Jette Sandholm Jensen Kastrup
Professor
Structural Biology
Universitetsparken 2
2100 København Ø
- 2024
- Published
Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators
Francotte, P., Bay, Y., Goffin, E., Colson, T., Lesenfants, C., Dorosz, J., Laulumaa, S., Fraikin, P., de Tullio, P., Beaufour, C., Botez, I., Pickering, Darryl S, Frydenvang, Karla Andrea, Danober, L., Kristensen, A. S., Kastrup, Jette Sandholm Jensen & Pirotte, B., 2024, In: European Journal of Medicinal Chemistry. 264, 15 p., 116036.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Recovery from desensitization in GluA2 AMPA receptors is affected by a single mutation in the N-terminal domain interface
Nørgrd Larsen, Andreas, Perozzo, A. M., Biggin, P. C., Bowie, D. & Kastrup, Jette Sandholm Jensen, 2024, In: Journal of Biological Chemistry. 300, 3, 10 p., 105717.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure
Bay, Y., Venskutonytė, R., Frantsen, S. M., Thorsen, T. S., Musgaard, M., Frydenvang, Karla Andrea, Francotte, P., Pirotte, B., Biggin, P. C., Kristensen, Anders Skov, Boesen, T., Pickering, Darryl S, Gajhede, Michael & Kastrup, Jette Sandholm Jensen, 2024, In: FEBS Journal. 291, 7, p. 1506-1529Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The positive allosteric modulator BPAM344 and L-glutamate introduce an active-like structure of the ligand-binding domain of GluK2
Bay, Y., Egeberg Jeppesen, M., Frydenvang, Karla Andrea, Francotte, P., Pirotte, B., Pickering, Darryl S, Kristensen, Anders Skov & Kastrup, Jette Sandholm Jensen, 2024, In: FEBS Letters. 598, 7, p. 743-757Research output: Contribution to journal › Journal article › Research › peer-review
- 2023
- Published
Differences between the GluD1 and GluD2 receptors revealed by GluD1 X-ray crystallography, binding studies and molecular dynamics
Masternak, Magdalena, Koch, A., Laulumaa, S., Tapken, D., Hollmann, M., Jørgensen, Flemming Steen & Kastrup, Jette Sandholm Jensen, 2023, In: F E B S Journal. 290, 15, p. 3781-3801Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- Published
Structural basis for positive allosteric modulation of AMPA and kainate receptors
Frydenvang, Karla Andrea, Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, 2022, In: The Journal of Physiology. 600, 2, p. 181-200Research output: Contribution to journal › Review › Research › peer-review
- 2021
- Published
Binding of a negative allosteric modulator and competitive antagonist can occur simultaneously at the ionotropic glutamate receptor GluA2
Krintel, C., Dorosz, J., Larsen, A. H., Thorsen, T. S., Venskutonytė, R., Mirza, Osman Asghar, Gajhede, Michael, Boesen, T. & Kastrup, Jette Sandholm Jensen, 2021, In: The FEBS Journal. 288, p. 995-1007 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Development of Thiochroman Dioxide Analogues of Benzothiadiazine Dioxides as New Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors
Etsè, K. S., Dorosz, J., McLain Christensen, K., Thomas, J. Y., Botez Pop, I., Goffin, E., Colson, T., Lestage, P., Danober, L., Pirotte, B., Kastrup, Jette Sandholm Jensen & Francotte, P., 2021, In: ACS Chemical Neuroscience. 12, 14, p. 2679-2692Research output: Contribution to journal › Journal article › Research › peer-review
- 2020
- Published
Ionotropic glutamate receptor GluA2 in complex with bicyclic pyrimidinedione-based compounds: when small compound modifications have distinct effects on binding interactions
Frydenvang, Karla Andrea, Pickering, Darryl S, Kshirsagar, G. U., Chemi, G., Gemma, S., Sprogøe, D., Kærn, A. M., Brogi, S., Campiani, G., Butini, S. & Kastrup, Jette Sandholm Jensen, 2020, In: ACS Chemical Neuroscience. 11, 12, p. 1791-1800Research output: Contribution to journal › Journal article › Research › peer-review
- 2019
- Published
Nanoscale Mobility of the Apo State and TARP Stoichiometry Dictate the Gating Behavior of Alternatively Spliced AMPA Receptors
Dawe, G. B., Kadir, M. F., Venskutonyte, R., Perozzo, A. M., Yan, Y., Alexander, R. P. D., Navarrete, C., Santander, E. A., Arsenault, M., Fuentes, C., Aurousseau, M. R. P., Frydenvang, Karla Andrea, Barrera, N. P., Kastrup, Jette Sandholm Jensen, Edwardson, J. M. & Bowie, D., 5 Jun 2019, In: Neuron. 102, 5, p. 976-+Research output: Contribution to journal › Journal article › Research › peer-review
- 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
Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor
Laulumaa, S., Hansen, K. V., Masternak, M., Drapier, T., Francotte, P., Pirotte, B., Frydenvang, Karla Andrea & Kastrup, Jette Sandholm Jensen, 14 Mar 2019, In: ACS Medicinal Chemistry Letters. 10, 3, p. 243-247 5 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
- Published
Use of the 4-Hydroxy-Triazole Moiety as a Bioisosteric Tool for the Development of Ionotropic Glutamate Receptor Ligands
Sainas, S., Temperini, P., Farnsworth, J. C., Yi, F., Møllerud, S., Jensen, Anders A., Nielsen, Birgitte, Kastrup, Jette Sandholm Jensen, Hansen, K. B., Boschi, D., Pickering, Darryl S, Clausen, Rasmus Prætorius & Lolli, M., 2019, In: Journal of Medicinal Chemistry. 62, p. 4467-4482Research output: Contribution to journal › Journal article › Research › peer-review
- 2018
- Published
Small-angle neutron scattering studies on the AMPA receptor GluA2 in the resting, AMPA-bound and GYKI-53655-bound states
Nørgrd Larsen, Andreas, Dorosz, J., Thorsen, T. S., Johansen, Nicolai Tidemand, Darwish, T., Midtgaard, S. R., Arleth, Lise & Kastrup, Jette Sandholm Jensen, Nov 2018, In: IUCrJ. 5, p. 780-793Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds
Drapier, T., Geubelle, P., Bouckaert, C., Nielsen, Lise Nikolic, Laulumaa, S., Goffin, E., Dilly, S., Francotte, P., Hanson, J., Pochet, L., Kastrup, Jette Sandholm Jensen & Pirotte, B., 28 Jun 2018, In: Journal of Medicinal Chemistry. 61, 12, p. 5279-5291 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation.
Brogi, S., Brindisi, M., Butini, S., Kshirsagar, G., Maramai, S., Chemi, G., Gemma, S., Campiani, G., Novellino, E., Fiorenzani, P., Pinassi, J., Aloisi, A. M., Gynther, M., Venskutonyte, R., Han, L., Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen & Pickering, Darryl S, 8 Mar 2018, In: Journal of Medicinal Chemistry. 61, 5, p. 2124-2130 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency
Goffin, E., Drapier, T., Larsen, A. P., Geubelle, P., Ptak, C. P., Laulumaa, S., Rovinskaja, K., Gilissen, J., Tullio, P. D., Olsen, L., Frydenvang, Karla Andrea, Pirotte, B., Hanson, J., Oswald, R. E., Kastrup, Jette Sandholm Jensen & Francotte, P., Jan 2018, In: Journal of Medicinal Chemistry. 61, 1, p. 251–264Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Invisible detergents for structure determination of membrane proteins by small-angle neutron scattering
Midtgaard, S. R., Darwish, T. A., Pedersen, M. C., Huda, P., Larsen, A. H., Jensen, G. V., Kynde, S. A. R., Skar-Gislinge, N., Nielsen, A. J. Z., Olesen, C., Blaise, M., Dorosz, J. J., Thorsen, T. S., Venskutonytė, R., Krintel, C., Møller, J. V., Frielinghaus, H., Gilbert, E. P., Martel, A., Kastrup, J. S. J. & 3 others, , Jan 2018, In: F E B S Journal. 285, 2, p. 357-371 15 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2017
- 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
Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors
Larsen, A. P., Fièvre, S., Frydenvang, Karla Andrea, Francotte, P., Pirotte, B., Kastrup, Jette Sandholm Jensen & Mulle, C., Jun 2017, In: Molecular Pharmacology. 91, 6, p. 576-585 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The low binding affinity of D-serine at the ionotropic glutamate receptor GluD2 can be attributed to the hinge region
Tapken, D., Steffensen, T. B., Leth, R., Kristensen, L. B., Gerbola, A., Gajhede, Michael, Jørgensen, Flemming Steen, Olsen, L. & Kastrup, Jette Sandholm Jensen, 7 Apr 2017, In: Scientific Reports. 7, 12 p., 46145.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The structure of the mite allergen Blo t 1 explains the limited antibody cross-reactivity to Der p 1
Meno, K. H., Kastrup, Jette Sandholm Jensen, Kuo, I., Chua, K. Y. & Gajhede, Michael, 1 Apr 2017, In: Allergy. 72, 4, p. 665-670 6 p., 13111.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Lessons from crystal structures of kainate receptors
Møllerud, S., Frydenvang, Karla Andrea, Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, 1 Jan 2017, In: Neuropharmacology. 112, Part A, p. 16-28 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Design and Synthesis of a Series of L-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid
Krogsgaard-Larsen, N., Delgar, C., Koch, K., Brown, P. M. G. E., Møller, C., Han, L., Huynh, Tri Hien Viet, Hansen, S. W., Nielsen, Birgitte, Bowie, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2017, In: Journal of Medicinal Chemistry. 60, 1, p. 441-457 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1298590
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Structure of rat acidic fibroblast growth factor at 1.4 A resolution.
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