David E. Gloriam
Professor
Pharmaceutical Informatics
Universitetsparken 2
2100 København Ø
- 2024
- 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-D475Research output: Contribution to journal › Journal article › Research › peer-review
- 2023
- 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. 531–535Research output: Contribution to journal › Comment/debate › Research › peer-review
- 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. 3045-3057Research output: Contribution to journal › Journal article › Research › peer-review
- 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–D402Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 978-990Research output: Contribution to journal › Review › Research › peer-review
- 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
- 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
- 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. 2727–2742Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 459-471Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- 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 journal › Journal article › Research › peer-review
- 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. 3651-3674Research output: Contribution to journal › Review › Research › peer-review
- 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. 12031–12043Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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. 226-238Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 210-213Research output: Contribution to journal › Letter › Research › peer-review
- 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-D525Research output: Contribution to journal › Journal article › Research › peer-review
- 2021
- 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
- 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 journal › Journal article › Research › peer-review
- 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. 875-878Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 879-888Research output: Contribution to journal › Journal article › Research › peer-review
- 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-D343Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 46-56Research output: Contribution to journal › Journal article › Research › peer-review
- 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
- 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
- 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. 469-473Research output: Contribution to journal › Journal article › Research › peer-review
- 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 ppResearch output: Contribution to journal › Journal article › Research › peer-review
- 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. 891-901Research output: Contribution to journal › Journal article › Research › peer-review
- 2020
- 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 journal › Journal article › Research › peer-review
- 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
- Published
24 Messages on a Sustainable Career in Research at UCPH
Larsen, K. R. (ed.), Wegener, H. C., Stein, A., Bach, A., Williams, A. R., Gall, C., Gravert, C., Gloriam, D. E., Lorenzen, E., Yvanez, E., Cappellini, E., Poulsen, F., Mortensen, J., Bentzen, J. S., Shik, J. Z., Miskowiak, K. W., Elgaard, K. K. E., Jønsson, K. A., Won, K. J., Nørgaard, L. C. & 9 others, , 2020, University of Copenhagen. 31 p.Research output: Book/Report › Report › Communication
- 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 journal › Journal article › Research › peer-review
- 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. 13850-13861Research output: Contribution to journal › Journal article › Research › peer-review
- 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, , 2020, In: Molecular Cell. 80, 3, p. 485-500Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Editorial › Research
- 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, , 2020, In: Nature Methods. 17, 8, p. 777-787Research output: Contribution to journal › Journal article › Research › peer-review
- 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
- 2019
- 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. 895-908Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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. 5797-5809Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 35-46Research output: Contribution to journal › Review › Research › peer-review
- 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. 5747-5758Research output: Contribution to journal › Journal article › Research › peer-review
- 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
- 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. 2798-2813Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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. 151-162Research output: Contribution to journal › Review › Research › peer-review
- 2018
- 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 proceeding › Book chapter › Research › peer-review
- 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. 41–54Research output: Contribution to journal › Journal article › Research › peer-review
ID: 5953796
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Kemogenomik: Receptoren set fra lægemiddelstoffets synspunkt
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Generic GPCR residue numbers - aligning topology maps while minding the gaps
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Pharmacogenomics of GPCR Drug Targets
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