David E. Gloriam
Professor
Pharmaceutical Informatics
Universitetsparken 2
2100 København Ø
- 2018
- 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. 75-89Research output: Contribution to journal › Review › Research › peer-review
- 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, , 2018, In: Cell. 172, 4, p. 719-730 P719-730.E14.Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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. 847-860Research output: Contribution to journal › Journal article › Research › peer-review
- 2017
- 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
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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
- 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
- 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 journal › Journal article › Research › peer-review
- 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. 105-113Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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
- 2016
- 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
- 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 journal › Journal article › Research › peer-review
- 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 journal › Comment/debate › Research
- 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 journal › Journal article › Research › peer-review
- 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. D356-64Research output: Contribution to journal › Journal article › Research › peer-review
- 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
- 2015
- 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
- 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
- Published
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
- Published
Generic GPCR residue numbers - aligning topology maps while minding the gaps
Isberg, V., de Graaf, C., Bortolato, A., Cherezov, V., Katritch, V., Marshall, F. H., Mordalski, S., Pin, J., Stevens, R. C., Vriend, G. & Gloriam, David E., 1 Jan 2015, In: Trends in Pharmacological Sciences. 36, 1, p. 22-31 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Identification and characterization of small molecular NPR-B receptor antagonists
Andresen, H., Moltzau, L., Fagerheim, S., Gloriam, David E., Bach, T. & Levy, F., 1 Jan 2015, In: BMC Pharmacology and Toxicology. 16, Suppl 1, p. A70Research output: Contribution to journal › Journal article › Communication
- Published
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
- Published
Identification of the first surrogate agonists for the G protein-coupled receptor GPR132
Shehata, M. A., Christensen, H. B., Isberg, V., Pedersen, D. S., Bender, A., Bräuner, Hans & Gloriam, David E., 2015, In: RSC Advances. 5, p. 48551-48557 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2014
- 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
- Published
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
- Published
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
- Published
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
- 2013
- 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
- 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
- Published
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
- Published
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
- Published
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
- 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
- 2012
- Published
Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors
Thiele, S., Malmgaard-Clausen, M., Engel-Andreasen, J., Steen, A., Rummel, P. C., Nielsen, M. C., Gloriam, David E., Frimurer, Thomas Michael, Ulven, Trond & Rosenkilde, Mette, 27 Sep 2012, In: Journal of Medicinal Chemistry. 55, 18, p. 8164-77 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 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
- 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. 440-451Research output: Contribution to journal › Journal article › Research › peer-review
- 2011
- Published
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
- Published
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
- Published
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
- Published
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
- Published
In silico identification of novel G protein-coupled receptors
Davies, M. N., Gloriam, David E. & Flower, D. R., 2011, Methods for the discovery and characterization of G protein-coupled receptors. Stevens, C. W. (ed.). New York: Humana Press, Vol. 60. p. 3-18 (Neuromethods, Vol. 60).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
- Published
Kemogenomik: Receptoren set fra lægemiddelstoffets synspunkt
Johansson, H., Jørgensen, T. B., Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Pedersen, D. S. & Bräuner, Hans, 2011, In: Dansk Kemi. 92, 11, p. 22-26Research output: Contribution to journal › Journal article › Research
- Published
Methods for the successful application of chemogenomics to GPCR drug design
Garland, S. L. (ed.) & Gloriam, David E. (ed.), 2011, In: Current Topics in Medicinal Chemistry. 11, 15, p. 1870-1871Research output: Contribution to journal › Editorial › Research
- 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. 1994-2009Research output: Contribution to journal › Journal article › Research › peer-review
- 2010
- Published
The SMARTCyp cytochrome P450 metabolism prediction server
Rydberg, P., Gloriam, David E. & Olsen, L., 1 Dec 2010, In: Bioinformatics. 26, 23, p. 2988-2989Research output: Contribution to journal › Letter › Research › peer-review
- Published
Kemogenomik: receptoren set fra lægemiddelstoffets synspunkt
Gloriam, David E., Wellendorph, Petrine, Johansen, L. D., Pedersen, D. S. & Bräuner, Hans, Dec 2010, In: Lægemiddelforskning. 2010, p. 28-30Research output: Contribution to journal › Journal article › Communication
- 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. 96-100Research output: Contribution to journal › Letter › 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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