David E. Gloriam

David E. Gloriam

Professor


  1. 2024
  2. 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

  3. 2023
  4. 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

  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. 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

  7. Published

    Ligand selectivity hotspots in serotonin GPCRs

    Simon, Ícaro Ariel, Bjørn-Yoshimoto, Walden, Harpsøe, Kasper, Iliadis, S., Svensson, B., Jensen, Anders A. & Gloriam, David E., 2023, In: Trends in Pharmacological Sciences. 44, 12, p. 978-990

    Research output: Contribution to journalReviewResearchpeer-review

  8. 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

  9. 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

  10. 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

  11. 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

  12. 2022
  13. 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

  14. 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

  15. 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

  16. 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

  17. 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

  18. 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

  19. Published

    Ligand-directed bias of G protein signaling at the dopamine D2 receptor

    Moo, Ee Von, Harpsøe, Kasper, Hauser, Alexander Sebastian, Masuho, I., Bräuner, Hans, Gloriam, David E. & Martemyanov, K. A., 2022, In: Cell Chemical Biology. 29, 2, p. 226-238

    Research output: Contribution to journalJournal articleResearchpeer-review

  20. Published

    Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139

    Zhou, Y., Daver, H., Trapkov, B., Wu, L., Wu, M., Harpsøe, Kasper, Gentry, P. R., Liu, K., Larionova, M., Liu, J., Chen, N., Bräuner, Hans, Gloriam, David E., Hua, T. & Liu, Z. J., 2022, In: Cell Research. 32, 2, p. 210-213

    Research output: Contribution to journalLetterResearchpeer-review

  21. 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

  22. 2021
  23. 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

  24. 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

  25. 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

  26. 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

  27. 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

  28. 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

  29. 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

  30. 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

  31. 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, I. 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

  32. 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

  33. 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

  34. 2020
  35. 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

  36. 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

  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. 2019
  45. 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

  46. 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

  47. 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

  48. 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

  49. 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

  50. 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

  51. 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

  52. 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

  53. 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

  54. 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

  55. 2018
  56. 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

  57. 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

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ID: 5953796