David E. Gloriam

David E. Gloriam

Professor


  1. 2016
  2. Published

    Total synthesis and structure–activity relationship studies of a series of selective G protein inhibitors

    Xiong, X., Zhang, H., Underwood, C. R., Harpsøe, Kasper, Gardella, T. J., Wöldike, M. F., Mannstadt, M., Gloriam, David E., Bräuner, Hans & Strømgaard, Kristian, 2016, In: Nature Chemistry. 8, 11, p. 1035-1041 7 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. 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

  4. 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

  5. Published

    Editorial overview: New technologies: GPCR drug design and function-exploiting the current (of) structures

    Tautermann, C. S. & Gloriam, David E., 2 Aug 2016, In: Current Opinion in Pharmacology. 30, p. 7-10 4 p.

    Research output: Contribution to journalComment/debateResearch

  6. 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

  7. 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

  8. 2017
  9. 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

  10. 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

  11. 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

  12. 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

  13. Published

    The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site

    Shehata, M. A., Jensen, A. C. N., Jespers, W., Floryan, L., Isberg, V., Andersen, K. B., Åqvist, J., Gutiérrez-de-Terán, H., Bräuner, Hans & Gloriam, David E., 25 Apr 2017, In: Scientific Reports. 7, 9 p., 1128.

    Research output: Contribution to journalJournal articleResearchpeer-review

  14. 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

  15. 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

  16. 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

  17. 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

  18. 2018
  19. 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

  20. 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

  21. Published

    Structure–activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359

    Zhang, H., Nielsen, A. L., Boesgaard, M. W., Harpsøe, Kasper, Daly, N. L., Xiong, X., Underwood, C. R., Haugaard-kedström, L. M., Bräuner, Hans, Gloriam, David E. & Strømgaard, Kristian, 2018, In: European Journal of Medicinal Chemistry. 156, p. 847-860

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. 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

  23. 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

  24. Published

    A Structural Framework for GPCR Chemogenomics: What’s In a Residue Number?

    Vass, M., Kooistra, Albert J., Verhoeven, S., Gloriam, David E., de Esch, I. J. P. & de Graaf, C., 1 Jan 2018, Methods in Molecular Biology. Humana Press, p. 73-113 41 p. (Methods in Molecular Biology, Vol. 1705).

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  25. 2019
  26. 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

  27. 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

  28. 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

  29. 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

  30. 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

  31. 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

  32. Published

    Pharmacology and function of the orphan GPR139 G protein-coupled receptor

    Vedel, L., Nøhr, A. C., Gloriam, David E. & Bräuner, Hans, 27 May 2019, In: Basic & Clinical Pharmacology & Toxicology. 126, p. 35-46

    Research output: Contribution to journalReviewResearchpeer-review

  33. 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

  34. Published

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

    Gaiser, B. I., Danielsen, Mia, 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

  35. 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

  36. 2020
  37. Published
  38. 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

  39. 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

  40. Published

    Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists

    Zhang, X., Belousoff, M. J., Zhao, P., Kooistra, A. J., Truong, T. T., Ang, S. Y., Underwood, C. R., Egebjerg, T., Šenel, P., Stewart, G. D., Liang, Y-L., Glukhova, A., Venugopal, H., Christopoulos, A., Furness, S. G. B., Miller, L. J., Reedtz-Runge, S., Langmead, C. J., Gloriam, D. E., Danev, R. & 2 others, Sexton, P. M. & Wootten, D., 2020, In: Molecular Cell. 80, 3, p. 485-500

    Research output: Contribution to journalJournal articleResearchpeer-review

  41. 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

  42. 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

  43. Published

    The European Research Network on Signal Transduction (ERNEST): Toward a Multidimensional Holistic Understanding of G Protein-Coupled Receptor Signaling

    Sommer, M. E., Selent, J., Carlsson, J., De Graaf, C., Gloriam, David E., Keseru, G. M., Kosloff, M., Mordalski, S., Rizk, A., Rosenkilde, Mette, Sotelo, E., Tiemann, Johanna Katarina Sofie, Tobin, A., Vardjan, N., Waldhoer, M. & Kolb, P., 2020, In: ACS Pharmacology & Translational Science. 3, 2, p. 361-370 10 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  44. 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

  45. 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

  46. 2021
  47. 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

  48. 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

  49. 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

  50. 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

  51. 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

  52. 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

  53. Published

    Structural dynamics bridge the gap between the genetic and functional levels of GPCRs

    Torrens-Fontanals, M., Stepniewski, T. M., Gloriam, David E. & Selent, J., 2021, In: Current Opinion in Structural Biology. 69, p. 150-159 10 p.

    Research output: Contribution to journalReviewResearchpeer-review

  54. Published

    Structural insights into the lipid and ligand regulation of serotonin receptors

    Xu, P., Huang, S., Zhang, H., Mao, C., Zhou, X. E., Cheng, X., Simon, Icaro A, Shen, D., Yen, H., Robinson, C. V., Harpsøe, Kasper, Svensson, B., Guo, J., Jiang, H., Gloriam, David E., Melcher, K., Jiang, Y., Zhang, Y. & Xu, H. E., 2021, In: Nature. 592, p. 469-473

    Research output: Contribution to journalJournal articleResearchpeer-review

  55. Published

    Structure of the class D GPCR Ste2 dimer coupled to two G proteins

    Velazhahan, V., Ma, N., Pándy-Szekeres, Gáspár, Kooistra, Albert J., Lee, Y., Gloriam, David E., Vaidehi, N. & Tate, C. G., 2021, In: Nature. 589, p. 148-153 +app 24 pp

    Research output: Contribution to journalJournal articleResearchpeer-review

  56. 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

ID: 5953796