Pharmacology
Pallesen, J. S., Møllerud, S., Frydenvang, Karla Andrea, Pickering, Darryl S, Bornholt, J., Nielsen, Birgitte, Pasini, D., Han, L., Marconi, L., Kastrup, Jette Sandholm Jensen & Johansen, Tommy Nørskov, 20 Mar 2019, In: A C S Chemical Neuroscience. 10, p. 1841-1853 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
N-(7-(1H-imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)benzamide - a new kainate receptor selective antagonist and analgesic: Synthesis, X-ray crystallography, structure-affinity relationships, in vitro and in vivo pharmacology
Møllerud, S., Hansen, R. B., Pallesen, J. S., Temperini, Piero, Pasini, D., Bornholdt, J., Nielsen, Birgitte, Mamedova, Esmira, Chalupnik, P., Paternain, A. V., Lerma, J., Del Castillo, M. D., Andreasen T., Jesper, Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen, Johansen, Tommy Nørskov & Pickering, Darryl S, 2019, In: ACS Chemical Neuroscience. 10, p. 4685-4695 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2017
- Published
Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
Szymańska, E., Chałupnik, P., Johansen, Tommy Nørskov, Nielsen, Birgitte, Cuñado Moral, A. M., Pickering, Darryl S & Kieć-Kononowicz, K., 1 Dec 2017, In: Chemical Biology & Drug Design. 90, p. 1271-1281 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Pharmacology and crystal structure of novel 2,3-quinoxalinediones at kainate receptors
Møllerud, S., Pallesen, J. S., Pasini, D., Marconi, L., Han, L., Bornholt, J., Johansen, Tommy Nørskov, Kastrup, Jette Sandholm Jensen, Pickering, Darryl S & Frydenvang, Karla Andrea, Aug 2017, In: Journal of Neurochemistry. 142, S1, p. 124 1 p., MTU07-13.Research output: Contribution to journal › Conference abstract in journal › Research › peer-review
- Published
Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors
Szymańska, E., Nielsen, Birgitte, Johansen, Tommy Nørskov, Cuñado Moral, A. M., Pickering, Darryl S, Szczepańska, K., Mickowska, A. & Kieć-Kononowicz, K., 2017, In: European Journal of Medicinal Chemistry. 138, p. 874-883 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2016
- Published
Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands
Szymańska, E., Chałupnik, P., Szczepańska, K., Moral, A. M. C., Pickering, Darryl S, Nielsen, Birgitte, Johansen, Tommy Nørskov & Kieć-Kononowicz, K., 2016, In: Bioorganic & Medicinal Chemistry Letters. 26, 22, p. 5568-5572 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors
Szymanska, E., Frydenvang, Karla Andrea, Pickering, Darryl S, Krintel, C., Nielsen, Birgitte, Kooshki, A., Zachariassen, L. G., Olsen, L., Kastrup, Jette Sandholm Jensen & Johansen, Tommy Nørskov, 2016, In: Journal of Medicinal Chemistry. 59, 1, p. 448-461 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2014
- Published
Design, synthesis and in vitro pharmacology of GluK1 and GluK3 antagonists. Studies towards the design of subtype-selective antagonists through 2-carboxyethyl-phenylalanines with substituents interacting with non-conserved residues in the GluK binding sites
Sköld, N., Nielsen, Birgitte, Olsen, J., Han, L., Olsen, L., Madsen, Ulf, Kristensen, Jesper Langgaard, Pickering, Darryl S & Johansen, Tommy Nørskov, 2 Aug 2014, In: Bioorganic & Medicinal Chemistry. 22, 19, p. 5368-5377 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2012
- Published
Structural and pharmacological characterization of phenylalanine-based AMPA receptor antagonists at kainate receptors
Venskutonyte, R., Frydenvang, Karla Andrea, Valadés, E. A., Szymanska, E. M., Johansen, Tommy Nørskov, Kastrup, Jette Sandholm Jensen & Pickering, Darryl S, Oct 2012, In: ChemMedChem. 7, 10, p. 1793-1798 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2011
- Published
A new phenylalanine derivative acts as an antagonist at the AMPA receptor GluA2 and introduces partial domain closure: Synthesis, resolution, pharmacology, and crystal structure
Szymanska, E., Frydenvang, Karla Andrea, Contreras-Sanz, A., Pickering, Darryl S, Frola, E., Serafimoska, Z., Nielsen, Birgitte, Kastrup, Jette Sandholm Jensen & Johansen, Tommy Nørskov, 4 Oct 2011, In: Journal of Medicinal Chemistry. 54, 20, p. 7289-7298Research output: Contribution to journal › Journal article › Research › peer-review
- 2010
- Published
Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones
Christensen, M. K., Erichsen, K. D., Trojel-Hansen, C., Tjørnelund, J., Nielsen, S. J., Frydenvang, Karla Andrea, Johansen, Tommy Nørskov, Nielsen, Birgitte, Sehested, M., Jensen, P. B., Ikaunieks, M., Zaichenko, A., Loza, E., Kalvinsh, I. & Björkling, Fredrik, 14 Oct 2010, In: Journal of Medicinal Chemistry. 53, 19, p. 7140-7145 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues
Lolli, M. L., Giordano, C., Pickering, Darryl S, Rolando, B., Hansen, K. B., Foti, A., Contreras-Sanz, A., Amir, A., Fruttero, R., Gasco, A., Nielsen, Birgitte & Johansen, Tommy Nørskov, 2010, In: Journal of Medicinal Chemistry. 53, 10, p. 4110-8 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2009
- Published
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
Szymanska, E., Pickering, Darryl S, Nielsen, Birgitte & Johansen, Tommy Nørskov, 2009, In: Bioorganic & Medicinal Chemistry. 17, 17, p. 6390-401 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2008
- Published
Bioactivation of diclofenac in vitro and in vivo: correlation to electrochemical studies
Madsen, K. G., Skonberg, C., Jurva, U., Cornett, Claus, Hansen, S. H., Johansen, Tommy Nørskov & Olsen, J., 2008, In: Chemical Research in Toxicology. 21, 5, p. 1107-19 12 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Palladium-catalyzed monoamination of dihalogenated benzenes
Larsen, S. B., Bang-Andersen, B., Johansen, Tommy Nørskov & Jørgensen, M., 2008, In: Tetrahedron. 64, 13, p. 2938-2950Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency
Beich-Frandsen, M., Pickering, Darryl S, Mirza, Osman Asghar, Johansen, Tommy Nørskov, Greenwood, J., Vestergaard, Bente, Schousboe, Arne, Gajhede, Michael, Liljefors, T. & Kastrup, Jette Sandholm Jensen, 2008, In: Journal of Medicinal Chemistry. 51, 5, p. 1459-63Research output: Contribution to journal › Journal article › Research › peer-review
- 2007
- Published
A tetrazolyl-substituted subtype-selective AMPA receptor agonist
Vogensen, S. B., Frydenvang, Karla Andrea, Greenwood, J. R., Postorino, G., Nielsen, Birgitte, Pickering, Darryl S, Ebert, B., Bølcho, U., Egebjerg, J., Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Johansen, Tommy Nørskov, Clausen, Rasmus Prætorius & Krogsgaard-Larsen, Povl, 2007, In: Journal of Medicinal Chemistry. 50, 10, p. 2408-2414Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA
Jensen, Anders A., Christesen, T., Bølcho, U., Greenwood, J. R., Postorino, G., Vogensen, S. B., Johansen, Tommy Nørskov, Egebjerg, J., Bräuner, Hans & Clausen, Rasmus Prætorius, 2007, In: Journal of Medicinal Chemistry. 50, 17, p. 4177-4185 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Selektive lægemiddelstoffer designet ud fra krystalstrukturer
Szymanska, E. M. & Johansen, Tommy Nørskov, 2007, In: Lægemiddelforskning. p. 34-35Research output: Contribution to journal › Journal article › Communication
- 2006
- Published
Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function.Synthesis, ionization constants and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds
Lolli, M. L., Hansen, S. L., Rolando, B., Nielsen, Birgitte, Wellendorph, Petrine, Madsen, K., Larsen, O. M., Kristiansen, Uffe, Fruttero, R., Gasco, A. & Johansen, Tommy Nørskov, 2006, In: J. Med. Chem.. 49, p. 4442-4446 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2005
- Published
Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues
Vogensen, S., Clausen, Rasmus Prætorius, Greenwood, J., Johansen, Tommy Nørskov, Pickering, Darryl S, Nielsen, Birgitte, Ebert, B. & Krogsgaard-Larsen, Povl, 5 May 2005, In: Journal of Medicinal Chemistry. 48, 9, p. 3438-3442Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302791
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Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
Research output: Contribution to journal › Journal article › Research › peer-review
Published -
28
downloads
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds
Research output: Contribution to journal › Journal article › Research › peer-review
Published