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Best matches for Harpsøe K[au]:

GPCRdb in 2018: adding GPCR structure models and ligands. Pándy-Szekeres G et al. Nucleic Acids Res. (2018)

Development of a human vasopressin V<sub>1a</sub>-receptor antagonist from an evolutionary-related insect neuropeptide. Di Giglio MG et al. Sci Rep. (2017)

GPCRdb: an information system for G protein-coupled receptors. Isberg V et al. Nucleic Acids Res. (2016)

Search results

Items: 34

1.

Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at -Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.

Giraudo A, Krall J, Bavo F, Nielsen B, Kongstad KT, Rolando B, De Blasio R, Gloriam DE, Löffler R, Thiesen L, Harpsøe K, Frydenvang K, Boschi D, Wellendorph P, Lolli ML, Jensen A, Frølund B.

J Med Chem. 2019 May 22. doi: 10.1021/acs.jmedchem.9b00026. [Epub ahead of print]

PMID:
31117514
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.

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
5.

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.

6.

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.

7.

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
8.

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.

9.

Structural insight to mutation effects uncover a common allosteric site in class C GPCRs.

Harpsøe K, Boesgaard MW, Munk C, Bräuner-Osborne H, Gloriam DE.

Bioinformatics. 2017 Apr 15;33(8):1116-1120. doi: 10.1093/bioinformatics/btw784.

10.

GPCRdb: an information system for G protein-coupled receptors.

Isberg V, Mordalski S, Munk C, Rataj K, Harpsøe K, Hauser AS, Vroling B, Bojarski AJ, Vriend G, Gloriam DE.

Nucleic Acids Res. 2017 Mar 17;45(5):2936. doi: 10.1093/nar/gkw1218. No abstract available.

11.

Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139.

Shehata MA, Nøhr AC, Lissa D, Bisig C, Isberg V, Andersen KB, Harpsøe K, Björkling F, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2016 Nov 10;6:36681. doi: 10.1038/srep36681.

12.

Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors.

Xiong XF, Zhang H, Underwood CR, Harpsøe K, Gardella TJ, Wöldike MF, Mannstadt M, Gloriam DE, Bräuner-Osborne H, Strømgaard K.

Nat Chem. 2016 Nov;8(11):1035-1041. doi: 10.1038/nchem.2577. Epub 2016 Jul 25.

13.

Integrating structural and mutagenesis data to elucidate GPCR ligand binding.

Munk C, Harpsøe K, Hauser AS, Isberg V, Gloriam DE.

Curr Opin Pharmacol. 2016 Oct;30:51-58. doi: 10.1016/j.coph.2016.07.003. Epub 2016 Jul 29. Review.

PMID:
27475047
14.

GPCRdb: the G protein-coupled receptor database - an introduction.

Munk C, Isberg V, Mordalski S, Harpsøe K, Rataj K, Hauser AS, Kolb P, Bojarski AJ, Vriend G, Gloriam DE.

Br J Pharmacol. 2016 Jul;173(14):2195-207. doi: 10.1111/bph.13509. Epub 2016 Jun 3. Review.

15.

GPCRdb: an information system for G protein-coupled receptors.

Isberg V, Mordalski S, Munk C, Rataj K, Harpsøe K, Hauser AS, Vroling B, Bojarski AJ, Vriend G, Gloriam DE.

Nucleic Acids Res. 2016 Jan 4;44(D1):D356-64. doi: 10.1093/nar/gkv1178. Epub 2015 Nov 17. Erratum in: Nucleic Acids Res. 2017 Mar 17;45(5):2936.

16.

Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

Harpsøe K, Isberg V, Tehan BG, Weiss D, Arsova A, Marshall FH, Bräuner-Osborne H, Gloriam DE.

Sci Rep. 2015 Sep 11;5:13869. doi: 10.1038/srep13869.

17.

Revision of the classical dopamine D2 agonist pharmacophore based on an integrated medicinal chemistry, homology modelling and computational docking approach.

Krogsgaard-Larsen N, Harpsøe K, Kehler J, Christoffersen CT, Brøsen P, Balle T.

Neurochem Res. 2014 Oct;39(10):1997-2007. doi: 10.1007/s11064-014-1314-2. Epub 2014 Jul 24. Review.

PMID:
25056287
18.

A ring system detected around the Centaur (10199) Chariklo.

Braga-Ribas F, Sicardy B, Ortiz JL, Snodgrass C, Roques F, Vieira-Martins R, Camargo JI, Assafin M, Duffard R, Jehin E, Pollock J, Leiva R, Emilio M, Machado DI, Colazo C, Lellouch E, Skottfelt J, Gillon M, Ligier N, Maquet L, Benedetti-Rossi G, Ramos Gomes A Jr, Kervella P, Monteiro H, Sfair R, El Moutamid M, Tancredi G, Spagnotto J, Maury A, Morales N, Gil-Hutton R, Roland S, Ceretta A, Gu SH, Wang XB, Harpsøe K, Rabus M, Manfroid J, Opitom C, Vanzi L, Mehret L, Lorenzini L, Schneiter EM, Melia R, Lecacheux J, Colas F, Vachier F, Widemann T, Almenares L, Sandness RG, Char F, Perez V, Lemos P, Martinez N, Jørgensen UG, Dominik M, Roig F, Reichart DE, LaCluyze AP, Haislip JB, Ivarsen KM, Moore JP, Frank NR, Lambas DG.

Nature. 2014 Apr 3;508(7494):72-5. doi: 10.1038/nature13155. Epub 2014 Mar 26.

PMID:
24670644
19.

mGluR5: exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery.

Mølck C, Harpsøe K, Gloriam DE, Mathiesen JM, Nielsen SM, Bräuner-Osborne H.

Neurochem Res. 2014 Oct;39(10):1862-75. doi: 10.1007/s11064-014-1248-8. Epub 2014 Feb 4.

PMID:
24493625
20.

Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain.

Krintel C, Harpsøe K, Zachariassen LG, Peters D, Frydenvang K, Pickering DS, Gajhede M, Kastrup JS.

Acta Crystallogr D Biol Crystallogr. 2013 Sep;69(Pt 9):1645-52. doi: 10.1107/S0907444913011839. Epub 2013 Aug 15.

PMID:
23999288
21.

Covalent trapping of methyllycaconitine at the α4-α4 interface of the α4β2 nicotinic acetylcholine receptor: antagonist binding site and mode of receptor inhibition revealed.

Absalom NL, Quek G, Lewis TM, Qudah T, von Arenstorff I, Ambrus JI, Harpsøe K, Karim N, Balle T, McLeod MD, Chebib M.

J Biol Chem. 2013 Sep 13;288(37):26521-32. doi: 10.1074/jbc.M113.475053. Epub 2013 Jul 26.

22.

Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors.

Harpsøe K, Hald H, Timmermann DB, Jensen ML, Dyhring T, Nielsen EØ, Peters D, Balle T, Gajhede M, Kastrup JS, Ahring PK.

J Biol Chem. 2013 Jan 25;288(4):2559-70. doi: 10.1074/jbc.M112.436337. Epub 2012 Dec 10.

23.

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 K, Gloriam DE, Clausen RP, Madsen U, Pedersen LØ, Jimenez HN, Nielsen SM, Mathiesen JM, Bräuner-Osborne H.

Mol Pharmacol. 2012 Nov;82(5):929-37. doi: 10.1124/mol.112.078808. Epub 2012 Aug 16.

PMID:
22899869
24.

Covalent attachment of antagonists to the α7 nicotinic acetylcholine receptor: synthesis and reactivity of substituted maleimides.

Ambrus JI, Halliday JI, Kanizaj N, Absalom N, Harpsøe K, Balle T, Chebib M, McLeod MD.

Chem Commun (Camb). 2012 Jul 7;48(53):6699-701. doi: 10.1039/c2cc32442c. Epub 2012 May 25.

PMID:
22627701
25.

Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site.

Trattnig SM, Harpsøe K, Thygesen SB, Rahr LM, Ahring PK, Balle T, Jensen AA.

J Biol Chem. 2012 Jul 20;287(30):25241-54. doi: 10.1074/jbc.M112.360370. Epub 2012 May 15.

26.

Structure-activity relationships for negative allosteric mGluR5 modulators.

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.

ChemMedChem. 2012 Mar 5;7(3):440-51. doi: 10.1002/cmdc.201100578. Epub 2012 Jan 20.

PMID:
22267204
27.

Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed.

Rohde LA, Ahring PK, Jensen ML, Nielsen EØ, Peters D, Helgstrand C, Krintel C, Harpsøe K, Gajhede M, Kastrup JS, Balle T.

J Biol Chem. 2012 Feb 3;287(6):4248-59. doi: 10.1074/jbc.M111.292243. Epub 2011 Dec 13.

28.

A robust force field based method for calculating conformational energies of charged drug-like molecules.

Poehlsgaard J, Harpsøe K, Jørgensen FS, Olsen L.

J Chem Inf Model. 2012 Feb 27;52(2):409-19. doi: 10.1021/ci200345f. Epub 2012 Jan 20.

PMID:
21985436
29.

Unraveling the high- and low-sensitivity agonist responses of nicotinic acetylcholine receptors.

Harpsøe K, Ahring PK, Christensen JK, Jensen ML, Peters D, Balle T.

J Neurosci. 2011 Jul 27;31(30):10759-66. doi: 10.1523/JNEUROSCI.1509-11.2011.

30.

Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.

Tosco P, Ahring PK, Dyhring T, Peters D, Harpsøe K, Liljefors T, Balle T.

J Med Chem. 2009 Apr 23;52(8):2311-6. doi: 10.1021/jm801060h.

PMID:
19301898
31.

Rational design of alpha-conotoxin analogues targeting alpha7 nicotinic acetylcholine receptors: improved antagonistic activity by incorporation of proline derivatives.

Armishaw C, Jensen AA, Balle T, Clark RJ, Harpsøe K, Skonberg C, Liljefors T, Strømgaard K.

J Biol Chem. 2009 Apr 3;284(14):9498-512. doi: 10.1074/jbc.M806136200. Epub 2009 Jan 8.

32.

Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites.

Kaae BH, Harpsøe K, Kastrup JS, Sanz AC, Pickering DS, Metzler B, Clausen RP, Gajhede M, Sauerberg P, Liljefors T, Madsen U.

Chem Biol. 2007 Nov;14(11):1294-303.

33.
34.

Identification of a putative binding site for 5-alkyl-benzothiadiazides in the AMPA receptor dimer interface.

Harpsøe K, Varming T, Gouliaev AH, Peters D, Liljefors T.

J Mol Graph Model. 2007 Jul;26(1):213-25. Epub 2006 Jul 11.

PMID:
16916614

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