David E. Gloriam

David E. Gloriam

Professor

ORCID: 0000-0002-4299-7561

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  1. 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 journal › Journal article › Research › peer-review

  2. 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 journal › Journal article › Research › peer-review

  3. 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 journal › Journal article › Research › peer-review

  4. 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 journal › Journal article › Research › peer-review

  5. 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 journal › Journal article › Research › peer-review

  6. 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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-review

  8. 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 journal › Journal article › Research › peer-review

  9. 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 journal › Letter › Research › peer-review

  10. 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 journal › Journal article › Research › peer-review

  11. 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 journal › Journal article › Research › peer-review

  12. 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 journal › Journal article › Research › peer-review

  13. 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 journal › Journal article › Research › peer-review

  14. 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 journal › Journal article › Research › peer-review

  15. 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 journal › Journal article › Research › peer-review

  16. 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 journal › Journal article › Research › peer-review

  17. 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 journal › Journal article › Research › peer-review

  18. 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 journal › Journal article › Research › peer-review

  19. 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, Icaro A, 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 journal › Journal article › Research › peer-review

  20. 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 journal › Journal article › Research › peer-review

  21. 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 journal › Journal article › Research › peer-review

  22. 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 journal › Journal article › Research › peer-review

  23. 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 journal › Journal article › Research › peer-review

  24. 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 journal › Journal article › Research › peer-review

  25. 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 journal › Journal article › Research › peer-review

  26. 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 journal › Review › Research › peer-review

  27. 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 journal › Review › Research › peer-review

  28. 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 journal › Journal article › Research › peer-review

  29. 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 journal › Journal article › Research › peer-review

  30. 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 journal › Journal article › Research › peer-review

  31. 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 journal › Journal article › Research › peer-review

  32. 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 journal › Journal article › Research › peer-review

  33. Published

    SMARTCyp web service

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

    Research output: Non-textual form › Interactive production › Research

  34. 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 journal › Letter › Research › peer-review

  35. 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 journal › Journal article › Research › peer-review

  36. 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 journal › Journal article › Research › peer-review

  37. 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 journal › Journal article › Research › peer-review

  38. ProteomeBinders: planning a European resource of affinity reagents for analysis of the human proteome

    Taussig, M. J., Stoevesandt, O., Borrebaeck, C. A. K., Bradbury, A. R., Cahill, D., Cambillau, C., de Daruvar, A., Dübel, S., Eichler, J., Frank, R., Gibson, T. J., Gloriam, D. E., Gold, L., Herberg, F. W., Hermjakob, H., Hoheisel, J. D., Joos, T. O., Kallioniemi, O., Koegl, M., Koegll, M. & 20 others, Konthur, Z., Korn, B., Kremmer, E., Krobitsch, S., Landegren, U., van der Maarel, S., McCafferty, J., Muyldermans, S., Nygren, P., Palcy, S., Plückthun, A., Polic, B., Przybylski, M., Saviranta, P., Sawyer, A., Sherman, D. J., Skerra, A., Templin, M., Ueffing, M. & Uhlén, M., Jan 2007, In: Nature Methods. 4, 1, p. 13-7 5 p.

    Research output: Contribution to journal › Journal article › Research › peer-review

  39. 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 journal › Journal article › Research › peer-review

  40. 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 journal › Journal article › Research › peer-review

  41. 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 journal › Review › Research › peer-review

  42. 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 journal › Journal article › Research › peer-review

  43. 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 journal › Journal article › Research › peer-review

  44. 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 journal › Journal article › Research › peer-review

  45. 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 journal › Conference abstract in journal › Research › peer-review

  46. 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 journal › Journal article › Research › peer-review

  47. 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 journal › Review › Research › peer-review

  48. 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 journal › Journal article › Research › peer-review

  49. 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 journal › Journal article › Research › peer-review

  50. 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 journal › Letter › Research › peer-review

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