Publications – University of Copenhagen

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Department of Drug Design and Pharmacology > Research > Biostructural Research > Gloriam Group > Publications

Publications in the Gloriam group

*Selected publications, #Shared last authors

Di Giglio MG, Muttenthaler M, Harpsøe K, Liutkeviciute Z, Keov P, Eder T, Rattei T, Arrowsmith S, Wray S, Marek A, Elbert T, Alewood PF, Gloriam DE, Gruber CW.
Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide.
Sci Rep. 2017 Feb 1;7:41002.

Nøhr AC, Shehata MA, Hauser AS, Isberg V, Mokrosinski J, Andersen KB, Farooqi
IS, Pedersen DS, Bräuner-Osborne H#, Gloriam DE#
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.
Neurochem Int. (IF 3.4) 2017 Jan;102:105-113

*Harpsøe K, Boesgaard MW, Munk C, Bräuner-Osborne H, Gloriam DE.
Structural insight to mutation effects uncover a common allosteric site in class C GPCRs.
Bioinformatics. (IF 5.8) 2016 Dec 22

Shehata MA, Nøhr AC, Lissa D, Bisig C, Isberg V, Andersen KB, Harpsøe K, Björkling F, #Bräuner-Osborne H, #Gloriam DE.
Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139.
Sci Rep. (IF 5.6) 2016 Nov 10;6:36681

*Xiong XF, Zhang H, Underwood CR, Harpsøe K, Gardella TJ, Wöldike MF, Mannstadt M, Gloriam DE, Bräuner-Osborne H, Strømgaard K.
Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors.
Nat Chem. (IF 25,3) 2016 Nov;8(11):1035-1041

Munk C, Harpsøe H, Hauser A, Isberg V, and Gloriam DE
Integrating structural and mutagenesis data to elucidate GPCR ligand binding.
Curr Opin Pharmacol (IF 4,6), 2016 Jul 28;30:51-58

Munk C, Isberg V, Mordalski S, Harpsøe K, Rataj K, Hauser A, Kolb P, Bojarski AJ, Vriend G, and Gloriam DE
GPCRdb: The G protein-coupled receptor database - An introduction.
Br J Pharmacol (IF 4,8), 2016 Jul;173(14):2195-207

*Isberg V, Mordalski S, Munk C, Rataj K, Harpsøe K, Hauser AS, Vroling B, Bojarski AJ, Vriend G, and Gloriam DE
GPCRdb: an information system for G protein-coupled receptors
Nucleic Acids Res (IF 9.1), 2016 Jan 4;44(D1):D356-64

*Johansson H, Worch Boesgaard M, Nørskov-Lauritsen L, Larsen I, Kuhne S, and #Gloriam DE, #Bräuner-Osborne H , #Sejer Pedersen D
Selective allosteric antagonists for the G protein-coupled receptor GPRC6A based on the 2-phenylindole privileged structure scaffold
J. Med Chem (IF 5.4), 2015 Nov 16.

*Harpsøe K, Isberg V, Tehan BG, Weiss D, Arsova A, Marshall FH, Bräuner-Osborne H, Gloriam DE.
Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors - A Structural Perspective of Ligands and Mutants.
Sci Rep (IF 5.6). 2015 Sep 11;5:13869.

Babbitt PC, Bagos PG, Bairoch A, Bateman A, Chatonnet A, Chen MJ, Craik DJ, Finn RD, Gloriam D, Haft DH, Henrissat B, Holliday GL, Isberg V, Kaas Q, Landsman D, Lenfant N, Manning G, Nagano N, Srinivasan N, O'Donovan C, Pruitt KD, Sowdhamini R, Rawlings ND, Saier MH Jr, Sharman JL, Spedding M, Tsirigos KD, Vastermark A, Vriend G.
Creating a specialist protein resource network: a meeting report for the protein bioinformatics and community resources retreat.
Database (IF 4.5). 2015 Jul 11; 2015

Shehata MA, Belcik Christensen H, Isberg V, Pedersen D, Bender A, #Bräuner-Osborne H, #Gloriam DE.
Identification of the first surrogate agonists for the G protein-coupled receptor GPR132.
RSC Advances (IF 3.8), 2015; May 12 (5):48551-48557

*Isberg V, de Graaf C, Bortolato A, Cherezov V, Katritch V, Marshall FH, Mordalski S, Pin JP, Stevens RC, Vriend G, Gloriam DE.
Generic GPCR residue numbers - aligning topology maps while minding the gaps.
Trends Pharmacol Sci (IF 11.5). 2015 Jan;36(1):22-31

Fidom K, Isberg V, Hauser AS, Mordalski S, Lehto T, Bojarski AJ, Gloriam DE.
A new crystal structure fragment-based pharmacophore method for G protein-coupled receptors.
Methods (IF 3.6) 2015 Jan;71:104-12

*Kufareva I, Katritch V, Gloriam DE, other GPCR Dock participants, Stevens RC, Abagyan R
Advances in GPCR modeling evaluated by the GPCR Dock 2013 assessment: meeting new challenges
Structure (IF 5.6) 2014 Aug 5;22(8):1120-39

Isberg V, Andersen KB, Bisig C, Dietz GPH, #Bräuner-Osborne H and #Gloriam DE
Computer-aided Discovery of Aromatic L-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139
J Chem Inf Model (IF 3.7) 2014 May 14

Mølck C, Harpsøe K, Gloriam DE, Mathiesen JM, Nielsen SM and Bräuner-Osborne H
mGluR5: Exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery
Neurochem Res (IF 2.1) 2014 Feb 4

*Isberg V, Vroling B, van der Kant R, Li K, Vriend G and Gloriam DE
GPCRDB: information system for G protein-coupled receptors
Nucleic Acids Res. (IF 9.1) 2014 Jan 1;42(1)

Isberg V, Paine J, Leth-Petersen S, Kristensen J, Gloriam DE
Structure-Activity Relationships of Constrained Phenylethylamine Ligands for the Serotonin 5-HT2 Receptors
PLoS One (IF 3.2) 2013 Nov 7;8(11):e78515

Chalikiopoulos A, Thiele S, Malmgaard-Clausen M, Rydberg P, Isberg V, Ulven T, Frimurer T, Rosenkilde M, Gloriam DE
Structure-activity relationships and identification of optimized CC-chemokine receptor CCR1, 5 and 8 metal-ion chelators
J Chem Inf Model (IF 3.7) 2013 Nov 25;53(11):2863-73

Gloriam DE
Chemogenomics of allosteric binding sites in GPCRs
Drug Discov Today Technol (IF NA) 2013 Summer;10(2):e307-13

Rydberg P, Rostkowski M, Gloriam DE, Olsen L
The contribution of atom accessibility to site of metabolism models for cytochromes P450
Mol Pharm (IF 4.3) 2013 Apr 1;10(4):1216-23
Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, Stensbøl TB, Gloriam DE, Krogsgaard-Larsen P, Frølund B
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
J Med Chem (IF 5.4) 2013 Feb 14;56(3):1211-27

Johansson H, Jørgensen TB, Gloriam DE, Bräuner-Osborne H, and Pedersen DS
3-Substituted 2-Phenyl-Indoles: Privileged Structures for Medicinal Chemistry
RSC Advances (IF 3.8) 21 Jan 2013; 3 (3) p. 945-960

Thiele S, Malmgaard-Clausen M, Engel-Andreasen J, Steen A, Rummel PC, Nielsen MC, Gloriam DE, Frimurer TM, Ulven T, Rosenkilde MM
Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors
J Med Chem (IF 5.4) 2012 Sep 27;55(18):8164-77

Mølck C, Harpsøe K, Gloriam DE, Clausen RP, Madsen U, Pedersen LO, Jimenez HN, Nielsen SM, Mathiesen JM, Bräuner-Osborne H
Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-selective Negative Allosteric Modulators
Mol Pharmacol (IF 4.1) 2012 Nov;82(5):929-37

Kaae BH, Harpsøe K, Kvist T, Mathiesen JM, Mølck C, Gloriam D, Jimenez HN, Uberti MA, Nielsen SM, Nielsen B, Bräuner-Osborne H, Sauerberg P, Clausen RP, Madsen U
Structure-Activity Relationships for Negative Allosteric mGluR5 Modulators
ChemMedChem. (IF 3.0) 2012 Mar 5;7(3):440-51

Gloriam DE, Wellendorph P, Johansen LD, Thomsen A, Phonekeo K, Pedersen DS, Bräuner-Osborne H
Chemogenomic Discovery of Novel Allosteric Antagonists at the GPRC6A Receptor
Chem Biol. (IF 5.3) 2011 Nov 23;18(11):1489-98

Davies MN, Gloriam DE, Secker A, Freitas AA, Timmis J, Flower DR
Present Perspectives on the Automated Classification of the G-Protein Coupled Receptors (GPCRs) at the Protein Sequence Level
Curr Top Med Chem (IF 3.4) 2011;11(15):1994-2009

Garland SL, Gloriam DE
A Ligand's View of Target Similarity: Chemogenomic Binding Site-Directed Techniques for Drug Discovery
Curr Top Med Chem (IF 3.4) 2011;11(15):1872-81

Ísberg V, Balle T, Sander T, Jørgensen FS, Gloriam DE
G Protein- and Agonist-Bound Serotonin 5-HT(2A) Receptor Model Activated by Steered Molecular Dynamics Simulations
J Chem Inf Model (3.7) 2011 Feb 28;51(2):315-25

Rydberg P, Gloriam DE, Olsen L
The SMARTCyp cytochrome P450 metabolism prediction server
Bioinformatics (IF 5.0) 2010 Dec 1;26(23):2988-9

*Bourbeillon J, Orchard S, Benhar I, Borrebaeck C, de Daruvar A, Dübel S, Frank R, Gibson F, Gloriam D, Haslam N, Hiltker T, Humphrey-Smith I, Hust M, Juncker D, Koegl M, Konthur Z, Korn B, Krobitsch S, Muyldermans S, Nygren PA, Palcy S, Polic B, Rodriguez H, Sawyer A, Schlapshy M, Snyder M, Stoevesandt O, Taussig MJ, Templin M, Uhlen M, van der Maarel S, Wingren C, Hermjakob H, Sherman D
Minimum information about a protein affinity reagent (MIAPAR)
Nat Biotechnol (IF 41.5) 2010 Jul;28(7):650-3

Rydberg P, Gloriam DE, Zaretzki J, Breneman C, Olsen L
SMARTCyp: A 2D Method for Prediction of Cytochrome P450-Mediated Drug Metabolism
ACS Medicinal Chemistry Letters (IF 3.1) 2010 1(3), 96-100

Gloriam DE, Orchard S, Bertinetti D, Björling E, Bongcam-Rudloff E, Borrebaeck CA, Bourbeillon J, Bradbury AR, de Daruvar A, Dübel S, Frank R, Gibson TJ, Gold L, Haslam N, Herberg FW, Hiltke T, Hoheisel JD, Kerrien S, Koegl M, Konthur Z, Korn B, Landegren U, Montecchi-Palazzi L, Palcy S, Rodriguez H, Schweinsberg S, Sievert V, Stoevesandt O, Taussig MJ, Ueffing M, Uhlén M, van der Maarel S, Wingren C, Woollard P, Sherman DJ, Hermjakob H
A community standard format for the representation of protein affinity reagents
Mol Cell Proteomics (IF 7.2) 2010 Jan;9(1):1-10

Nordström KJ, Mirza MA, Almén MS, Gloriam DE, Fredriksson R, Schiöth HB
Critical evaluation of the FANTOM3 non-coding RNA transcripts
Genomics (IF 3.3) 2009 Sep;94(3):169-76

Gloriam DE, Foord SM, Blaney FE, Garland SL
Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design
J Med Chem (IF 5.4) 2009 Jul 23;52(14):4429-42

Haitina T, Fredriksson R, Foord SM, Schiöth HB, Gloriam DE
The G protein-coupled receptor subset of the dog genome is more similar to that in humans than rodents
BMC Genomics (IF 4.0) 2009 Jan 15;10:24