Darryl S Pickering

Darryl S Pickering

Associate Professor


  1. 2018
  2. 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. 85-92

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. 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 journalJournal articleResearchpeer-review

  4. 2019
  5. 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 journalJournal articleResearchpeer-review

  6. 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. 4467-4482

    Research output: Contribution to journalJournal articleResearchpeer-review

  7. 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 journalJournal articleResearchpeer-review

  8. 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 journalJournal articleResearchpeer-review

  9. 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 journalJournal articleResearchpeer-review

  10. 2020
  11. 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. 1791-1800

    Research output: Contribution to journalJournal articleResearchpeer-review

  12. 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 journalJournal articleResearchpeer-review

  13. 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 journalJournal articleResearchpeer-review

  14. 2022
  15. 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. 1580–1587

    Research output: Contribution to journalJournal articleResearchpeer-review

  16. 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 journalJournal articleResearchpeer-review

  17. 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. 181-200

    Research output: Contribution to journalReviewResearchpeer-review

  18. 2023
  19. 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 journalJournal articleResearchpeer-review

  20. 2024
  21. 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 journalJournal articleResearchpeer-review

  22. 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. 1506-1529

    Research output: Contribution to journalJournal articleResearchpeer-review

  23. 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. 743-757

    Research output: Contribution to journalJournal articleResearchpeer-review

  24. 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 journalJournal articleResearchpeer-review

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