David E. Gloriam

David E. Gloriam

Professor


  1. 2019
  2. Published

    Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at -Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters. / Giraudo, Alessandro; Krall, Jacob; Bavo, Francesco; Nielsen, Birgitte; Kongstad, Kenneth Thermann; Rolando, Barbara; De Blasio, Rosella; Gloriam, David E; Löffler, Rebekka; Thiesen, Louise; Harpsøe, Kasper; Frydenvang, Karla; Boschi, Donatella; Wellendorph, Petrine; Lolli, Marco L; Jensen, Anders A.; Frølund, Bente.

    In: Journal of Medicinal Chemistry, Vol. 62, No. 12, 27.06.2019, p. 5797-5809.

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity. / Malfacini, Davide; Patt, Julian; Annala, Suvi; Harpsøe, Kasper; Eryilmaz, Funda; Reher, Raphael; Crüsemann, Max; Hanke, Wiebke; Zhang, Hang; Tietze, Daniel; Gloriam, David E; Bräuner-Osborne, Hans; Strømgaard, Kristian; König, Gabriele M; Inoue, Asuka; Gomeza, Jesus; Kostenis, Evi.

    In: The Journal of Biological Chemistry, Vol. 294, No. 15, 12.04.2019, p. 5747-5758.

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Published

    Receptor selectivity between the G proteins Gα 12 and Gα 13 is defined by a single leucine-to-isoleucine variation. / Mackenzie, Amanda E.; Quon, Tezz; Lin, Li Chiung; Hauser, Alexander S.; Jenkins, Laura; Inoue, Asuka; Tobin, Andrew B.; Gloriam, David E.; Hudson, Brian D.; Milligan, Graeme.

    In: FASEB journal : official publication of the Federation of American Societies for Experimental Biology, Vol. 33, No. 4, 01.04.2019, p. 5005-5017.

    Research output: Contribution to journalJournal articleResearchpeer-review

  5. 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, Jacob; Bavo, Francesco; Falk-Petersen, Christina B; Jensen, Claus Hatt; Nielsen, Julie Olsson; Tian, Yongsong; Anglani, Valeria; Kongstad, Kenneth Thermann; Piilgaard, Louise; Nielsen, Birgitte; Gloriam, David E; Kehler, Jan; Jensen, Anders A.; Harpsøe, Kasper; Wellendorph, Petrine; Frølund, Bente.

    In: Journal of Medicinal Chemistry, Vol. 62, No. 5, 14.03.2019, p. 2798-2813.

    Research output: Contribution to journalJournal articleResearchpeer-review

  6. Published

    Identification of a novel scaffold for a small molecule GPR139 receptor agonist. / Nøhr, Anne Cathrine; Shehata, Mohamed A; Palmer, Daniel; Pokhrel, Rina; Vallianou, Maria; Foster, Simon R; Gentry, Patrick R; Gloriam, David E; Bräuner-Osborne, Hans.

    In: Scientific Reports, Vol. 9, No. 1, 07.03.2019, p. 3802.

    Research output: Contribution to journalJournal articleResearchpeer-review

  7. Published

    Bigger is better in virtual drug screens. / Gloriam, David E.

    In: Nature, Vol. 566, No. 7743, 14.02.2019, p. 193-194.

    Research output: Contribution to journalLetterResearchpeer-review

  8. 2018
  9. Published

    Structure–activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. / Zhang, Hang; Nielsen, Alexander L.; Boesgaard, Michael W.; Harpsøe, Kasper; Daly, Norelle L.; Xiong, Xiao-feng; Underwood, Christina R.; Haugaard-kedström, Linda M.; Bräuner-osborne, Hans; Gloriam, David E.; Strømgaard, Kristian.

    In: European Journal of Medicinal Chemistry, Vol. 156, 05.08.2018, p. 847-860.

    Research output: Contribution to journalJournal articleResearchpeer-review

  10. Published

    A Structural Framework for GPCR Chemogenomics : What’s In a Residue Number? / Vass, Márton; Kooistra, Albert J.; Verhoeven, Stefan; Gloriam, David; de Esch, Iwan J.P.; de Graaf, Chris.

    Methods in Molecular Biology. Humana Press, 2018. p. 73-113 (Methods in Molecular Biology, Vol. 1705).

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  11. Published

    Pharmacogenomics of GPCR Drug Targets. / Hauser, Alexander Sebastian; Chavali, Sreenivas; Masuho, Ikuo; Jahn, Leonie; Martemyanov, Kirill; Gloriam, David E.; Babu, Madan.

    In: Cell, Vol. 172, 01.2018, p. 41–54.

    Research output: Contribution to journalJournal articleResearchpeer-review

  12. Published

    Structural Mapping of Adenosine Receptor Mutations : Ligand Binding and Signaling Mechanisms. / Jespers, Willem; Schiedel, Anke C; Heitman, Laura H; Cooke, Robert M; Kleene, Lisa; van Westen, Gerard J P; Gloriam, David E; Müller, Christa E; Sotelo, Eddy; Gutiérrez-de-Terán, Hugo.

    In: Trends in Pharmacological Sciences, Vol. 39, No. 1, 01.2018, p. 75-89.

    Research output: Contribution to journalReviewResearchpeer-review

  13. Published

    5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. / Peng, Yao; McCorvy, John D.; Harpsøe, Kasper; Lansu, Katherine; Yuan, Shuguang; Popov, Petr; Qu, Lu; Pu, Mengchen; Che, Tao; Nikolajsen, Louise F.; Huang, Xi-ping; Wu, Yiran; Shen, Ling; Bjørn-Yoshimoto, Walden E.; Ding, Kang; Wacker, Daniel; Han, Gye Won; Cheng, Jianjun; Katritch, Vsevolod; Jensen, Anders A.; Hanson, Michael A.; Zhao, Suwen; Gloriam, David E.; Roth, Bryan L.; Stevens, Raymond C.; Liu, Zhi-jie.

    In: Cell, Vol. 172, No. 4, P719-730.E14, 2018, p. 719-730.

    Research output: Contribution to journalJournal articleResearchpeer-review

  14. Published

    GPCRdb in 2018 : adding GPCR structure models and ligands. / Pándy-Szekeres, Gáspár; Munk, Christian; Tsonkov, Tsonko M; Mordalski, Stefan; Harpsøe, Kasper; Hauser, Alexander S; Bojarski, Andrzej J; Gloriam, David E.

    In: Nucleic Acids Research, Vol. 46, No. D1, gkx1109, 2018.

    Research output: Contribution to journalJournal articleResearchpeer-review

  15. 2017
  16. Published

    Trends in GPCR drug discovery: new agents, targets and indications. / Hauser, Alexander Sebastian; Gloriam, David E.; Attwood, Misty M.; Rask-Andersen, Mathias ; Schiöth, Helgi B. .

    In: Nature Reviews. Drug Discovery, Vol. 16, 178, 27.10.2017, p. 829-842.

    Research output: Contribution to journalJournal articleResearchpeer-review

  17. Published

    Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils. / Christensen, Hanna B; Gloriam, David E; Pedersen, Daniel Sejer; Cowland, Jack B; Borregaard, Niels; Bräuner-Osborne, Hans.

    In: Journal of Pharmacological and Toxicological Methods, Vol. 88, No. Pt 1, 15.07.2017, p. 72-78.

    Research output: Contribution to journalJournal articleResearchpeer-review

  18. Published

    Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method. / Frandsen, Ida Osborn; Boesgaard, Michael W; Fidom, Kimberley; Hauser, Alexander S; Isberg, Vignir; Bräuner-Osborne, Hans; Wellendorph, Petrine; Gloriam, David E.

    In: Scientific Reports, Vol. 7, No. 1, 4829, 06.07.2017.

    Research output: Contribution to journalJournal articleResearchpeer-review

  19. Published

    Selectivity determinants of GPCR-G-protein binding. / Flock, Tilman; Hauser, Alexander S; Lund, Nadia; Gloriam, David E; Balaji, Santhanam; Babu, M Madan.

    In: Nature, Vol. 545, No. 7654, 18.05.2017, p. 317-322.

    Research output: Contribution to journalJournal articleResearchpeer-review

  20. Published

    The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site. / Shehata, Mohamed A.; Jensen, Anne Cathrine Nøhr; Jespers, Willem; Floryan, Leonard; Isberg, Vignir; Andersen, Kirsten Bayer; Åqvist, Johan; Gutiérrez-de-Terán, Hugo; Bräuner-Osborne, Hans; Gloriam, David E.

    In: Scientific Reports, Vol. 7, 1128, 25.04.2017.

    Research output: Contribution to journalJournal articleResearchpeer-review

  21. Published

    Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide. / Di Giglio, Maria Giulia; Muttenthaler, Markus; Harpsøe, Kasper; Liutkeviciute, Zita; Keov, Peter; Eder, Thomas; Rattei, Thomas; Arrowsmith, Sarah; Wray, Susan; Marek, Ales; Elbert, Tomas; Alewood, Paul F; Gloriam, David E; Gruber, Christian W.

    In: Scientific Reports, Vol. 7, 41002, 01.02.2017.

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. 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, Anne Cathrine Nøhr; Shehata, Mohamed A; Hauser, Alexander S; Isberg, Vignir; Mokrosinski, Jacek; Farooqi, I Sadaf; Pedersen, Daniel Sejer; Gloriam, David E; Bräuner-Osborne, Hans.

    In: Neurochemistry International, Vol. 102, 01.01.2017, p. 105-113.

    Research output: Contribution to journalJournal articleResearchpeer-review

  23. 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, Jacob; Jensen, Claus Hatt; Bavo, Francesco; Falk-Petersen, Christina Birkedahl; Haugaard, Anne Stæhr; Vogensen, Stine Byskov; Tian, Yongsong; Nittegaard-Nielsen, Mia; Sigurdardóttir, Sara Björk; Kehler, Jan; Kongstad, Kenneth Thermann; Gloriam, David E.; Clausen, Rasmus Prætorius; Harpsøe, Kasper; Wellendorph, Petrine; Frølund, Bente.

    In: Journal of Medicinal Chemistry, Vol. 60, No. 21, 2017, p. 9022-9039.

    Research output: Contribution to journalJournal articleResearchpeer-review

  24. Published

    Structural insight to mutation effects uncover a common allosteric site in class C GPCRs. / Harpsøe, Kasper; Boesgaard, Michael W; Munk, Christian; Bräuner-Osborne, Hans; Gloriam, David E.

    In: Bioinformatics (Oxford, England), Vol. 33, No. 8, btw784, 2017, p. 1116-1120.

    Research output: Contribution to journalJournal articleResearchpeer-review

  25. 2016
  26. Published

    Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139. / Shehata, Mohamed A; Jensen, Anne Cathrine Nøhr; Lissa, Delphine; Bisig, Christoph; Isberg, Vignir; Andersen, Kirsten B; Harpsøe, Kasper; Björkling, Fredrik; Bräuner-Osborne, Hans; Gloriam, David E.

    In: Scientific Reports, Vol. 6, 36681, 10.11.2016, p. 1-13.

    Research output: Contribution to journalJournal articleResearchpeer-review

  27. Published

    Integrating structural and mutagenesis data to elucidate GPCR ligand binding. / Munk, Christian; Harpsøe, Kasper; Hauser, Alexander S; Isberg, Vignir; Gloriam, David E.

    In: Current Opinion in Pharmacology, Vol. 30, 10.2016, p. 51-58.

    Research output: Contribution to journalJournal articleResearchpeer-review

  28. Published

    Editorial overview : New technologies: GPCR drug design and function-exploiting the current (of) structures. / Tautermann, Christofer S; Gloriam, David E.

    In: Current Opinion in Pharmacology, Vol. 30, 02.08.2016, p. 7-10.

    Research output: Contribution to journalComment/debateResearch

  29. Published

    GPCRdb: The G protein-coupled receptor database - an introduction. / Munk, C; Isberg, V; Mordalski, S; Harpsøe, K; Rataj, K; Hauser, A S; Kolb, P; Bojarski, A J; Vriend, G; Gloriam, D E.

    In: British Journal of Pharmacology, Vol. 173, No. 14, 07.2016, p. 2195-207.

    Research output: Contribution to journalJournal articleResearchpeer-review

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