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Biased Signaling of CCL21 and CCL19 Does Not Rely on N-Terminal Differences, but Markedly on the Chemokine Core Domains and Extracellular Loop 2 of CCR7.

Jørgensen AS, Larsen O, Uetz-von Allmen E, Lückmann M, Legler DF, Frimurer TM, Veldkamp CT, Hjortø GM, Rosenkilde MM.

Front Immunol. 2019 Sep 13;10:2156. doi: 10.3389/fimmu.2019.02156. eCollection 2019.


Allostery in Coagulation Factor VIIa Revealed by Ensemble Refinement of Crystallographic Structures.

Sorensen AB, Madsen JJ, Frimurer TM, Overgaard MT, Gandhi PS, Persson E, Olsen OH.

Biophys J. 2019 May 21;116(10):1823-1835. doi: 10.1016/j.bpj.2019.03.024. Epub 2019 Apr 2.


Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1.

Lückmann M, Trauelsen M, Bentsen MA, Nissen TAD, Martins J, Fallah Z, Nygaard MM, Papaleo E, Lindorff-Larsen K, Schwartz TW, Frimurer TM.

Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7123-7128. doi: 10.1073/pnas.1811066116. Epub 2019 Mar 14.


Human substance P receptor binding mode of the antagonist drug aprepitant by NMR and crystallography.

Chen S, Lu M, Liu D, Yang L, Yi C, Ma L, Zhang H, Liu Q, Frimurer TM, Wang MW, Schwartz TW, Stevens RC, Wu B, Wüthrich K, Zhao Q.

Nat Commun. 2019 Feb 7;10(1):638. doi: 10.1038/s41467-019-08568-5.


Preassociation between the 5-HT7 serotonin receptor and G protein Gs: molecular determinants and association with low potency activation of adenylyl cyclase.

Ulsund AH, Dahl M, Frimurer TM, Manfra O, Schwartz TW, Levy FO, Andressen KW.

FASEB J. 2019 Mar;33(3):3870-3886. doi: 10.1096/fj.201800805RR. Epub 2018 Dec 3.


Translating biased signaling in the ghrelin receptor system into differential in vivo functions.

Mende F, Hundahl C, Plouffe B, Skov LJ, Sivertsen B, Madsen AN, Lückmann M, Diep TA, Offermanns S, Frimurer TM, Bouvier M, Holst B.

Proc Natl Acad Sci U S A. 2018 Oct 23;115(43):E10255-E10264. doi: 10.1073/pnas.1804003115. Epub 2018 Oct 9.


Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1.

Rexen Ulven E, Trauelsen M, Brvar M, Lückmann M, Bielefeldt LØ, Jensen LKI, Schwartz TW, Frimurer TM.

Sci Rep. 2018 Jul 3;8(1):10010. doi: 10.1038/s41598-018-28263-7.


Inhibiting RHOA Signaling in Mice Increases Glucose Tolerance and Numbers of Enteroendocrine and Other Secretory Cells in the Intestine.

Petersen N, Frimurer TM, Terndrup Pedersen M, Egerod KL, Wewer Albrechtsen NJ, Holst JJ, Grapin-Botton A, Jensen KB, Schwartz TW.

Gastroenterology. 2018 Oct;155(4):1164-1176.e2. doi: 10.1053/j.gastro.2018.06.039. Epub 2018 Jun 20.


Ligand-selective small molecule modulators of the constitutively active vGPCR US28.

Amărandi RM, Lückmann M, Melynis M, Jakobsen MH, Fallah Z, Spiess K, Hjortø GM, Pui A, Frimurer TM, Rosenkilde MM.

Eur J Med Chem. 2018 Jul 15;155:244-254. doi: 10.1016/j.ejmech.2018.05.053. Epub 2018 May 31.


The HETE Is on FFAR1 and Pancreatic Islet Cells.

Trauelsen M, Lückmann M, Frimurer TM, Schwartz TW.

Cell Metab. 2018 Feb 6;27(2):273-275. doi: 10.1016/j.cmet.2018.01.006.


Structural changes at the myrtenol backbone reverse its positive allosteric potential into inhibitory GABAA receptor modulation.

Milanos S, Kuenzel K, Gilbert DF, Janzen D, Sasi M, Buettner A, Frimurer TM, Villmann C.

Biol Chem. 2018 May 24;399(6):549-563. doi: 10.1515/hsz-2017-0262.


Receptor structure-based discovery of non-metabolite agonists for the succinate receptor GPR91.

Trauelsen M, Rexen Ulven E, Hjorth SA, Brvar M, Monaco C, Frimurer TM, Schwartz TW.

Mol Metab. 2017 Dec;6(12):1585-1596. doi: 10.1016/j.molmet.2017.09.005. Epub 2017 Sep 30.


Structural biology: Full monty of family B GPCRs.

Schwartz TW, Frimurer TM.

Nat Chem Biol. 2017 Jul 18;13(8):819-821. doi: 10.1038/nchembio.2438. No abstract available.


Biased agonism and allosteric modulation of G protein-coupled receptor 183 - a 7TM receptor also known as Epstein-Barr virus-induced gene 2.

Daugvilaite V, Madsen CM, Lückmann M, Echeverria CC, Sailer AW, Frimurer TM, Rosenkilde MM, Benned-Jensen T.

Br J Pharmacol. 2017 Jul;174(13):2031-2042. doi: 10.1111/bph.13801. Epub 2017 May 4.


Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions.

Frimurer TM, Mende F, Graae AS, Engelstoft MS, Egerod KL, Nygaard R, Gerlach LO, Hansen JB, Schwartz TW, Holst B.

J Med Chem. 2017 Feb 9;60(3):886-898. doi: 10.1021/acs.jmedchem.6b00648. Epub 2017 Jan 23.


Molecular Mechanism of Action for Allosteric Modulators and Agonists in CC-chemokine Receptor 5 (CCR5).

Karlshøj S, Amarandi RM, Larsen O, Daugvilaite V, Steen A, Brvar M, Pui A, Frimurer TM, Ulven T, Rosenkilde MM.

J Biol Chem. 2016 Dec 23;291(52):26860-26874. doi: 10.1074/jbc.M116.740183. Epub 2016 Nov 10.


Structure-based discovery of novel US28 small molecule ligands with different modes of action.

Lückmann M, Amarandi RM, Papargyri N, Jakobsen MH, Christiansen E, Jensen LJ, Pui A, Schwartz TW, Rosenkilde MM, Frimurer TM.

Chem Biol Drug Des. 2017 Mar;89(3):289-296. doi: 10.1111/cbdd.12848. Epub 2016 Sep 28.


In Silico Investigation of the Neurotensin Receptor 1 Binding Site: Overlapping Binding Modes for Small Molecule Antagonists and the Endogenous Peptide Agonist.

Lückmann M, Holst B, Schwartz TW, Frimurer TM.

Mol Inform. 2016 Jan;35(1):19-24. doi: 10.1002/minf.201500080. Epub 2015 Sep 16.


Role of Conserved Disulfide Bridges and Aromatic Residues in Extracellular Loop 2 of Chemokine Receptor CCR8 for Chemokine and Small Molecule Binding.

Barington L, Rummel PC, Lückmann M, Pihl H, Larsen O, Daugvilaite V, Johnsen AH, Frimurer TM, Karlshøj S, Rosenkilde MM.

J Biol Chem. 2016 Jul 29;291(31):16208-20. doi: 10.1074/jbc.M115.706747. Epub 2016 May 19.


Mutation-Guided Unbiased Modeling of the Fat Sensor GPR119 for High-Yield Agonist Screening.

Norn C, Hauge M, Engelstoft MS, Kim SH, Lehmann J, Jones RM, Schwartz TW, Frimurer TM.

Structure. 2015 Dec 1;23(12):2377-2386. doi: 10.1016/j.str.2015.09.014. Epub 2015 Oct 29.


Biased Gs versus Gq proteins and β-arrestin signaling in the NK1 receptor determined by interactions in the water hydrogen bond network.

Valentin-Hansen L, Frimurer TM, Mokrosinski J, Holliday ND, Schwartz TW.

J Biol Chem. 2015 Oct 2;290(40):24495-508. doi: 10.1074/jbc.M115.641944. Epub 2015 Aug 12.


GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo.

Hauge M, Vestmar MA, Husted AS, Ekberg JP, Wright MJ, Di Salvo J, Weinglass AB, Engelstoft MS, Madsen AN, Lückmann M, Miller MW, Trujillo ME, Frimurer TM, Holst B, Howard AD, Schwartz TW.

Mol Metab. 2014 Oct 24;4(1):3-14. doi: 10.1016/j.molmet.2014.10.002. eCollection 2015 Jan.


Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.

Sasmal PK, Krishna CV, Adabala SS, Roshaiah M, Rawoof KA, Thadi E, Sukumar KP, Cheera S, Abbineni C, Rao KV, Prasanthi A, Nijhawan K, Jaleel M, Iyer LR, Chaitanya TK, Tiwari NK, Krishna NL, Potluri V, Khanna I, Frimurer TM, Lückmann M, Rist Ø, Elster L, Högberg T.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):887-92. doi: 10.1016/j.bmcl.2014.12.064. Epub 2015 Jan 6.


Structural basis for constitutive activity and agonist-induced activation of the enteroendocrine fat sensor GPR119.

Engelstoft MS, Norn C, Hauge M, Holliday ND, Elster L, Lehmann J, Jones RM, Frimurer TM, Schwartz TW.

Br J Pharmacol. 2014 Dec;171(24):5774-89. doi: 10.1111/bph.12877.


Gating function of isoleucine-116 in TM-3 (position III:16/3.40) for the activity state of the CC-chemokine receptor 5 (CCR5).

Steen A, Sparre-Ulrich AH, Thiele S, Guo D, Frimurer TM, Rosenkilde MM.

Br J Pharmacol. 2014 Mar;171(6):1566-79. doi: 10.1111/bph.12553.


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 T, Frimurer TM, Rosenkilde MM, Gloriam DE.

J Chem Inf Model. 2013 Nov 25;53(11):2863-73. doi: 10.1021/ci4003848. Epub 2013 Oct 22.


Assessment and challenges of ligand docking into comparative models of G-protein coupled receptors.

Nguyen ED, Norn C, Frimurer TM, Meiler J.

PLoS One. 2013 Jul 2;8(7):e67302. doi: 10.1371/journal.pone.0067302. Print 2013.


Biased and constitutive signaling in the CC-chemokine receptor CCR5 by manipulating the interface between transmembrane helices 6 and 7.

Steen A, Thiele S, Guo D, Hansen LS, Frimurer TM, Rosenkilde MM.

J Biol Chem. 2013 May 3;288(18):12511-21. doi: 10.1074/jbc.M112.449587. Epub 2013 Mar 14.


PheVI:09 (Phe6.44) as a sliding microswitch in seven-transmembrane (7TM) G protein-coupled receptor activation.

Valentin-Hansen L, Holst B, Frimurer TM, Schwartz TW.

J Biol Chem. 2012 Dec 21;287(52):43516-26. doi: 10.1074/jbc.M112.395137. Epub 2012 Nov 7.


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 PC, Nielsen MC, Gloriam DE, Frimurer TM, Ulven T, Rosenkilde MM.

J Med Chem. 2012 Sep 27;55(18):8164-77. Epub 2012 Sep 18.


Melanin concentrating hormone receptor 1 (MCHR1) antagonists-Still a viable approach for obesity treatment?

Högberg T, Frimurer TM, Sasmal PK.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6039-47. doi: 10.1016/j.bmcl.2012.08.025. Epub 2012 Aug 19.


An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.

Els S, Schild E, Petersen PS, Kilian TM, Mokrosinski J, Frimurer TM, Chollet C, Schwartz TW, Holst B, Beck-Sickinger AG.

J Med Chem. 2012 Sep 13;55(17):7437-49. doi: 10.1021/jm300414b. Epub 2012 Sep 5.


Modulation of constitutive activity and signaling bias of the ghrelin receptor by conformational constraint in the second extracellular loop.

Mokrosiński J, Frimurer TM, Sivertsen B, Schwartz TW, Holst B.

J Biol Chem. 2012 Sep 28;287(40):33488-502. Epub 2012 Jul 30.


The arginine of the DRY motif in transmembrane segment III functions as a balancing micro-switch in the activation of the β2-adrenergic receptor.

Valentin-Hansen L, Groenen M, Nygaard R, Frimurer TM, Holliday ND, Schwartz TW.

J Biol Chem. 2012 Sep 14;287(38):31973-82. doi: 10.1074/jbc.M112.348565. Epub 2012 Jul 26.


Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: part 2.

Sasmal S, Balasubrahmanyam D, Kanna Reddy HR, Balaji G, Srinivas G, Cheera S, Abbineni C, Sasmal PK, Khanna I, Sebastian VJ, Jadhav VP, Singh MP, Talwar R, Suresh J, Shashikumar D, Harinder Reddy K, Sihorkar V, Frimurer TM, Rist Ø, Elster L, Högberg T.

Bioorg Med Chem Lett. 2012 May 1;22(9):3163-7. doi: 10.1016/j.bmcl.2012.03.049. Epub 2012 Mar 23.


Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists.

Sasmal S, Balaji G, Kanna Reddy HR, Balasubrahmanyam D, Srinivas G, Kyasa S, Sasmal PK, Khanna I, Talwar R, Suresh J, Jadhav VP, Muzeeb S, Shashikumar D, Harinder Reddy K, Sebastian VJ, Frimurer TM, Rist Ø, Elster L, Högberg T.

Bioorg Med Chem Lett. 2012 May 1;22(9):3157-62. doi: 10.1016/j.bmcl.2012.03.050. Epub 2012 Mar 23.


Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2.

Jensen PC, Thiele S, Steen A, Elder A, Kolbeck R, Ghosh S, Frimurer TM, Rosenkilde MM.

Br J Pharmacol. 2012 May;166(1):258-75. doi: 10.1111/j.1476-5381.2011.01771.x.


Allosteric and orthosteric sites in CC chemokine receptor (CCR5), a chimeric receptor approach.

Thiele S, Steen A, Jensen PC, Mokrosinski J, Frimurer TM, Rosenkilde MM.

J Biol Chem. 2011 Oct 28;286(43):37543-54. doi: 10.1074/jbc.M111.243808. Epub 2011 Aug 30.


Drug design of GPCR ligands using physicogenetics and chemogenomics--principles and case studies.

Frimurer TM, Högberg T.

Curr Top Med Chem. 2011;11(15):1882-901. Review.


Unique interaction pattern for a functionally biased ghrelin receptor agonist.

Sivertsen B, Lang M, Frimurer TM, Holliday ND, Bach A, Els S, Engelstoft MS, Petersen PS, Madsen AN, Schwartz TW, Beck-Sickinger AG, Holst B.

J Biol Chem. 2011 Jun 10;286(23):20845-60. doi: 10.1074/jbc.M110.173237. Epub 2011 Mar 14.


The minor binding pocket: a major player in 7TM receptor activation.

Rosenkilde MM, Benned-Jensen T, Frimurer TM, Schwartz TW.

Trends Pharmacol Sci. 2010 Dec;31(12):567-74. doi: 10.1016/ Epub 2010 Sep 25.


Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.

Sasmal PK, Sasmal S, Rao PT, Venkatesham B, Roshaiah M, Abbineni C, Khanna I, Jadhav VP, Suresh J, Talwar R, Muzeeb S, Receveur JM, Frimurer TM, Rist Ø, Elster L, Högberg T.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5443-8. doi: 10.1016/j.bmcl.2010.07.086. Epub 2010 Jul 29.


Conserved water-mediated hydrogen bond network between TM-I, -II, -VI, and -VII in 7TM receptor activation.

Nygaard R, Valentin-Hansen L, Mokrosinski J, Frimurer TM, Schwartz TW.

J Biol Chem. 2010 Jun 18;285(25):19625-36. doi: 10.1074/jbc.M110.106021. Epub 2010 Apr 15.


Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.

Grimstrup M, Receveur JM, Rist Ø, Frimurer TM, Nielsen PA, Mathiesen JM, Högberg T.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1638-41. doi: 10.1016/j.bmcl.2010.01.092. Epub 2010 Jan 22.


Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.

Rist Ø, Grimstrup M, Receveur JM, Frimurer TM, Ulven T, Kostenis E, Högberg T.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80. doi: 10.1016/j.bmcl.2009.12.008. Epub 2009 Dec 4.


Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.

Grimstrup M, Rist Ø, Receveur JM, Frimurer TM, Ulven T, Mathiesen JM, Kostenis E, Högberg T.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1181-5. doi: 10.1016/j.bmcl.2009.12.015. Epub 2009 Dec 6.


A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors.

Holst B, Nygaard R, Valentin-Hansen L, Bach A, Engelstoft MS, Petersen PS, Frimurer TM, Schwartz TW.

J Biol Chem. 2010 Feb 5;285(6):3973-85. doi: 10.1074/jbc.M109.064725. Epub 2009 Nov 17.


Ligand binding and micro-switches in 7TM receptor structures.

Nygaard R, Frimurer TM, Holst B, Rosenkilde MM, Schwartz TW.

Trends Pharmacol Sci. 2009 May;30(5):249-59. doi: 10.1016/ Epub 2009 Apr 16. Review.


Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor.

Holst B, Frimurer TM, Mokrosinski J, Halkjaer T, Cullberg KB, Underwood CR, Schwartz TW.

Mol Pharmacol. 2009 Jan;75(1):44-59. doi: 10.1124/mol.108.049189. Epub 2008 Oct 15.


Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism.

Holst B, Mokrosinski J, Lang M, Brandt E, Nygaard R, Frimurer TM, Beck-Sickinger AG, Schwartz TW.

J Biol Chem. 2007 May 25;282(21):15799-811. Epub 2007 Mar 19.

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