David E. Gloriam
Professor
Pharmaceutical Informatics
Universitetsparken 2
2100 København Ø
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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
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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. 945-960Research output: Contribution to journal › Journal article › Research › peer-review
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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, , 2018, In: Cell. 172, 4, p. 719-730 P719-730.E14.Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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
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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, , 2010, In: Molecular and Cellular Proteomics. 9, 1, p. 1-10Research output: Contribution to journal › Journal article › Research › peer-review
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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. 1872-1881Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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
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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, , 2014, In: Structure. 22, 8, p. 1120-1139 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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
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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 journal › Journal article › Research › peer-review
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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
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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. 43-43Research output: Contribution to journal › Conference abstract in journal › Research
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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. 1489-1498Research output: Contribution to journal › Journal article › Research › peer-review
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Chemogenomics of allosteric binding sites in GPCRs
Gloriam, David E., 2013, In: Drug Discovery Today: Technologies. 10, 2, p. e307-13Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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
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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
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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
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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 journal › Journal article › Research › peer-review
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 journal › Journal article › Research › peer-review
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Computer-aided discovery of aromatic L-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139
Ísberg, V., Andersen, K. B., Bisig, C., Dietz, G. P., Bräuner, Hans & Gloriam, David E., 14 May 2014, In: Journal of Chemical Information and Modeling. 54, 6, p. 1553-1557 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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, , 18 May 2015, In: Database: The Journal of Biological Databases and Curation. 2015, p. 1-5 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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. 169-176Research output: Contribution to journal › Journal article › Research › peer-review
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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. 4429-4442Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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 journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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
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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
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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
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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
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Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT2A Receptor Agonists
Poulie, Christian Bernard Matthijs, Pottie, E., Simon, Icaro 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
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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
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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 journal › Comment/debate › Research
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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
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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
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G protein- and agonist-bound serotonin 5-HT2A receptor model activated by steered molecular dynamics simulations
Ísberg, V., Balle, T., Sander, T., Jørgensen, Flemming Steen & Gloriam, David E., 28 Feb 2011, In: Journal of Chemical Information and Modeling. 51, 2, p. 315-325Research output: Contribution to journal › Journal article › Research › peer-review
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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
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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
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GPCRDB: an information system for G protein-coupled receptors
Ísberg, V., Vroling, B., van der Kant, R., Li, K., Vriend, G. & Gloriam, David E., Jan 2014, In: Nucleic Acids Research. 42, Database issue, p. D422-D425Research output: Contribution to journal › Journal article › Research › peer-review
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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. D356-64Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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
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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
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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 journal › Journal article › Research › peer-review
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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
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GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors
Huang, S., Xu, P., Shen, D., Simon, Icaro 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
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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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