David E. Gloriam
Professor
Pharmaceutical Informatics
Universitetsparken 2
2100 København Ø
- 2003
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
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
- 2004
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
- 2005
High species variation within the repertoire of trace amine receptors
Gloriam, David E., Bjarnadóttir, T. K., Schiöth, H. B. & Fredriksson, R., Apr 2005, In: Annals of the New York Academy of Sciences. 5 p.Research output: Contribution to journal › Conference article › Research
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
- 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
- 2006
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. e54Research 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
- Published
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
- 2007
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. 338Research output: Contribution to journal › Journal article › Research › peer-review
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, , Jan 2007, In: Nature Methods. 4, 1, p. 13-7 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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
- 2008
- Published
How can I teach to maximize the learning of “Roberts” (slow/nonambitious) and “Susans” (fast/ambitious)? Improving University Science Teaching and Learning - Pedagogical Projects 2008
Gloriam, David E., 2008, Improving University Science Teaching and Learning - Pedagogical Projects 2008. Christiansen, F. V., Rump, C. & Degn, L. (eds.). København: Department of Science Education, University of Copenhagen, Denmark, Vol. 1. p. 227-244 18 p.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
- 2009
- Published
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
- Published
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
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. 24Research output: Contribution to journal › Journal article › Research › peer-review
- 2010
- Published
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
- Published
Minimum information about a protein affinity reagent (MIAPAR)
Bourbeillon, J., Orchard, S., Benhar, I., Borrebaeck, C., de Daruvar, A., Dübel, S., Frank, R., Gibson, F., Gloriam, D. E. I., Haslam, N., Hiltker, T., Humphrey-Smith, I., Hust, M., Juncker, D., Koegl, M., Konthur, Z., Korn, B., Krobitsch, S., Muyldermans, S., Nygren, P-Å. & 14 others, , 2010, In: Nature Biotechnology. 28, 7, p. 650-653Research output: Contribution to journal › Journal article › Research
- Published
SMARTCyp web service
Rydberg, P., Gloriam, David E. & Olsen, L., 2010Research output: Non-textual form › Interactive production › Research
- 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
- 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
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
- 2011
- 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
- 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
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
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
- 2012
- 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
- 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
- 2013
- 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
- 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
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
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
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
- 2014
- 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
- 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
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
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
- 2015
- 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
- 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
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
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
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
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
- 2016
- 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
- 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
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
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
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
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
- 2017
- 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
- 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
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 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
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
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
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
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
- 2018
- 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
- 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
- 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
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
- 2019
- 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
- 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
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
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
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
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
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
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
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
- 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
- 2020
- 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
- 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
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
- 2021
- 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, 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. 469-473Research 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
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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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