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Items: 25

1.

NF-κB activation in astrocytes drives a stage-specific beneficial neuroimmunological response in ALS.

Ouali Alami N, Schurr C, Olde Heuvel F, Tang L, Li Q, Tasdogan A, Kimbara A, Nettekoven M, Ottaviani G, Raposo C, Röver S, Rogers-Evans M, Rothenhäusler B, Ullmer C, Fingerle J, Grether U, Knuesel I, Boeckers TM, Ludolph A, Wirth T, Roselli F, Baumann B.

EMBO J. 2018 Aug 15;37(16). pii: e98697. doi: 10.15252/embj.201798697. Epub 2018 Jun 6.

2.

Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells.

Soethoudt M, Stolze SC, Westphal MV, van Stralen L, Martella A, van Rooden EJ, Guba W, Varga ZV, Deng H, van Kasteren SI, Grether U, IJzerman AP, Pacher P, Carreira EM, Overkleeft HS, Ioan-Facsinay A, Heitman LH, van der Stelt M.

J Am Chem Soc. 2018 May 16;140(19):6067-6075. doi: 10.1021/jacs.7b11281. Epub 2018 Feb 16.

3.

From Structure-Activity Relationships on Thiazole Derivatives to the In Vivo Evaluation of a New Radiotracer for Cannabinoid Subtype 2 PET Imaging.

Caillé F, Cacheux F, Peyronneau MA, Jego B, Jaumain E, Pottier G, Ullmer C, Grether U, Winkeler A, Dollé F, Damont A, Kuhnast B.

Mol Pharm. 2017 Nov 6;14(11):4064-4078. doi: 10.1021/acs.molpharmaceut.7b00746. Epub 2017 Oct 18.

PMID:
28968497
4.

A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies.

Martella A, Sijben H, Rufer AC, Grether U, Fingerle J, Ullmer C, Hartung T, IJzerman AP, van der Stelt M, Heitman LH.

Mol Pharmacol. 2017 Oct;92(4):389-400. doi: 10.1124/mol.117.108605. Epub 2017 Jul 26.

5.

Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.

Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, van der Stelt M.

Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958.

6.

Novel Triazolopyrimidine-Derived Cannabinoid Receptor 2 Agonists as Potential Treatment for Inflammatory Kidney Diseases.

Nettekoven M, Adam JM, Bendels S, Bissantz C, Fingerle J, Grether U, Grüner S, Guba W, Kimbara A, Ottaviani G, Püllmann B, Rogers-Evans M, Röver S, Rothenhäusler B, Schmitt S, Schuler F, Schulz-Gasch T, Ullmer C.

ChemMedChem. 2016 Jan 19;11(2):179-89. doi: 10.1002/cmdc.201500218. Epub 2015 Jul 21.

PMID:
26228928
7.

Discovery of a high affinity and selective pyridine analog as a potential positron emission tomography imaging agent for cannabinoid type 2 receptor.

Slavik R, Grether U, Müller Herde A, Gobbi L, Fingerle J, Ullmer C, Krämer SD, Schibli R, Mu L, Ametamey SM.

J Med Chem. 2015 May 28;58(10):4266-77. doi: 10.1021/acs.jmedchem.5b00283. Epub 2015 May 14.

PMID:
25950914
8.

Highly potent and selective cannabinoid receptor 2 agonists: initial hit optimization of an adamantyl hit series identified from high-through-put screening.

Nettekoven M, Fingerle J, Grether U, Grüner S, Kimbara A, Püllmann B, Rogers-Evans M, Röver S, Schuler F, Schulz-Gasch T, Ullmer C.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1177-81. doi: 10.1016/j.bmcl.2013.01.044. Epub 2013 Jan 23.

PMID:
23380378
9.

Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors.

Dietz M, Mohr P, Kuhn B, Maerki HP, Hartman P, Ruf A, Benz J, Grether U, Wright MB.

ChemMedChem. 2012 Jun;7(6):1101-11. doi: 10.1002/cmdc.201100598. Epub 2012 Apr 4.

10.

Impedance measurement: a new method to detect ligand-biased receptor signaling.

Kammermann M, Denelavas A, Imbach A, Grether U, Dehmlow H, Apfel CM, Hertel C.

Biochem Biophys Res Commun. 2011 Sep 2;412(3):419-24. doi: 10.1016/j.bbrc.2011.07.087. Epub 2011 Jul 30.

PMID:
21827738
11.

G protein-coupled receptor transmembrane binding pockets and their applications in GPCR research and drug discovery: a survey.

Kratochwil NA, Gatti-McArthur S, Hoener MC, Lindemann L, Christ AD, Green LG, Guba W, Martin RE, Malherbe P, Porter RH, Slack JP, Winnig M, Dehmlow H, Grether U, Hertel C, Narquizian R, Panousis CG, Kolczewski S, Steward L.

Curr Top Med Chem. 2011;11(15):1902-24.

PMID:
21470172
12.

Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.

Richter HG, Benson GM, Bleicher KH, Blum D, Chaput E, Clemann N, Feng S, Gardes C, Grether U, Hartman P, Kuhn B, Martin RE, Plancher JM, Rudolph MG, Schuler F, Taylor S.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1134-40. doi: 10.1016/j.bmcl.2010.12.123. Epub 2010 Dec 31.

PMID:
21269824
13.

Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes.

Richter HG, Benson GM, Blum D, Chaput E, Feng S, Gardes C, Grether U, Hartman P, Kuhn B, Martin RE, Plancher JM, Rudolph MG, Schuler F, Taylor S, Bleicher KH.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):191-4. doi: 10.1016/j.bmcl.2010.11.039. Epub 2010 Nov 12.

PMID:
21134747
14.

New Insights on the mechanism of PPAR-targeted drugs.

Grether U, Klaus W, Kuhn B, Maerki HP, Mohr P, Wright MB.

ChemMedChem. 2010 Dec 3;5(12):1973-6. doi: 10.1002/cmdc.201000446. No abstract available.

PMID:
21069658
15.

Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.

Peters JU, Kühne H, Dehmlow H, Grether U, Conte A, Hainzl D, Hertel C, Kratochwil NA, Otteneder M, Narquizian R, Panousis CG, Ricklin F, Röver S.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5426-30. doi: 10.1016/j.bmcl.2010.07.108. Epub 2010 Jul 29.

PMID:
20724150
16.

Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.

Bénardeau A, Benz J, Binggeli A, Blum D, Boehringer M, Grether U, Hilpert H, Kuhn B, Märki HP, Meyer M, Püntener K, Raab S, Ruf A, Schlatter D, Mohr P.

Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. doi: 10.1016/j.bmcl.2009.03.036. Epub 2009 Mar 14.

PMID:
19349176
17.

Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist.

Feng S, Yang M, Zhang Z, Wang Z, Hong D, Richter H, Benson GM, Bleicher K, Grether U, Martin RE, Plancher JM, Kuhn B, Rudolph MG, Chen L.

Bioorg Med Chem Lett. 2009 May 1;19(9):2595-8. doi: 10.1016/j.bmcl.2009.03.008. Epub 2009 Mar 9.

PMID:
19328688
18.

Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists.

Grether U, Bénardeau A, Benz J, Binggeli A, Blum D, Hilpert H, Kuhn B, Märki HP, Meyer M, Mohr P, Püntener K, Raab S, Ruf A, Schlatter D.

ChemMedChem. 2009 Jun;4(6):951-6. doi: 10.1002/cmdc.200800425.

PMID:
19326383
19.

Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.

Kuhn B, Hilpert H, Benz J, Binggeli A, Grether U, Humm R, Märki HP, Meyer M, Mohr P.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4016-20. Epub 2006 Jun 5.

PMID:
16737814
20.

Multistep solid-phase synthesis of an antibiotic and receptor tyrosine kinase inhibitors using the traceless phenylhydrazide linker.

Stieber F, Grether U, Mazitschek R, Soric N, Giannis A, Waldmann H.

Chemistry. 2003 Jul 21;9(14):3282-91.

PMID:
12866072
21.

Development of the traceless phenylhydrazide linker for solid-phase synthesis.

Stieber F, Grether U, Waldmann H.

Chemistry. 2003 Jul 21;9(14):3270-81.

PMID:
12866071
22.

An enzyme-labile safety catch linker for synthesis on a soluble polymeric support.

Grether U, Waldmann H.

Chemistry. 2001 Mar 2;7(5):959-71.

PMID:
11303876
23.
24.

An oxidation-labile traceless linker for solid-phase synthesis.

Stieber F, Grether U, Waldmann H.

Angew Chem Int Ed Engl. 1999;38(8):1073-7. doi: 10.1002/(SICI)1521-3773(19990419)38:8<1073::AID-ANIE1073>3.0.CO;2-Y.

PMID:
25138498
25.

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