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Items: 1 to 20 of 74

1.

Identification of a novel scaffold for a small molecule GPR139 receptor agonist.

Nøhr AC, Shehata MA, Palmer D, Pokhrel R, Vallianou M, Foster SR, Gentry PR, Gloriam DE, Bräuner-Osborne H.

Sci Rep. 2019 Mar 7;9(1):3802. doi: 10.1038/s41598-019-40085-9.

2.

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 F, Falk-Petersen CB, Jensen CH, Nielsen JO, Tian Y, Anglani V, Kongstad KT, Piilgaard L, Nielsen B, Gloriam DE, Kehler J, Jensen AA, Harpsøe K, Wellendorph P, Frølund B.

J Med Chem. 2019 Mar 14;62(5):2798-2813. doi: 10.1021/acs.jmedchem.9b00131. Epub 2019 Feb 27.

PMID:
30763084
3.

Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity.

Malfacini D, Patt J, Annala S, Harpsøe K, Eryilmaz F, Reher R, Crüsemann M, Hanke W, Zhang H, Tietze D, Gloriam DE, Bräuner-Osborne H, Strømgaard K, König GM, Inoue A, Gomeza J, Kostenis E.

J Biol Chem. 2019 Apr 12;294(15):5747-5758. doi: 10.1074/jbc.RA118.007250. Epub 2019 Feb 11.

4.

Bigger is better in virtual drug screens.

Gloriam DE.

Nature. 2019 Feb;566(7743):193-194. doi: 10.1038/d41586-019-00145-6. No abstract available.

PMID:
30737502
5.

An online resource for GPCR structure determination and analysis.

Munk C, Mutt E, Isberg V, Nikolajsen LF, Bibbe JM, Flock T, Hanson MA, Stevens RC, Deupi X, Gloriam DE.

Nat Methods. 2019 Feb;16(2):151-162. doi: 10.1038/s41592-018-0302-x. Epub 2019 Jan 21. Review.

PMID:
30664776
6.

Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine-to-isoleucine variation.

Mackenzie AE, Quon T, Lin LC, Hauser AS, Jenkins L, Inoue A, Tobin AB, Gloriam DE, Hudson BD, Milligan G.

FASEB J. 2019 Apr;33(4):5005-5017. doi: 10.1096/fj.201801956R. Epub 2019 Jan 2.

7.

Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359.

Zhang H, Nielsen AL, Boesgaard MW, Harpsøe K, Daly NL, Xiong XF, Underwood CR, Haugaard-Kedström LM, Bräuner-Osborne H, Gloriam DE, Strømgaard K.

Eur J Med Chem. 2018 Aug 5;156:847-860. doi: 10.1016/j.ejmech.2018.07.023. Epub 2018 Jul 12.

PMID:
30055466
8.

5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.

Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjørn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ.

Cell. 2018 Feb 8;172(4):719-730.e14. doi: 10.1016/j.cell.2018.01.001. Epub 2018 Feb 1.

9.

Pharmacogenomics of GPCR Drug Targets.

Hauser AS, Chavali S, Masuho I, Jahn LJ, Martemyanov KA, Gloriam DE, Babu MM.

Cell. 2018 Jan 11;172(1-2):41-54.e19. doi: 10.1016/j.cell.2017.11.033. Epub 2017 Dec 14.

10.

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms.

Jespers W, Schiedel AC, Heitman LH, Cooke RM, Kleene L, van Westen GJP, Gloriam DE, Müller CE, Sotelo E, Gutiérrez-de-Terán H.

Trends Pharmacol Sci. 2018 Jan;39(1):75-89. doi: 10.1016/j.tips.2017.11.001. Epub 2017 Dec 5. Review.

PMID:
29203139
11.

A Structural Framework for GPCR Chemogenomics: What's In a Residue Number?

Vass M, Kooistra AJ, Verhoeven S, Gloriam D, de Esch IJP, de Graaf C.

Methods Mol Biol. 2018;1705:73-113. doi: 10.1007/978-1-4939-7465-8_4.

PMID:
29188559
12.

GPCRdb in 2018: adding GPCR structure models and ligands.

Pándy-Szekeres G, Munk C, Tsonkov TM, Mordalski S, Harpsøe K, Hauser AS, Bojarski AJ, Gloriam DE.

Nucleic Acids Res. 2018 Jan 4;46(D1):D440-D446. doi: 10.1093/nar/gkx1109.

13.

Trends in GPCR drug discovery: new agents, targets and indications.

Hauser AS, Attwood MM, Rask-Andersen M, Schiöth HB, Gloriam DE.

Nat Rev Drug Discov. 2017 Dec;16(12):829-842. doi: 10.1038/nrd.2017.178. Epub 2017 Oct 27. Review.

PMID:
29075003
14.

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 CH, Bavo F, Falk-Petersen CB, Haugaard AS, Vogensen SB, Tian Y, Nittegaard-Nielsen M, Sigurdardóttir SB, Kehler J, Kongstad KT, Gloriam DE, Clausen RP, Harpsøe K, Wellendorph P, Frølund B.

J Med Chem. 2017 Nov 9;60(21):9022-9039. doi: 10.1021/acs.jmedchem.7b01351. Epub 2017 Oct 30.

PMID:
29028338
15.

Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils.

Christensen HB, Gloriam DE, Pedersen DS, Cowland JB, Borregaard N, Bräuner-Osborne H.

J Pharmacol Toxicol Methods. 2017 Nov;88(Pt 1):72-78. doi: 10.1016/j.vascn.2017.07.003. Epub 2017 Jul 15.

PMID:
28716665
16.

Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method.

Frandsen IO, Boesgaard MW, Fidom K, Hauser AS, Isberg V, Bräuner-Osborne H, Wellendorph P, Gloriam DE.

Sci Rep. 2017 Jul 6;7(1):4829. doi: 10.1038/s41598-017-05058-w.

17.

Selectivity determinants of GPCR-G-protein binding.

Flock T, Hauser AS, Lund N, Gloriam DE, Balaji S, Babu MM.

Nature. 2017 May 18;545(7654):317-322. doi: 10.1038/nature22070. Epub 2017 May 10.

18.

The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site.

Nøhr AC, Jespers W, Shehata MA, Floryan L, Isberg V, Andersen KB, Åqvist J, Gutiérrez-de-Terán H, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2017 Apr 25;7(1):1128. doi: 10.1038/s41598-017-01049-z.

19.

Proteome-Scale Human Interactomics.

Luck K, Sheynkman GM, Zhang I, Vidal M.

Trends Biochem Sci. 2017 May;42(5):342-354. doi: 10.1016/j.tibs.2017.02.006. Epub 2017 Mar 8. Review.

20.

Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide.

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.

Sci Rep. 2017 Feb 1;7:41002. doi: 10.1038/srep41002.

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