Darryl S Pickering
Associate Professor
Molecular and Cellular Pharmacology
Jagtvej 160, København Ø
- 2024
- Published
Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure
Bay, Yasmin, 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, Yasmin, 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
- Accepted/In press
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, (Accepted/In press) In: Journal of Labelled Compounds and Radiopharmaceuticals.Research output: Contribution to journal › Journal article › Research › peer-review
- 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, Yasmin, 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
- 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, B., Bay, Yasmin, 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, Yasmin, 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
- 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
- Published
(S)-2-Mercaptohistidine: A First Selective Orthosteric GluK3 Antagonist
Poulie, Christian Bernard Matthijs, Larsen, Y., Leteneur, C., Barthet, G., Bjørn-Yoshimoto, Walden, Malhaire, F., Nielsen, Birgitte, Pin, J. P., Mulle, C., Pickering, Darryl S & Bunch, Lennart, 2022, In: ACS Chemical Neuroscience. 13, 10, p. 1580–1587Research 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
- Published
A Diversity Oriented Synthesis Approach to New 2,3-trans-Substituted l-Proline Analogs as Potential Ligands for the Ionotropic Glutamate Receptors
Kayser, S., Temperini, Piero, Poulie, Christian Bernard Matthijs, Staudt, Markus, Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 4 Mar 2020, In: ACS Chemical Neuroscience. 11, p. 702-714 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors
Kayser, S., Hansen, J. C., Staudt, Markus, Moroz, A., Larsen, Y., Temperini, Piero, Yi, F., Syrenne, J. T., Krogsgaard-Larsen, N., Iliadis, S., Nielsen, Birgitte, Hansen, K. B., Pickering, Darryl S & Bunch, Lennart, 2020, In: ACS Chemical Neuroscience. 11, p. 674-701 28 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2019
- 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
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
Design and Synthesis of 2,3-trans-Proline Analogs as Ligands for the Ionotropic Glutamate Receptors and the Excitatory Amino Acid Transporters
Poulie, Christian Bernard Matthijs, Alcaide Lopez, A., Krell-Jørgensen, M. P., Larsen, Y., Astier, E., Bjørn-Yoshimoto, Walden, Yi, F., Syrenne, J. T., Storgaard, M., Nielsen, Birgitte, Frydenvang, Karla Andrea, Jensen, Anders A., Hansen, K. B., Pickering, Darryl S & Bunch, Lennart, 19 Jun 2019, In: A C S Chemical Neuroscience. 10, 6, p. 2989-3007 19 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
- Published
The Presence of Calcitonin Gene-Related Peptide and Its Receptors in Rat, Pig and Human Brain: Species Differences in Calcitonin Gene-Related Peptide Pharmacology
Warfvinge, K., Edvinsson, L., Pickering, Darryl S & Sheykhzade, Majid, 1 Dec 2019, In: Pharmacology. 104, p. 332-341 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2018
- 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
Vascular and molecular pharmacology of the metabolically stable CGRP analogue, SAX
Sheykhzade, Majid, Abdolalizadeh, B., Koole, C., Pickering, Darryl S, Dreisig, K., Johansson, S. E., Abboud, B. K., Dreier, R., Berg, J. O., Jeppesen, J. L., Sexton, P., Edvinsson, L., Wootten, D. & Sams, A., 2018, In: European Journal of Pharmacology. 829, p. 85-92Research output: Contribution to journal › Journal article › Research › peer-review
- 2017
- Published
Revisiting the Quinoxalinedione scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors.
Demmer, C. S., Rombach, D., Liu, N., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 1 Dec 2017, In: A C S Chemical Neuroscience. 8, 11, p. 2477-2495 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist
Gynther, M., Proietti Silvestri, I., Hansen, J. C., Hansen, K. B., Malm, T., Ishchenko, Y., Larsen, Y., Han, L., Kayser, S., Auriola, S., Petsalo, A., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 14 Dec 2017, In: Journal of Medicinal Chemistry. 60, 23, p. 9885-9904 20 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
- 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
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
Structure and affinity of two bicyclic glutamate analogues at AMPA and kainate receptors
Møllerud, S., Pinto, A., Marconi, L., Frydenvang, Karla Andrea, Thorsen, T. S., Laulumaa, S. K., Venskutonyte, R., Winther, Nikolaj Sebastian, Cunado Moral, A. M., Tamborini, L., Conti, P., Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, 2017, In: A C S Chemical Neuroscience. 8, 9, p. 2056-2064 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Investigation of antidepressant-like and anxiolytic-like actions and cognitive and motor side effects of four N-methyl-D-aspartate receptor antagonists in mice
Refsgaard, L. K., Pickering, Darryl S & Andreasen T., Jesper, 1 Feb 2017, In: Behavioural Pharmacology. 28, 1, p. 37-47 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1299533
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Investigation of the presence and antinociceptive function of muscarinic acetylcholine receptors in the African naked mole-rat (Heterocephalus glaber)
Research output: Contribution to journal › Journal article › Research › peer-review
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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