David E. Gloriam

David E. Gloriam

Professor


  1. Published

    Identification and characterization of small molecular NPR-B receptor antagonists

    Andresen, H., Moltzau, L., Fagerheim, S., Gloriam, David E., Bach, T. & Levy, F., 1 Jan 2015, In: BMC Pharmacology and Toxicology. 16, Suppl 1, p. A70

    Research output: Contribution to journalJournal articleCommunication

  2. Published

    Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs

    Avet, C., Mancini, A., Breton, B., Le Gouill, C., Hauser, Alexander Sebastian, Normand, C., Kobayashi, H., Gross, F., Hogue, M., Lukasheva, V., St-Onge, S., Carrier, M., Héroux, M., Morissette, S., Fauman, E. B., Fortin, J. P., Schann, S., Leroy, X., Gloriam, David E. & Bouvier, M., 2022, In: eLife. 11, 34 p., e74101.

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    Creating a specialist protein resource network: a meeting report for the protein bioinformatics and community resources retreat

    Babbitt, P. C., Bagos, P. G., Bairoch, A., Bateman, A., Chatonnet, A., Chen, M. J., Craik, D. J., Finn, R. D., Gloriam, D., Haft, D. H., Henrissat, B., Holliday, G. L., Isberg, V., Kaas, Q., Landsman, D., Lenfant, N., Manning, G., Nagano, N., Srinivasan, N., O’Donovan, C. & 9 others, Pruitt, K. D., Sowdhamini, R., Rawlings, N. D., Saier, M. H., Sharman, J. L., Spedding, M., Tsirigos, Konstantinos, Vastermark, A. & Vriend, G., 18 May 2015, In: Database: The Journal of Biological Databases and Curation. 2015, p. 1-5 5 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Published

    Targeting the APP-Mint2 Protein-Protein Interaction with a Peptide-Based Inhibitor Reduces Amyloid-β Formation

    Bartling, Christian Reinhard Otto, Jensen, T. M. T., Henry, S. M., Colliander, A. L., Sereikaité, Vita, Wenzler, M., Jain, P., Maric, H. M., Harpsøe, Kasper, Pedersen, S. W., Clemmensen, L. S., Haugaard-Kedström, L. M., Gloriam, David E., Ho, A. & Strømgaard, Kristian, 2021, In: Journal of the American Chemical Society. 143, 2, p. 891-901

    Research output: Contribution to journalJournal articleResearchpeer-review

  5. Published

    Comprehensive Peptide Cyclization Examination Yields Optimized APP Scaffolds with Improved Affinity toward Mint2

    Bartling, Christian Reinhard Otto, Alexopoulou, Flora, Kuschert, S., Chin, Y. K. Y., Jia, X., Sereikaité, Vita, Özcelik, D., Jensen, T. M., Jain, P., Nygaard, M. M., Harpsøe, Kasper, Gloriam, David E., Mobli, M. & Strømgaard, Kristian, 2023, In: Journal of Medicinal Chemistry. 66, 4, p. 3045-3057

    Research output: Contribution to journalJournal articleResearchpeer-review

  6. Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse

    Bjarnadóttir, T. K., Gloriam, David E., Hellstrand, S. H., Kristiansson, H., Fredriksson, R. & Schiöth, H. B., Sep 2006, In: Genomics. 88, 3, p. 263-73 11 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  7. The human and mouse repertoire of the adhesion family of G-protein-coupled receptors

    Bjarnadóttir, T. K., Fredriksson, R., Höglund, P. J., Gloriam, David E., Lagerström, M. C. & Schiöth, H. B., Jul 2004, In: Genomics. 84, 1, p. 23-33 11 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  8. Published

    Delineation of molecular determinants for FR900359 inhibition of Gq/11 unlocks inhibition of Gαs

    Boesgaard, M. W., Harpsøe, Kasper, Malmberg, M., Underwood, C. R., Inoue, A., Mathiesen, Jesper M., König, G. M., Kostenis, E., Gloriam, David E. & Bräuner, Hans, 2020, In: Journal of Biological Chemistry. 295, 40, p. 13850-13861

    Research output: Contribution to journalJournal articleResearchpeer-review

  9. Published

    Minimum information about a protein affinity reagent (MIAPAR)

    Bourbeillon, J., Orchard, S., Benhar, I., Borrebaeck, C., de Daruvar, A., Dübel, S., Frank, R., Gibson, F., Gloriam, D. E. I., Haslam, N., Hiltker, T., Humphrey-Smith, I., Hust, M., Juncker, D., Koegl, M., Konthur, Z., Korn, B., Krobitsch, S., Muyldermans, S., Nygren, P-Å. & 14 others, Palcy, S., Polic, B., Rodriguez, H., Sawyer, A., Schlapshy, M., Snyder, M., Stoevesandt, O., Taussig, M. J., Templin, M., Uhlen, M., van der Maarel, S., Wingren, C., Hermjakob, H. & Sherman, D., 2010, In: Nature Biotechnology. 28, 7, p. 650-653

    Research output: Contribution to journalJournal articleResearch

  10. Published

    G protein-coupled receptor pharmacology-The next generation

    Bräuner, Hans, Rosenkilde, Mette, Gether, Ulrik & Gloriam, David E., 2020, In: Basic & Clinical Pharmacology & Toxicology. 126, Supplement 6, p. 3-4 2 p.

    Research output: Contribution to journalEditorialResearch

  11. Published

    A community Biased Signaling Atlas

    Caroli, J., Mamyrbekov, A., Harpsøe, Kasper, Gardizi, S., Dörries, L., Ghosh, E., Hauser, Alexander Sebastian, Kooistra, Albert J. & Gloriam, David E., 2023, In: Nature Chemical Biology. 19, p. 531–535

    Research output: Contribution to journalComment/debateResearchpeer-review

  12. Published

    Structure-Activity Relationships and Identification of Optmized CC-Chemokine Receptor CCR1, 5, and 8 Metal-Ion Chelators

    Chalikiopoulos, A., Thiele, S., Malmgaard-Clausen, M., Rydberg, P., Isberg, V., Ulven, Trond, Frimurer, Thomas Michael, Rosenkilde, Mette & Gloriam, David E., 25 Nov 2013, In: Journal of Chemical Information and Modeling. 53, 11, p. 2863-73 11 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  13. Published

    Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils

    Christensen, H. B., Gloriam, David E., Pedersen, D. S., Cowland, J. B., Borregaard, N. & Bräuner, Hans, 15 Jul 2017, In: Journal of Pharmacological and Toxicological Methods. 88, Pt 1, p. 72-78 7 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  14. Published

    Peptide inhibitors as tool compounds targeting GPCR signaling

    Daver, H., Harpsøe, Kasper & Gloriam, David E., 2021, In: European Biophysics Journal. 50, SUPPL 1, p. 161-161 238.

    Research output: Contribution to journalConference abstract in journalResearchpeer-review

  15. Published

    Present perspectives on the automated classification of the G-protein coupled receptors (GPCRs) at the protein sequence level

    Davies, M. N., Gloriam, David E., Secker, A., Freitas, A. A., Timmis, J. & Flower, D. R., 2011, In: Current Topics in Medicinal Chemistry. 11, 15, p. 1994-2009

    Research output: Contribution to journalJournal articleResearchpeer-review

  16. Published

    In silico identification of novel G protein-coupled receptors

    Davies, M. N., Gloriam, David E. & Flower, D. R., 2011, Methods for the discovery and characterization of G protein-coupled receptors. Stevens, C. W. (ed.). New York: Humana Press, Vol. 60. p. 3-18 (Neuromethods, Vol. 60).

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

  17. Proteomic applications of automated GPCR classification

    Davies, M. N., Gloriam, David E., Secker, A., Freitas, A. A., Mendao, M., Timmis, J. & Flower, D. R., Aug 2007, In: Proteomics. 7, 16, p. 2800-14 15 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  18. Published

    Structure–activity relationship of GPR15L peptide analogues and investigation of their interaction with the GPR15 receptor

    Deng, Y., Perez Almeria, C. V., van Gijzel, L., Schaller, Kay, Vedel, L., Gloriam, David E., Ulven, Trond & Bräuner, Hans, 2023, In: Basic and Clinical Pharmacology and Toxicology. 132, 6, p. 459-471

    Research output: Contribution to journalJournal articleResearchpeer-review

  19. Published

    Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide

    Di Giglio, M. G., Muttenthaler, M., Harpsøe, Kasper, Liutkeviciute, Z., Keov, P., Eder, T., Rattei, T., Arrowsmith, S., Wray, S., Marek, A., Elbert, T., Alewood, P. F., Gloriam, David E. & Gruber, C. W., 1 Feb 2017, In: Scientific Reports. 7, 15 p., 41002.

    Research output: Contribution to journalJournal articleResearchpeer-review

  20. Published

    Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors

    Falk-Petersen, C. B., Rostrup, F., Löffler, R., Buchleihtner, S., Harpsøe, Kasper, Gloriam, David E., Frølund, Bente & Wellendorph, Petrine, 2021, In: Molecular Pharmacology. 100, 1, p. 46-56

    Research output: Contribution to journalJournal articleResearchpeer-review

  21. Published

    Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors

    Falk-Petersen, C. B., Tsonkov, T. M., Nielsen, M. S., Harpsøe, Kasper, Bundgaard, C., Frølund, Bente, Kristiansen, Uffe, Gloriam, David E. & Wellendorph, Petrine, 22 Jun 2020, In: Scientific Reports. 10, 1, 12 p., 10078.

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. Published

    A new crystal structure fragment-based pharmacophore method for G protein-coupled receptors

    Fidom, K., Isberg, V., Hauser, Alexander Sebastian, Mordalski, S., Lehto, T., Bojarski, A. J. & Gloriam, David E., Jan 2015, In: Methods. 71, p. 104-112 9 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  23. Published

    Selectivity determinants of GPCR-G-protein binding

    Flock, T., Hauser, Alexander Sebastian, Lund, N., Gloriam, David E., Balaji, S. & Babu, M. M., 18 May 2017, In: Nature. 545, 7654, p. 317-322 6 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  24. Published

    Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors

    Foster, S. R., Hauser, Alexander Sebastian, Vedel, L., Strachan, R. T., Huang, X., Gavin, A. C., Shah, S. D., Nayak, A. P., Haugaard-Kedström, L. M., Penn, R. B., Roth, B. L., Bräuner, Hans & Gloriam, David E., 31 Oct 2019, In: Cell. 179, 4, p. 895-908

    Research output: Contribution to journalJournal articleResearchpeer-review

  25. Published

    Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method

    Frandsen, I. O., Boesgaard, M. W., Fidom, K., Hauser, Alexander Sebastian, Isberg, V., Bräuner, Hans, Wellendorph, Petrine & Gloriam, David E., 6 Jul 2017, In: Scientific Reports. 7, 1, 10 p., 4829.

    Research output: Contribution to journalJournal articleResearchpeer-review

  26. Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives

    Fredriksson, R., Höglund, P. J., Gloriam, David E., Lagerström, M. C. & Schiöth, H. B., 20 Nov 2003, In: F E B S Letters. 554, 3, p. 381-8 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  27. There exist at least 30 human G-protein-coupled receptors with long Ser/Thr-rich N-termini

    Fredriksson, R., Gloriam, David E., Höglund, P. J., Lagerström, M. C. & Schiöth, H. B., 14 Feb 2003, In: Biochemical and Biophysical Research Communications. 301, 3, p. 725-34 10 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  28. Published

    Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands

    Gaiser, B. I., Danielsen, M., Marcher, Emil, Røpke Jørgensen, K., Wróbel, T. M., Frykman, M., Johansson, H., Bräuner, Hans, Gloriam, David E., Mathiesen, Jesper M. & Sejer Pedersen, D., 12 Sep 2019, In: Journal of Medicinal Chemistry. 62, 17, p. 7806-7839 34 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  29. Published

    A ligand's view of target similarity: chemogenomic binding site-directed techniques for drug discovery

    Garland, S. L. & Gloriam, David E., 2011, In: Current Topics in Medicinal Chemistry. 11, 15, p. 1872-1881

    Research output: Contribution to journalJournal articleResearchpeer-review

  30. Published

    Methods for the successful application of chemogenomics to GPCR drug design

    Garland, S. L. (ed.) & Gloriam, David E. (ed.), 2011, In: Current Topics in Medicinal Chemistry. 11, 15, p. 1870-1871

    Research output: Contribution to journalEditorialResearch

  31. Published

    Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at gamma-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters

    Giraudo, A., Krall, J., Bavo, Francesco, Nielsen, Birgitte, Kongstad, Kenneth Thermann, Rolando, B., De Blasio, R., Gloriam, David E., Löffler, R., Thiesen, L., Harpsøe, Kasper, Frydenvang, Karla Andrea, Boschi, D., Wellendorph, Petrine, Lolli, M. L., Jensen, Anders A. & Frølund, Bente, 27 Jun 2019, In: Journal of Medicinal Chemistry. 62, 12, p. 5797-5809

    Research output: Contribution to journalJournal articleResearchpeer-review

  32. Published

    Bigger is better in virtual drug screens

    Gloriam, David E., Feb 2019, In: Nature. 566, p. 193-194 2 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  33. Published

    How can I teach to maximize the learning of “Roberts” (slow/nonambitious) and “Susans” (fast/ambitious)? Improving University Science Teaching and Learning - Pedagogical Projects 2008

    Gloriam, David E., 2008, Improving University Science Teaching and Learning - Pedagogical Projects 2008. Christiansen, F. V., Rump, C. & Degn, L. (eds.). København: Department of Science Education, University of Copenhagen, Denmark, Vol. 1. p. 227-244 18 p.

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

  34. Published

    Chemogenomics of allosteric binding sites in GPCRs

    Gloriam, David E., 2013, In: Drug Discovery Today: Technologies. 10, 2, p. e307-13

    Research output: Contribution to journalJournal articleResearchpeer-review

  35. High species variation within the repertoire of trace amine receptors

    Gloriam, David E., Bjarnadóttir, T. K., Schiöth, H. B. & Fredriksson, R., Apr 2005, In: Annals of the New York Academy of Sciences. 5 p.

    Research output: Contribution to journalConference articleResearch

  36. Published

    The repertoire of trace amine G-protein-coupled receptors: large expansion in zebrafish

    Gloriam, David E., Bjarnadóttir, T. K., Yan, Y., Postlethwait, J. H., Schiöth, H. B. & Fredriksson, R., May 2005, In: Molecular Phylogenetics and Evolution. 35, 2, p. 470-82 13 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  37. Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship

    Gloriam, David E., Schiöth, H. B. & Fredriksson, R., 15 Apr 2005, In: BBA General Subjects. 1722, 3, p. 235-46 12 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  38. The G protein-coupled receptor subset of the rat genome

    Gloriam, David E., Fredriksson, R. & Schiöth, H. B., 2007, In: B M C Genomics. 8, p. 338

    Research output: Contribution to journalJournal articleResearchpeer-review

  39. Published

    Chemogenomic discovery of allosteric antagonists at the GPRC6A receptor

    Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Thomsen, A. R. B., Phonekeo, K., Pedersen, D. S. & Bräuner, Hans, 23 Nov 2011, In: Chemistry & Biology. 18, 11, p. 1489-1498

    Research output: Contribution to journalJournal articleResearchpeer-review

  40. Published

    Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design

    Gloriam, David E., Foord, S. M., Blaney, F. E. & Garland, S. L., 2009, In: Journal of Medicinal Chemistry. 52, 14, p. 4429-4442

    Research output: Contribution to journalJournal articleResearchpeer-review

  41. Published

    Kemogenomik: receptoren set fra lægemiddelstoffets synspunkt

    Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Pedersen, D. S. & Bräuner, Hans, Dec 2010, In: Lægemiddelforskning. 2010, p. 28-30

    Research output: Contribution to journalJournal articleCommunication

  42. Published

    A community standard format for the representation of protein affinity reagents

    Gloriam, D. E. I., Orchard, S., Bertinetti, D., Björling, E., Bongcam-Rudloff, E., Borrebaeck, C. A. K., Bourbeillon, J., Bradbury, A. R. M., de Daruvar, A., Dübel, S., Frank, R., Gibson, T. J., Gold, L., Haslam, N., Herberg, F. W., Hiltke, T., Hoheisel, J. D., Kerrien, S., Koegl, M., Konthur, Z. & 16 others, Korn, B., Landegren, U., Montecchi-Palazzi, L., Palcy, S., Rodriguez, H., Schweinsberg, S., Sievert, V., Stoevesandt, O., Taussig, M. J., Ueffing, M., Uhlén, M., van der Maarel, S., Wingren, C., Woollard, P., Sherman, D. J. & Hermjakob, H., 2010, In: Molecular and Cellular Proteomics. 9, 1, p. 1-10

    Research output: Contribution to journalJournal articleResearchpeer-review

  43. Published

    Pathway selectivity in Frizzleds is achieved by conserved micro-switches defining pathway-determining, active conformations

    Grätz, L., Kowalski-Jahn, M., Scharf, M. M., Kozielewicz, P., Jahn, M., Bous, J., Lambert, N. A., Gloriam, David E. & Schulte, G., 2023, In: Nature Communications. 14, 1, 17 p., 4573.

    Research output: Contribution to journalJournal articleResearchpeer-review

  44. The G protein-coupled receptor subset of the dog genome is more similar to that in humans than rodents

    Haitina, T., Fredriksson, R., Foord, S. M., Schiöth, H. B. & Gloriam, David E., 2009, In: B M C Genomics. 10, p. 24

    Research output: Contribution to journalJournal articleResearchpeer-review

  45. Published

    Structural insight to mutation effects uncover a common allosteric site in class C GPCRs

    Harpsøe, Kasper, Boesgaard, M. W., Munk, C., Bräuner, Hans & Gloriam, David E., 2017, In: Bioinformatics (Oxford, England). 33, 8, p. 1116-1120 5 p., btw784.

    Research output: Contribution to journalJournal articleResearchpeer-review

  46. Published

    Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors - A Structural Perspective of Ligands and Mutants

    Harpsøe, Kasper, Isberg, V., Tehan, B. G., Weiss, D., Arsova, A., Marshall, F. H., Bräuner, Hans & Gloriam, David E., 11 Sep 2015, In: Scientific Reports. 5, p. 1-11 11 p., 13869.

    Research output: Contribution to journalJournal articleResearchpeer-review

  47. Published

    GPCR activation mechanisms across classes and macro/microscales

    Hauser, Alexander Sebastian, Kooistra, Albert J., Munk, C., Heydenreich, F. M., Veprintsev, D. B., Bouvier, M., Babu, M. M. & Gloriam, David E., 2021, In: Nature Structural and Molecular Biology. 28, 11, p. 879-888

    Research output: Contribution to journalJournal articleResearchpeer-review

  48. Published

    Common coupling map advances GPCR-G protein selectivity

    Hauser, Alexander Sebastian, Avet, C., Normand, C., Mancini, A., Inoue, A., Bouvier, M. & Gloriam, David E., 2022, In: eLife. 11, 22 p., e74107.

    Research output: Contribution to journalJournal articleResearchpeer-review

  49. Published

    Novel approaches leading towards peptide GPCR de-orphanisation

    Hauser, Alexander Sebastian, Gloriam, David E., Bräuner, Hans & Foster, S. R., 1 Mar 2020, In: British Journal of Pharmacology. 177, 5, p. 961-968 8 p.

    Research output: Contribution to journalReviewResearchpeer-review

  50. Published

    Pharmacogenomics of GPCR Drug Targets

    Hauser, Alexander Sebastian, Chavali, S., Masuho, I., Jahn, L., Martemyanov, K., Gloriam, David E. & Babu, M., Jan 2018, In: Cell. 172, p. 41–54

    Research output: Contribution to journalJournal articleResearchpeer-review

  51. Published

    Trends in GPCR drug discovery: new agents, targets and indications

    Hauser, Alexander Sebastian, Gloriam, David E., Attwood, M. M., Rask-Andersen, M. & Schiöth, H. B., 27 Oct 2017, In: Nature Reviews. Drug Discovery. 16, p. 829-842 14 p., 178.

    Research output: Contribution to journalJournal articleResearchpeer-review

  52. Published

    GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors

    Huang, S., Xu, P., Shen, D., Simon, I. A., Mao, C., Tan, Y., Zhang, H., Harpsøe, Kasper, Li, H., Zhang, Y., You, C., Yu, X., Jiang, Y., Zhang, Y., Gloriam, David E. & Xu, H. E., 2022, In: Molecular Cell. 82, 14, p. 2681-2695.e6 15 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  53. Published

    Structure-activity relationships of constrained phenylethylamine ligands for the serotonin 5-ht2 receptors

    Isberg, V., Paine, J., Leth-Petersen, S., Kristensen, Jesper Langgaard & Gloriam, David E., 2013, In: P L o S One. 8, 11, e78515.

    Research output: Contribution to journalJournal articleResearchpeer-review

  54. Published

    Generic GPCR residue numbers - aligning topology maps while minding the gaps

    Isberg, V., de Graaf, C., Bortolato, A., Cherezov, V., Katritch, V., Marshall, F. H., Mordalski, S., Pin, J., Stevens, R. C., Vriend, G. & Gloriam, David E., 1 Jan 2015, In: Trends in Pharmacological Sciences. 36, 1, p. 22-31 10 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  55. Published

    GPCRdb: an information system for G protein-coupled receptors

    Isberg, V., Mordalski, S., Munk, C., Rataj, K., Harpsøe, Kasper, Hauser, Alexander Sebastian, Vroling, B., Bojarski, A. J., Vriend, G. & Gloriam, David E., 4 Jan 2016, In: Nucleic Acids Research. 44, D1, p. D356-64

    Research output: Contribution to journalJournal articleResearchpeer-review

  56. Published

    Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties

    Jensen, Anders A., Plath, N., Pedersen, M. H. F., Isberg, V., Krall, J., Wellendorph, Petrine, Stensbøl, T. B., Gloriam, David E., Krogsgaard-Larsen, Povl & Frølund, Bente, 14 Feb 2013, In: Journal of Medicinal Chemistry. 56, 3, p. 1211-27 17 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  57. Published

    The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW

    Jensen, A. C. N., Shehata, M. A., Hauser, Alexander Sebastian, Isberg, V., Mokrosinski, J., Farooqi, I. S., Pedersen, D. S., Gloriam, David E. & Bräuner, Hans, 1 Jan 2017, In: Neurochemistry International. 102, p. 105-113

    Research output: Contribution to journalJournal articleResearchpeer-review

  58. Published

    Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

    Jespers, W., Schiedel, A. C., Heitman, L. H., Cooke, R. M., Kleene, L., van Westen, G. J. P., Gloriam, David E., Müller, C. E., Sotelo, E. & Gutiérrez-de-Terán, H., Jan 2018, In: Trends in Pharmacological Sciences. 39, 1, p. 75-89

    Research output: Contribution to journalReviewResearchpeer-review

  59. Published

    Kemogenomik: Receptoren set fra lægemiddelstoffets synspunkt

    Johansson, H., Jørgensen, T. B., Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Pedersen, D. S. & Bräuner, Hans, 2011, In: Dansk Kemi. 92, 11, p. 22-26

    Research output: Contribution to journalJournal articleResearch

  60. Published

    Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold

    Johansson, H., Boesgaard, M. W., Nørskov-Lauritsen, L., Larsen, I., Kuhne, S., Gloriam, David E., Bräuner, Hans & Sejer Pedersen, D., 25 Nov 2015, In: Journal of Medicinal Chemistry. 58, 22, p. 8938-51 14 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  61. Published

    3-Substituted 2-phenyl-indoles: Privileged structures for medicinal chemistry

    Johansson, K. H., Jørgensen, T. B., Gloriam, David E., Bräuner, Hans & Pedersen, D. S., 21 Jan 2013, In: R S C Advances. 3, 3, p. 945-960

    Research output: Contribution to journalJournal articleResearchpeer-review

  62. Published

    Structure-activity relationships for negative allosteric mGluR5 modulators

    Kaae, B. H., Harpsøe, Kasper, Kvist, T., Mathiesen, Jesper M., Mølck, C., Gloriam, David E., Jimenez, H. N., Uberti, M. A., Nielsen, S. M., Nielsen, Birgitte, Bräuner, Hans, Sauerberg, P., Clausen, Rasmus Prætorius & Madsen, Ulf, 2012, In: ChemMedChem. 7, 3, p. 440-451

    Research output: Contribution to journalJournal articleResearchpeer-review

  63. Published

    Community guidelines for GPCR ligand bias: IUPHAR review 32

    Kolb, P., Kenakin, T., Alexander, S. P. H., Bermudez, M., Bohn, L. M., Breinholt, C. S., Bouvier, M., Hill, S. J., Kostenis, E., Martemyanov, K. A., Neubig, R. R., Onaran, H. O., Rajagopal, S., Roth, B. L., Selent, J., Shukla, A. K., Sommer, M. E. & Gloriam, David E., 2022, In: British Journal of Pharmacology. 179, 14, p. 3651-3674

    Research output: Contribution to journalReviewResearchpeer-review

  64. Published

    GPCRdb in 2021: integrating GPCR sequence, structure and function

    Kooistra, Albert J., Mordalski, S., Pándy-Szekeres, Gáspár, Esguerra, M., Mamyrbekov, A., Munk, C., Keserű, G. M. & Gloriam, David E., 2021, In: Nucleic Acids Research. 49, D1, p. D335-D343

    Research output: Contribution to journalJournal articleResearchpeer-review

  65. Published

    An online GPCR structure analysis platform

    Kooistra, Albert J., Munk, C., Hauser, Alexander Sebastian & Gloriam, David E., 2021, In: Nature Structural and Molecular Biology. 28, 11, p. 875-878

    Research output: Contribution to journalJournal articleResearchpeer-review

  66. Published

    Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites

    Krall, J., Bavo, Francesco, Falk-Petersen, C. B., Jensen, C. H., Nielsen, J. O., Tian, Yongsong, Anglani, V., Kongstad, Kenneth Thermann, Petersen, Louise Piilgaard, Nielsen, Birgitte, Gloriam, David E., Kehler, J., Jensen, Anders A., Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 14 Mar 2019, In: Journal of Medicinal Chemistry. 62, 5, p. 2798-2813

    Research output: Contribution to journalJournal articleResearchpeer-review

  67. Published

    Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs

    Krall, J., Jensen, C. H., Bavo, F., Falk-Petersen, C. B., Haugaard, A. S., Vogensen, S. B., Tian, Y., Nittegaard-Nielsen, M., Sigurdardóttir, S. B., Kehler, J., Kongstad, Kenneth Thermann, Gloriam, David E., Clausen, Rasmus Prætorius, Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 9022-9039 18 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  68. Published

    Advances in GPCR modeling evaluated by the GPCR Dock 2013 assessment: meeting new challenges

    Kufareva, I., Katritch, V., Biggin, P., Kim, M., Park, K., Jung, S. W., Cho, A. E., Sands, Z. A., Ostopovici-Halip, L., Bologa, C. G., Norn, C., Brylinski, M., Skolnick, J., Keränen, H., Lenselink, B. E., Van Westen, G., Overington, J. P., De Teráán, H. G., Isberg, V., Fidom, K. M. & 96 others, Lehto, T. M., Gloriam, David E., Ghosh, A., Sonavane, U., Joshi, R., Xia, J., Hsieh, J. H., Zhang, L., Wang, X. S., Vogel, H., Yuan, S., Feng, X., Chen, M., Ambia, J., Barth, P., Gageat, C., Stepniewski, M., Xhaard, H., Kelm, S., Pitt, W. R., Shi, J., Larsen, A., Li, H., Wagner, J., Bhattacharya, S., Vaidehi, N., Kanou, K., Cvicek, V., Kim, S. K., Trzaskowski, B., Goddard, W. A., Abrol, R., Selvam, B., Tikhonova, I. G., Cuzzolin, A., Sabbadin, D., Ciancetta, A., Moro, S., Freyd, T., Gabrielsen, M., Kristiansen, K., Sylte, I., Gaffney, K. J., Petasis, N. A., Latek, D., Bajda, M., Młynarczyk, K., Filipek, S., López, L., Kuiper, M., Beuming, T., Perez-Aguilar, J. M., Wang, R. Y. R., Park, H., Greisen, P., Song, Y., DiMaio, F., Baker, D., Shin, W. H., Heo, L., Lee, G. R., Seok, C., Yang, J., Zhang, Y., Ponassi, M., Rosano, C., Cheremovskiy, G., Grudinin, S., Chaudhari, R., Heim, A. J., Li, Z., Lv, Q., Grigorov, M. G., Hu, X., Sun, H., Shen, M., Southall, N., Jadhav, A., Rodríguez, D., Ranganathan, A., Carlsson, J., Najmanovich, R., Durdagi, S., De March, C., Diharce, J., Golebiowski, J., Antonczak, S., Fiorucci, S., Nguyen, E., Meiler, J., Gutcaits, A., Marti-Solano, M., Pastor, M., Selent, J., Stevens, R. C. & Abagyan, R., 2014, In: Structure. 22, 8, p. 1120-1139 20 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  69. The G protein-coupled receptor subset of the chicken genome

    Lagerström, M. C., Hellström, A. R., Gloriam, David E., Larsson, T. P., Schiöth, H. B. & Fredriksson, R., 2 Jun 2006, In: P L o S Computational Biology (Online). 2, 6, p. e54

    Research output: Contribution to journalJournal articleResearchpeer-review

  70. Published
  71. Published

    Receptor selectivity between the G proteins Gα 12 and Gα 13 is defined by a single leucine-to-isoleucine variation

    Mackenzie, A. E., Quon, T., Lin, L. C., Hauser, Alexander Sebastian, Jenkins, L., Inoue, A., Tobin, A. B., Gloriam, David E., Hudson, B. D. & Milligan, G., 1 Apr 2019, In: FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 33, 4, p. 5005-5017 13 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  72. Published

    Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

    Malfacini, D., Patt, J., Annala, S., Harpsøe, Kasper, Eryilmaz, F., Reher, R., Crüsemann, M., Hanke, W., Zhang, H., Tietze, D., Gloriam, David E., Bräuner, Hans, Strømgaard, Kristian, König, G. M., Inoue, A., Gomeza, J. & Kostenis, E., 12 Apr 2019, In: The Journal of Biological Chemistry. 294, 15, p. 5747-5758

    Research output: Contribution to journalJournal articleResearchpeer-review

  73. Published

    Combinatorial expression of GPCR isoforms affects signalling and drug responses

    Marti-Solano, M., Crilly, S. E., Malinverni, D., Munk, C., Harris, M., Pearce, A., Quon, T., Mackenzie, A. E., Wang, X., Peng, J., Tobin, A. B., Ladds, G., Milligan, G., Gloriam, David E., Puthenveedu, M. A. & Babu, M. M., 2020, In: Nature. 587, p. 650-656 28 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  74. Published

    Binding Mode of a Novel MPEP-Derived Metabotropic Glutamate Receptor Subtype 5 (mGluR5) NAM, 1,3-Bis(pyridin-2-ylethynyl)Benzene

    Molck, C., Harpsøe, Kasper, Gloriam, David E., Kaae, B. H., Jimenez, H. N., Uberti, M. A., Topiol, S., Clausen, Rasmus Prætorius, Madsen, Ulf, Nielsen, S. M., Mathiesen, Jesper M. & Bräuner, Hans, Sep 2011, In: Current Neuropharmacology. 9, p. 43-43

    Research output: Contribution to journalConference abstract in journalResearch

  75. Published

    GPCRdb: The G protein-coupled receptor database - an introduction

    Munk, C., Isberg, V., Mordalski, S., Harpsøe, Kasper, Rataj, K., Hauser, Alexander Sebastian, Kolb, P., Bojarski, A. J., Vriend, G. & Gloriam, David E., Jul 2016, In: British Journal of Pharmacology. 173, 14, p. 2195-207 13 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  76. Published

    Integrating structural and mutagenesis data to elucidate GPCR ligand binding

    Munk, C., Harpsøe, Kasper, Hauser, Alexander Sebastian, Isberg, V. & Gloriam, David E., Oct 2016, In: Current Opinion in Pharmacology. 30, p. 51-58 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  77. Published

    An online resource for GPCR structure determination and analysis

    Munk, C., Mutt, E., Isberg, V., Nikolajsen, L. F., Bibbe, J. M., Flock, T., Hanson, M. A., Stevens, R. C., Deupi, X. & Gloriam, David E., 2019, In: Nature Methods. 16, 2, p. 151-162

    Research output: Contribution to journalReviewResearchpeer-review

  78. Published

    Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

    Mølck, C., Harpsøe, Kasper, Gloriam, David E., Clausen, Rasmus Prætorius, Madsen, Ulf, Pedersen, L., Jimenez, H. N., Nielsen, S. M., Mathiesen, Jesper M. & Bräuner, Hans, 2012, In: Molecular Pharmacology. 82, 5, p. 929-37 9 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  79. Published

    mGluR5: Exploration of Orthosteric and Allosteric Ligand Binding Pockets and Their Applications to Drug Discovery

    Mølck, C., Harpsøe, Kasper, Gloriam, David E., Mathiesen, Jesper M., Nielsen, S. M. & Bräuner, Hans, Oct 2014, In: Neurochemical Research. 39, 10, p. 1862-1875 14 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  80. Published

    A novel red fluorescence dopamine biosensor selectively detects dopamine in the presence of norepinephrine in vitro

    Nakamoto, C., Goto, Y., Tomizawa, Y., Fukata, Y., Fukata, M., Harpsøe, Kasper, Gloriam, David E., Aoki, K. & Takeuchi, T., 2021, In: Molecular Brain. 14, 1, 14 p., 173.

    Research output: Contribution to journalJournal articleResearchpeer-review

  81. Published

    Critical evaluation of the FANTOM3 non-coding RNA transcripts

    Nordström, K. J. V., Mirza, M. A. I., Almén, M. S., Gloriam, David E., Fredriksson, R. & Schiöth, H. B., 2009, In: Genomics. 94, 3, p. 169-176

    Research output: Contribution to journalJournal articleResearchpeer-review

  82. Published

    Comprehensive comparisons of the current human, mouse, and rat RefSeq, Ensembl, EST, and FANTOM3 datasets: identification of new human genes with specific tissue expression profile

    Nordström, K. J. V., Mirza, M. A. I., Larsson, T. P., Gloriam, David E., Fredriksson, R. & Schiöth, H. B., 29 Sep 2006, In: Biochemical and Biophysical Research Communications. 348, 3, p. 1063-74 12 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  83. Published

    Identification of a novel scaffold for a small molecule GPR139 receptor agonist

    Nøhr, A. C., Shehata, M. A., Palmer, D., Pokhrel, R., Vallianou, M., Foster, S. R., Gentry, P. R., Gloriam, David E. & Bräuner, Hans, 7 Mar 2019, In: Scientific Reports. 9, 1, 10 p., 3802.

    Research output: Contribution to journalJournal articleResearchpeer-review

  84. Published

    Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139

    Pallareti, L., Rath, T. F., Trapkov, Boris, Tsonkov, T., Nielsen, A. T., Harpsøe, Kasper, Gentry, P. R., Bräuner, Hans, Gloriam, David E. & Foster, S. R., 2023, In: European Journal of Pharmacology. 943, 175553.

    Research output: Contribution to journalJournal articleResearchpeer-review

  85. Published

    The G protein database, GproteinDb

    Pándy-Szekeres, Gáspár, Esguerra, M., Hauser, Alexander Sebastian, Caroli, J., Munk, C., Pilger, S., Keseru, G. M., Kooistra, Albert J. & Gloriam, David E., 2022, In: Nucleic Acids Research. 50, D1, p. D518-D525

    Research output: Contribution to journalJournal articleResearchpeer-review

  86. Published

    5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology

    Peng, Y., McCorvy, J. D., Harpsøe, K., Lansu, K., Yuan, S., Popov, P., Qu, L., Pu, M., Che, T., Nikolajsen, L. F., Huang, X., Wu, Y., Shen, L., Bjørn-Yoshimoto, W. E., Ding, K., Wacker, D., Han, G. W., Cheng, J., Katritch, V., Jensen, A. A. & 6 others, Hanson, M. A., Zhao, S., Gloriam, David E., Roth, B. L., Stevens, R. C. & Liu, Z., 2018, In: Cell. 172, 4, p. 719-730 P719-730.E14.

    Research output: Contribution to journalJournal articleResearchpeer-review

  87. Published

    Structure–Activity Assessment and In-Depth Analysis of Biased Agonism in a Set of Phenylalkylamine 5-HT2A Receptor Agonists

    Pottie, E., Poulie, Christian Bernard Matthijs, Simon, Ícaro Ariel, Harpsøe, Kasper, D’Andrea, L., Komarov, I. V., Gloriam, David E., Jensen, Anders A., Kristensen, Jesper Langgaard & Stove, C. P., 2023, In: ACS Chemical Neuroscience. 14, 15, p. 2727–2742

    Research output: Contribution to journalJournal articleResearchpeer-review

  88. Published

    Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT2A Receptor Agonists

    Poulie, Christian Bernard Matthijs, Pottie, E., Simon, I. A., Harpsøe, Kasper, D’andrea, L., Komarov, I. V., Gloriam, David E., Jensen, Anders A., Stove, C. P. & Kristensen, Jesper Langgaard, 2022, In: Journal of Medicinal Chemistry. 65, 18, p. 12031–12043

    Research output: Contribution to journalJournal articleResearchpeer-review

  89. Published

    GproteinDb in 2024: new G protein-GPCR couplings, AlphaFold2-multimer modelsãnd interface interactions

    Pándy-Szeker es, G., Taracena Herrera, Luis Pablo, Caroli, J., Kermani, A. A., Kulkarni, Yashraj, Keseru, G. M. & Gloriam, David E., 2024, In: Nucleic Acids Research. 52, D1, p. D466-D475

    Research output: Contribution to journalJournal articleResearchpeer-review

  90. Published

    GPCRdb in 2018: adding GPCR structure models and ligands

    Pándy-Szekeres, Gáspár, Munk, C., Tsonkov, T. M., Mordalski, S., Harpsøe, Kasper, Hauser, Alexander Sebastian, Bojarski, A. J. & Gloriam, David E., 2018, In: Nucleic Acids Research. 46, D1, 7 p., gkx1109.

    Research output: Contribution to journalJournal articleResearchpeer-review

  91. Published

    GPCRdb in 2023: state-specific structure models using AlphaFold2 and new ligand resources

    Pándy-Szekeres, Gáspár, Caroli, J., Mamyrbekov, A., Kermani, A. A., Keserű, G. M., Kooistra, Albert J. & Gloriam, David E., 2023, In: Nucleic Acids Research. 51, D1, p. D395–D402

    Research output: Contribution to journalJournal articleResearchpeer-review

  92. Published

    GPCRmd uncovers the dynamics of the 3D-GPCRome

    Rodríguez-Espigares, I., Torrens-Fontanals, M., Tiemann, J. K. S., Aranda-García, D., Ramírez-Anguita, J. M., Stepniewski, T. M., Worp, N., Varela-Rial, A., Morales-Pastor, A., Medel-Lacruz, B., Pándy-Szekeres, G., Mayol, E., Giorgino, T., Carlsson, J., Deupi, X., Filipek, S., Filizola, M., Gómez-Tamayo, J. C., Gonzalez, A., Gutiérrez-de-Terán, H. & 27 others, Jiménez-Rosés, M., Jespers, W., Kapla, J., Khelashvili, G., Kolb, P., Latek, D., Marti-Solano, M., Matricon, P., Matsoukas, M., Miszta, P., Olivella, M., Perez-Benito, L., Provasi, D., Ríos, S., Torrecillas, I. R., Sallander, J., Sztyler, A., Vasile, S., Weinstein, H., Zachariae, U., Hildebrand, P. W., De Fabritiis, G., Sanz, F., Gloriam, David E., Cordomi, A., Guixà-González, R. & Selent, J., 2020, In: Nature Methods. 17, 8, p. 777-787

    Research output: Contribution to journalJournal articleResearchpeer-review

  93. Published

    Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors

    Rostrup, F., Falk-petersen, C. B., Harpsøe, Kasper, Buchleithner, S., Conforti, I., Jung, S., Gloriam, David E., Schirmeister, T., Wellendorph, Petrine & Frølund, Bente, 22 Apr 2021, In: Journal of Medicinal Chemistry. 64, 8, p. 4730-4743 14 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  94. Published

    SMARTCyp web service

    Rydberg, P., Gloriam, David E. & Olsen, L., 2010

    Research output: Non-textual formInteractive productionResearch

  95. Published

    The contribution of atom accessibility to site of metabolism models for cytochromes P450

    Rydberg, P., Rostkowski, M., Gloriam, David E. & Olsen, L., 1 Apr 2013, In: Molecular Pharmaceutics. 10, 4, p. 1216-1223 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  96. Published

    The SMARTCyp cytochrome P450 metabolism prediction server

    Rydberg, P., Gloriam, David E. & Olsen, L., 1 Dec 2010, In: Bioinformatics. 26, 23, p. 2988-2989

    Research output: Contribution to journalLetterResearchpeer-review

  97. Published

    SMARTCyp: A 2D method for prediction of cytochrome P450-mediated drug metabolism

    Rydberg, P., Gloriam, David E., Zaretzki, J., Breneman, C. & Olsen, L., 15 Mar 2010, In: ACS Medicinal Chemistry Letters. 1, 3, p. 96-100

    Research output: Contribution to journalLetterResearchpeer-review

  98. Published

    Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity

    Sandhu, M., Cho, A., Ma, N., Mukhaleva, E., Namkung, Y., Lee, S., Ghosh, S., Lee, J. H., Gloriam, David E., Laporte, S. A., Babu, M. M. & Vaidehi, N., 2022, In: Nature Communications. 13, 1, 14 p., 7428.

    Research output: Contribution to journalJournal articleResearchpeer-review

  99. Published

    Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139

    Shehata, M. A., Jensen, A. C. N., Lissa, D., Bisig, C., Isberg, V., Andersen, K. B., Harpsøe, Kasper, Björkling, Fredrik, Bräuner, Hans & Gloriam, David E., 10 Nov 2016, In: Scientific Reports. 6, p. 1-13 13 p., 36681.

    Research output: Contribution to journalJournal articleResearchpeer-review

  100. Published

    Identification of the first surrogate agonists for the G protein-coupled receptor GPR132

    Shehata, M. A., Christensen, H. B., Isberg, V., Pedersen, D. S., Bender, A., Bräuner, Hans & Gloriam, David E., 2015, In: RSC Advances. 5, p. 48551-48557 7 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

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