Darryl S Pickering

Darryl S Pickering

Associate Professor


  1. Published

    1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators. / Butini, Stefania; Pickering, Darryl S; Morelli, Elena; Coccone, Salvatore Sanna; Trotta, Francesco; De Angelis, Meri; Guarino, Egeria; Fiorini, Isabella; Campiani, Giuseppe; Novellino, Ettore; Schousboe, Arne; Christensen, Jeppe K; Gemma, Sandra.

    In: Journal of Medicinal Chemistry, Vol. 51, No. 20, 2008, p. 6614-8.

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Published

    3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands. / Szymanska, Ewa; Pickering, Darryl S; Nielsen, Birgitte; Johansen, Tommy N.

    In: Bioorganic & Medicinal Chemistry, Vol. 17, No. 17, 2009, p. 6390-401.

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    3-hydroxypyridazine 1-oxides as carboxylate bioisosteres : a new series of subtype-selective AMPA receptor agonists. / Greenwood, Jeremy R; Mewett, Ken N; Allan, Robin D; Martín, Belén Ortiz; Pickering, Darryl.

    In: Neuropharmacology, Vol. 51, No. 1, 07.2006, p. 52-9.

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Published

    4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters. / Bunch, Lennart; Pickering, Darryl S; Gefflaut, Thierry; Vinatier, Virginie; Helaine, Virgil; Amir, Ahmad; Nielsen, Birgitte; Jensen, Anders Asbjørn.

    In: ChemMedChem, Vol. 4, No. 11, 2009, p. 1925-1929.

    Research output: Contribution to journalJournal articleResearchpeer-review

  5. 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, Marco L; Giordano, Cecilia; Pickering, Darryl S; Rolando, Barbara; Hansen, Kasper B; Foti, Antonio; Contreras-Sanz, Alberto; Amir, Ahmad; Fruttero, Roberta; Gasco, Alberto; Nielsen, Birgitte; Johansen, Tommy N.

    In: Journal of Medicinal Chemistry, Vol. 53, No. 10, 2010, p. 4110-8.

    Research output: Contribution to journalJournal articleResearchpeer-review

  6. 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, Ewa; Frydenvang, Karla; Contreras-Sanz, Alberto; Pickering, Darryl S; Frola, Elena; Serafimoska, Zorica; Nielsen, Birgitte; Kastrup, Jette Sandholm; Johansen, Tommy Nørskov.

    In: Journal of Medicinal Chemistry, Vol. 54, No. 20, 04.10.2011, p. 7289-7298.

    Research output: Contribution to journalJournal articleResearchpeer-review

  7. Published

    A tetrazolyl-substituted subtype-selective AMPA receptor agonist. / Vogensen, Stine Byskov; Frydenvang, Karla Andrea; Greenwood, Jeremy R.; Postorino, Giovanna; Nielsen, Birgitte; Pickering, Darryl Scott; Ebert, Bjarke; Bølcho, Ulrik; Egebjerg, Jan; Gajhede, Michael; Kastrup, Jette Sandholm Jensen; Johansen, Tommy Nørskov; Clausen, Rasmus Prætorius; Krogsgaard-Larsen, Povl.

    In: Journal of Medicinal Chemistry, Vol. 50, No. 10, 2007, p. 2408-2414.

    Research output: Contribution to journalJournal articleResearchpeer-review

  8. Published
  9. Published

    Binding site and interlobe interactions of the ionotropic glutamate receptor GluK3 ligand binding domain revealed by high resolution crystal structure in complex with (S)-glutamate. / Venskutonyte, Raminta; Frydenvang, Karla; Gajhede, Michael; Bunch, Lennart; Pickering, Darryl S; Kastrup, Jette Sandholm.

    In: Journal of Structural Biology, Vol. 176, No. 3, 12.2011, p. 307-314.

    Research output: Contribution to journalJournal articleResearchpeer-review

  10. Published

    Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid. / Frydenvang, Karla Andrea; Pickering, Darryl S; Greenwood, Jeremy R; Krogsgaard-Larsen, Niels; Brehm, Lotte; Nielsen, Birgitte; Vogensen, Stine Byskov; Hald, Helle; Kastrup, Jette Sandholm; Krogsgaard-Larsen, Povl; Clausen, Rasmus Prætorius.

    In: Journal of Medicinal Chemistry, Vol. 53, No. 23, 10.11.2010, p. 8354-8361.

    Research output: Contribution to journalJournal articleResearchpeer-review

  11. Published

    Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid : a novel selective inhibitor of human excitatory amino acid transporter subtype 2. / Sagot, Emanuelle; Jensen, Anders A.; Pickering, Darryl S; Pu, Xiaosui; Umberti, Michelle; Stensbøl, Tine B.; Nielsen, Birgitte; Assaf, Zeinab; Aboab, Bétina; Bolte, Jean; Gefflaut, Thierry; Bunch, Lennart.

    In: Journal of Medicinal Chemistry, Vol. 51, No. 14, 2008, p. 4085-4092.

    Research output: Contribution to journalJournal articleResearchpeer-review

  12. Published

    Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7. / Sagot, Emanuelle; Pickering, Darryl S; Pu, Xiaosui; Umberti, Michelle; Stensbøl, Tine B; Nielsen, Birgitte; Chapelet, Marion; Bolte, Jean; Gefflaut, Thierry; Bunch, Lennart.

    In: Journal of Medicinal Chemistry, Vol. 51, No. 14, 2008, p. 4093-103.

    Research output: Contribution to journalJournal articleResearchpeer-review

  13. Published

    Chemo-enzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters. / Assaf, Z.; Larsen, Anja Probst; Venskutonyte, Raminta; Han, Liwei; Abrahamsen, Bjarke; Nielsen, Birgitte; Gajhede, Michael; Kastrup, Jette Sandholm; Jensen, Anders A.; Pickering, Darryl S; Frydenvang, Karla ; Gefflaut, T; Bunch, Lennart.

    In: Journal of Medicinal Chemistry, Vol. 56, No. 4, 2013, p. 1614-1628.

    Research output: Contribution to journalJournal articleResearchpeer-review

  14. Published

    Cognitive enhancing effects of an AMPA receptor positive modulator on place learning in mice. / Rytter, Hana Malá; Chen, Yuxia; Worm, Vivi Hu; Kure, Julie; Kaae, Birgitte H.; Madsen, Ulf; Badolo, Lassina; Pickering, Darryl S; Mogensen, Jesper.

    In: Behavioural Brain Research, Vol. 226, No. 1, 2012, p. 18-25.

    Research output: Contribution to journalJournal articleResearchpeer-review

  15. Published

    Computeren viser vejen til et nyt potentielt lægemiddel. / Harpsøe, Kasper; Kaae, Birgitte Høiriis; Balle, Thomas; Pickering, Darryl S; Kastrup, Jette Sandholm Jensen.

    In: Lægemiddelforskning, 2008, p. 28-30.

    Research output: Contribution to journalJournal articleCommunication

  16. Published

    Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. / Kvist, Trine; Steffensen, Thomas Bielefeldt; Greenwood, Jeremy R; Mehrzad Tabrizi, Fatemeh; Hansen, Kasper Bø; Gajhede, Michael; Pickering, Darryl S; Traynelis, Stephen F; Kastrup, Jette Sandholm; Bräuner-Osborne, Hans.

    In: The Journal of Biological Chemistry, Vol. 288, 2013, p. 33124-35.

    Research output: Contribution to journalJournal articleResearchpeer-review

  17. Published

    Design and characterization of dimeric ligands cross-linking two identical modulatory AMPA receptor sites. / Kaae, Birgitte H.; Harpsoe, Kasper; Sanz, Alberto Contreras; Pickering, Darryl S.; Sauerberg, Per; Clausen, Rasmus Prætorius; Kastrup, Jette S.; Liljefors, Tommy; Madsen, Ulf.

    In: American Chemical Society. Abstracts of Papers (at the National Meeting), Vol. 234, 19.08.2007.

    Research output: Contribution to journalConference abstract in journalResearch

  18. Published
  19. Published

    Discovery of a New Class of Ionotropic Glutamate Receptor Antagonists by the Rational Design of (2S,3R)-3-(3-Carboxyphenyl)-pyrrolidine-2-carboxylic Acid. / Larsen, Ann Møller; Venskutonyte, Raminta; Valadés, Elena Antón; Nielsen, Birgitte; Pickering, Darryl S; Bunch, Lennart.

    In: ACS Chemical Neuroscience, Vol. 2, No. 2, 04.11.2011, p. 107-114.

    Research output: Contribution to journalJournal articleResearchpeer-review

  20. Published

    Does increasing the ratio of AMPA-to-NMDA receptor mediated neurotransmission engender antidepressant action? Studies in the mouse forced swim and tail suspension tests. / Andreasen T., Jesper; Gynther, Mikko Otto Oskari; Rygaard, Allan; Bøgelund, Trine; Nielsen, Simon Dalsgaard; Clausen, Rasmus Prætorius; Mogensen, Jesper; Pickering, Darryl S.

    In: Neuroscience Letters, Vol. 546, 2013, p. 6-10.

    Research output: Contribution to journalJournal articleResearchpeer-review

  21. Published

    Effect of synthetic and natural phospholipids on N-acylphosphatidylethanolamine-hydrolyzing phospholipase D activity. / Petersen, Gitte; Pedersen, Anders H; Pickering, Darryl S; Begtrup, Mikael; Hansen, Harald S.

    In: Chemistry and Physics of Lipids, Vol. 162, No. 1-2, 2009, p. 53-61.

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. Published
  23. Published

    Full domain closure of the ligand-binding core of the ionotropic glutamate receptor iGluR5 induced by the high affinity agonist dysiherbaine and the functional antagonist 8,9-dideoxyneodysiherbaine. / Frydenvang, Karla Andrea; Lash, L Leanne; Naur, Peter; Postila, Pekka A; Pickering, Darryl S; Smith, Caleb M; Gajhede, Michael; Sasaki, Makoto; Sakai, Ryuichi; Pentikäinen, Olli T; Swanson, Geoffrey T; Kastrup, Jette Sandholm.

    In: Journal of Biological Chemistry, Vol. 284, No. 21, 2009, p. 14219-14229.

    Research output: Contribution to journalJournal articleResearchpeer-review

  24. Published

    GABA transporter localization to lipid raft membrane microdomains in neurons and astrocytes. / Madsen, Karsten Kirkegaard; Pickering, Darryl S; Hansen, G.H.; Danielsen, E.M.; Larsson, Orla Miller; Schousboe, Arne.

    In: Journal of Neurochemistry, Vol. 102, No. s1, 2007, p. 46.

    Research output: Contribution to journalConference abstract in journalResearch

  25. Published

    Ionotropic glutamate-like receptor d2 binds D-serine and glycine. / Naur, Peter; Hansen, Kasper Bø; Kristensen, Anders Skov; Dravid, Shashank M.; Pickering, Darryl Scott; Olsen, Lars; Vestergaard, Bente; Egebjerg, Jan; Gajhede, Michael; Traynelis, Stephen F.; Kastrup, Jette Sandholm Jensen.

    In: Proceedings of the National Academy of Science of the United States of America, Vol. 104, No. 35, 2007, p. 14116-14121.

    Research output: Contribution to journalJournal articleResearchpeer-review

  26. Published

    L-Asp is a useful tool in the purification of the ionotropic glutamate receptor A2 ligand-binding domain. / Krintel, Christian; Frydenvang, Karla; Ceravalls de Rabassa, Anna; Kaern, Anne Mette; Gajhede, Michael; Pickering, Darryl S; Kastrup, Jette S.

    In: F E B S Journal, 27.03.2014, p. 2422–2430.

    Research output: Contribution to journalJournal articleResearchpeer-review

  27. Published

    Molecular mechanism of agonist recognition by the ligand-binding core of the ionotropic glutamate receptor 4 . / Kasper, Christina; Frydenvang, Karla Andrea; Naur, Peter; Gajhede, Michael; Pickering, Darryl S; Kastrup, Jette Sandholm Jensen.

    In: FEBS Letters, Vol. 582, No. 29, 2008, p. 4089-4094.

    Research output: Contribution to journalJournal articleResearchpeer-review

  28. Published

    Molecular recognition of two 2,4-syn-functionalized (S)-glutamate analogues by the kainate receptor GluK3 ligand-binding domain. / Venskutonyte, Raminta; Larsen, Anja Probst; Frydenvang, Karla Andrea; Gajhede, Michael; Gefflaut, Thierry; Pickering, Darryl S; Bunch, Lennart; Kastrup, Jette Sandholm Jensen.

    In: ChemMedChem, Vol. 9, No. 10, 2014, p. 2254-2259.

    Research output: Contribution to journalJournal articleResearchpeer-review

  29. Published

    Partial agonism and antagonism of the ionotropic glutamate receptor iGLuR5 : Structures of the ligand-bining core in complex with domoic acid and 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid. / Hald, Helle; Naur, Peter; Pickering, Darryl Scott; Sprogøe, Desiree; Madsen, Ulf; Timmermann, Daniel B.; Ahring, Philip K.; Liljefors, Tommy; Schousboe, Arne; Egebjerg, Jan; Gajhede, Michael; Kastrup, Jette Sandholm Jensen.

    In: Journal of Biological Chemistry, Vol. 282, No. 35, 2007, p. 25726-25736.

    Research output: Contribution to journalJournal articleResearchpeer-review

  30. Published

    Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors. / Juknaite, Lina; Venskutonyte, Raminta; Assaf, Zeinab; Faure, Sophie; Gefflaut, Thierry; Aitken, David J.; Nielsen, Birgitte; Gajhede, Michael; Kastrup, Jette Sandholm Jensen; Bunch, Lennart; Frydenvang, Karla; Pickering, Darryl S.

    In: Journal of Structural Biology, Vol. 180, No. 1, 2012, p. 39-46.

    Research output: Contribution to journalJournal articleResearchpeer-review

  31. Published

    Pharmacological characterisation of biarylisopropylalsulphonamide AMPA-R potentiators. / Pickering, Darryl S; Sanz, Contreraz; Harpsøe, Kasper; Clausen, Rasmus Prætorius; Sauerberg, P.; Liljefors, Tommy; Madsen, Ulf; Kaae, B.H.

    In: Journal of Neurochemistry, Vol. 102 (suppl. 1), No. 41, 2007.

    Research output: Contribution to journalConference abstract in journalResearch

  32. Published

    Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors : focus on subtypes iGlu5-7. / Bunch, Lennart; Gefflaut, Thierry; Alaux, Sebastien; Sagot, Emanuelle; Nielsen, Birgitte; Pickering, Darryl S.

    In: European Journal of Pharmacology, Vol. 609, 2009, p. 1-4.

    Research output: Contribution to journalJournal articleResearchpeer-review

  33. Published

    Rational Design, Synthesis and Pharmacological Evaluation of the (2R)- and (2S)-Stereoisomers of 3-(2-Carboxypyrrolidinyl)-2-methyl Acetic Acid as Ligands for the Ionotropic Glutamate Receptors. / Rasmussen, Julie; Storgaard, Morten; Pickering, Darryl S; Bunch, Lennart.

    In: ChemMedChem, Vol. 6, No. 3, 07.03.2011, p. 498-504.

    Research output: Contribution to journalJournal articleResearchpeer-review

  34. Published

    Selective kainate receptor (GluK1) ligands structurally based upon1H-Cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. / Venskutonyte, Raminta; Butini, Stefania; Coccone, Salvatore Sanna; Gemma, Sandra; Brindisi, Margherita; Kumar, Vinod; Guarino, Ergeria; Maramai, Samuele; Valenti, Salvatore; Amir, Ahmad; Valades, Elena Anton; Frydenvang, Karla Andrea; Kastrup, Jette Sandholm Jensen; Novellino, Ettore; Campiani, Giuseppe; Pickering, Darryl S.

    In: Journal of Medicinal Chemistry, Vol. 54, No. 13, 14.07.2011, p. 4793-4805.

    Research output: Contribution to journalJournal articleResearchpeer-review

  35. Published

    Simple cellemodeller for kommunikation i hjernen. / Schousboe, Arne; Madsen, Karsten Kirkegaard; Pickering, Darryl S.

    Bioteknologi - en temabog. ed. / Peder Gasbjerg; Gunnar Jensen; Annette Sørensen. Aarhus Danmark : Systime Academic, 2011. p. 98-107.

    Research output: Chapter in Book/Report/Conference proceedingBook chapterEducation

  36. Published

    Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain. / Krintel, Christian; Harpsøe, Kasper; Zachariassen, Linda G; Peters, Dan; Frydenvang, Karla; Pickering, Darryl S; Gajhede, Michael; Kastrup, Jette S.

    In: Acta crystallographica. Section D, Biological crystallography, Vol. 69, No. Pt 9, 09.2013, p. 1645-52.

    Research output: Contribution to journalJournal articleResearchpeer-review

  37. Published

    Structural and pharmacological characterization of phenylalanine-based AMPA receptor antagonists at kainate receptors. / Venskutonyte, Raminta; Frydenvang, Karla; Valadés, Elena Antón; Szymanska, Ewa Monika; Johansen, Tommy N; Kastrup, Jette S; Pickering, Darryl S.

    In: ChemMedChem, Vol. 7, No. 10, 10.2012, p. 1793-1798.

    Research output: Contribution to journalJournal articleResearchpeer-review

  38. Published

    Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites. / Kaae, Birgitte Høiriis; Harpsøe, Kasper; Kastrup, Jette Sandholm Jensen; Sanz, Alberto Contreras; Pickering, Darryl Scott; Metzler, Bjørn; Clausen, Rasmus Prætorius; Gajhede, Michael; Sauerberg, Per; Liljefors, Tommy; Madsen, Ulf.

    In: Chemistry & Biology, Vol. 14, No. 11, 2007, p. 1294-303.

    Research output: Contribution to journalJournal articleResearchpeer-review

  39. 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, Mads; Pickering, Darryl S; Mirza, Osman; Johansen, Tommy N; Greenwood, Jeremy; Vestergaard, Bente; Schousboe, Arne; Gajhede, Michael; Liljefors, Tommy; Kastrup, Jette S.

    In: Journal of Medicinal Chemistry, Vol. 51, No. 5, 2008, p. 1459-63.

    Research output: Contribution to journalJournal articleResearchpeer-review

  40. Published

    Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159 : asymmetric synthesis, neuroactivity, and structural characterization. / Juknaite, Lina; Sugamata, Yutaro; Tokiwa, Kazuya; Ishikawa, Yuichi; Takamizawa, Satoshi; Eng, Andrew; Sakai, Ryuichi; Pickering, Darryl S; Frydenvang, Karla; Swanson, Geoffrey T; Kastrup, Jette Sandholm Jensen; Oikawa, Masato.

    In: Journal of Medicinal Chemistry, Vol. 56, No. 6, 2013, p. 2283-2293.

    Research output: Contribution to journalJournal articleResearchpeer-review

  41. Published

    Targeting specific sub-domains of the GluA4 ionotropic glutamate receptor by murine Fab fragments. / Mohr, Andreas Ørgaard; Riise, Erik Skjold; Pickering, Darryl S; Jensen, Anders A.; Madden, Dean; Kastrup, Jette Sandholm Jensen; Clausen, Rasmus Prætorius; Skottrup, Peter Durand.

    2011. Poster session presented at Affinity2011, Tavira, Portugal.

    Research output: Contribution to conferencePosterResearchpeer-review

  42. Published

    The antagonistic effect of antipsychotic drugs on a HEK293 cell line stably expressing human alpha(1A1)-adrenoceptors. / Nourian, Zahra; Mulvany, Michael J; Nielsen, Karsten Bork; Pickering, Darryl S; Kristensen, Torsten.

    In: European Journal of Pharmacology, Vol. 596, No. 1-3, 2008, p. 32-40.

    Research output: Contribution to journalJournal articleResearchpeer-review

  43. Published

    The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue : synthesis, molecular pharmacology, and biostructural characterization. / Clausen, Rasmus Prætorius; Naur, Peter; Kristensen, Anders Skov; Greenwood, Jeremy R; Strange, Mette; Bräuner-Osborne, Hans; Jensen, Anders Asbjørn; Nielsen, Anne Sophie T; Geneser, Ulla; Ringgaard, Lone M; Nielsen, Birgitte; Pickering, Darryl S; Brehm, Lotte; Gajhede, Michael; Krogsgaard-Larsen, Povl; Kastrup, Jette Sandholm.

    In: Journal of Medicinal Chemistry, Vol. 52, No. 15, 2009, p. 4911-4922.

    Research output: Contribution to journalJournal articleResearchpeer-review

  44. Published

    The structure of a mixed GluR2 ligand-binding core dimer in complex with (S)-glutamate and the antagonist (S)-NS1209. / Kasper, Christina; Pickering, Darryl S; Mirza, Osman; Olsen, Lars; Kristensen, Anders S; Greenwood, Jeremy R; Liljefors, Tommy; Schousboe, Arne; Wätjen, Frank; Gajhede, Michael; Sigurskjold, Bent W; Kastrup, Jette S.

    In: Journal of Molecular Biology, Vol. 357, No. 4, 2006, p. 1184-201.

    Research output: Contribution to journalJournal articleResearchpeer-review

  45. Published

ID: 1299533