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Items: 1 to 50 of 208

1.

Structure optimization of a new class of PPARγ antagonists.

Hernandez-Olmos V, Knape T, Heering J, von Knethen A, Kilu W, Kaiser A, Wurglics M, Helmstädter M, Merk D, Schubert-Zsilavecz M, Parnham MJ, Steinhilber D, Proschak E.

Bioorg Med Chem. 2019 Nov 1;27(21):115082. doi: 10.1016/j.bmc.2019.115082. Epub 2019 Aug 27.

PMID:
31548084
2.

Molecular tuning of farnesoid X receptor partial agonism.

Merk D, Sreeramulu S, Kudlinzki D, Saxena K, Linhard V, Gande SL, Hiller F, Lamers C, Nilsson E, Aagaard A, Wissler L, Dekker N, Bamberg K, Schubert-Zsilavecz M, Schwalbe H.

Nat Commun. 2019 Jul 2;10(1):2915. doi: 10.1038/s41467-019-10853-2.

3.

Zafirlukast Is a Dual Modulator of Human Soluble Epoxide Hydrolase and Peroxisome Proliferator-Activated Receptor γ.

Göbel T, Diehl O, Heering J, Merk D, Angioni C, Wittmann SK, Buscato E, Kottke R, Weizel L, Schader T, Maier TJ, Geisslinger G, Schubert-Zsilavecz M, Steinhilber D, Proschak E, Kahnt AS.

Front Pharmacol. 2019 Mar 20;10:263. doi: 10.3389/fphar.2019.00263. eCollection 2019.

4.

Detection of lawsone (2-hydroxy-1,4-naphthoquinone) in henna treated hair.

Petzel-Witt S, Meier SI, Schubert-Zsilavecz M, Toennes SW.

Forensic Sci Int. 2019 Apr;297:184-188. doi: 10.1016/j.forsciint.2019.01.037. Epub 2019 Feb 6.

PMID:
30802647
5.

Urate transporter inhibitor lesinurad is a selective peroxisome proliferator-activated receptor gamma modulator (sPPARγM) in vitro.

Heitel P, Gellrich L, Heering J, Goebel T, Kahnt A, Proschak E, Schubert-Zsilavecz M, Merk D.

Sci Rep. 2018 Sep 10;8(1):13554. doi: 10.1038/s41598-018-31833-4.

6.

Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation.

Cheung SY, Werner M, Esposito L, Troisi F, Cantone V, Liening S, König S, Gerstmeier J, Koeberle A, Bilancia R, Rizza R, Rossi A, Roviezzo F, Temml V, Schuster D, Stuppner H, Schubert-Zsilavecz M, Werz O, Hanke T, Pace S.

Eur J Med Chem. 2018 Aug 5;156:815-830. doi: 10.1016/j.ejmech.2018.07.031. Epub 2018 Jul 25.

PMID:
30053720
7.

Allosteric modulation of the farnesoid X receptor by a small molecule.

Gabler M, Kramer J, Schmidt J, Pollinger J, Weber J, Kaiser A, Löhr F, Proschak E, Schubert-Zsilavecz M, Merk D.

Sci Rep. 2018 May 1;8(1):6846. doi: 10.1038/s41598-018-25158-5.

8.

Combined Approach of Backbone Amide Linking and On-Resin N-Methylation for the Synthesis of Bioactive and Metabolically Stable Peptides.

Wesche F, Adihou H, Kaiser A, Wurglics M, Schubert-Zsilavecz M, Kaiser M, Bode HB.

J Med Chem. 2018 May 10;61(9):3930-3938. doi: 10.1021/acs.jmedchem.7b01809. Epub 2018 Apr 20.

PMID:
29660276
9.

MH84 improves mitochondrial dysfunction in a mouse model of early Alzheimer's disease.

Pohland M, Pellowska M, Asseburg H, Hagl S, Reutzel M, Joppe A, Berressem D, Eckert SH, Wurglics M, Schubert-Zsilavecz M, Eckert GP.

Alzheimers Res Ther. 2018 Feb 13;10(1):18. doi: 10.1186/s13195-018-0342-6.

10.

PTCA (1H-pyrrole-2,3,5-tricarboxylic acid) as a marker for oxidative hair treatment.

Petzel-Witt S, Meier SI, Schubert-Zsilavecz M, Toennes SW.

Drug Test Anal. 2018 Apr;10(4):768-773. doi: 10.1002/dta.2305. Epub 2017 Nov 17.

PMID:
28940782
11.

Nonacidic Farnesoid X Receptor Modulators.

Flesch D, Cheung SY, Schmidt J, Gabler M, Heitel P, Kramer J, Kaiser A, Hartmann M, Lindner M, Lüddens-Dämgen K, Heering J, Lamers C, Lüddens H, Wurglics M, Proschak E, Schubert-Zsilavecz M, Merk D.

J Med Chem. 2017 Aug 24;60(16):7199-7205. doi: 10.1021/acs.jmedchem.7b00903. Epub 2017 Aug 8.

PMID:
28749691
12.

Quantification of active ingredients in semi-solid pharmaceutical formulations by near infrared spectroscopy.

Schlegel LB, Schubert-Zsilavecz M, Abdel-Tawab M.

J Pharm Biomed Anal. 2017 Aug 5;142:178-189. doi: 10.1016/j.jpba.2017.04.048. Epub 2017 May 6.

PMID:
28514717
13.

Influence of bleaching and coloring on ethyl glucuronide content in human hair.

Petzel-Witt S, Pogoda W, Wunder C, Paulke A, Schubert-Zsilavecz M, Toennes SW.

Drug Test Anal. 2018 Jan;10(1):177-183. doi: 10.1002/dta.2206. Epub 2017 Jun 22.

PMID:
28407398
14.

Analysis of drugs of abuse in Cerumen - correlation of postmortem analysis results with those for blood, urine and hair.

Meier SI, Koelzer SC, Schubert-Zsilavecz M, Toennes SW.

Drug Test Anal. 2017 Oct;9(10):1572-1585. doi: 10.1002/dta.2177. Epub 2017 Apr 12.

PMID:
28240418
15.

Transepithelial Transport of Curcumin in Caco-2 Cells Is significantly Enhanced by Micellar Solubilisation.

Frank J, Schiborr C, Kocher A, Meins J, Behnam D, Schubert-Zsilavecz M, Abdel-Tawab M.

Plant Foods Hum Nutr. 2017 Mar;72(1):48-53. doi: 10.1007/s11130-016-0587-9.

16.

Prunella vulgaris L. active components and their hypoglycemic and antinociceptive effects in alloxan-induced diabetic mice.

Raafat K, Wurglics M, Schubert-Zsilavecz M.

Biomed Pharmacother. 2016 Dec;84:1008-1018. doi: 10.1016/j.biopha.2016.09.095. Epub 2016 Oct 18.

PMID:
27768926
17.

A single-dose, randomized, cross-over, two-way, open-label study for comparing the absorption of boswellic acids and its lecithin formulation.

Riva A, Morazzoni P, Artaria C, Allegrini P, Meins J, Savio D, Appendino G, Schubert-Zsilavecz M, Abdel-Tawab M.

Phytomedicine. 2016 Nov 15;23(12):1375-1382. doi: 10.1016/j.phymed.2016.07.009. Epub 2016 Jul 27.

18.

Characterization of the molecular mechanism of 5-lipoxygenase inhibition by 2-aminothiazoles.

Kretschmer SB, Woltersdorf S, Vogt D, Lillich FF, Rühl M, Karas M, Maucher IV, Roos J, Häfner AK, Kaiser A, Wurglics M, Schubert-Zsilavecz M, Angioni C, Geisslinger G, Stark H, Steinhilber D, Hofmann B.

Biochem Pharmacol. 2017 Jan 1;123:52-62. doi: 10.1016/j.bcp.2016.09.021. Epub 2016 Sep 23.

PMID:
27671344
19.

Survey on the Quality of the Top-Selling European and American Botanical Dietary Supplements Containing Boswellic Acids.

Meins J, Artaria C, Riva A, Morazzoni P, Schubert-Zsilavecz M, Abdel-Tawab M.

Planta Med. 2016 Apr;82(6):573-9. doi: 10.1055/s-0042-103497. Epub 2016 Apr 7.

PMID:
27054914
20.

Substrate-specific effects of pirinixic acid derivatives on ABCB1-mediated drug transport.

Michaelis M, Rothweiler F, Wurglics M, Aniceto N, Dittrich M, Zettl H, Wiese M, Wass M, Ghafourian T, Schubert-Zsilavecz M, Cinatl J.

Oncotarget. 2016 Mar 8;7(10):11664-76. doi: 10.18632/oncotarget.7345.

21.

SAR studies on FXR modulators led to the discovery of the first combined FXR antagonistic/TGR5 agonistic compound.

Lamers C, Merk D, Gabler M, Flesch D, Kaiser A, Schubert-Zsilavecz M.

Future Med Chem. 2016;8(2):133-48. doi: 10.4155/fmc.15.178. Epub 2016 Jan 29.

PMID:
26824277
22.

MH84: A Novel γ-Secretase Modulator/PPARγ Agonist--Improves Mitochondrial Dysfunction in a Cellular Model of Alzheimer's Disease.

Pohland M, Hagl S, Pellowska M, Wurglics M, Schubert-Zsilavecz M, Eckert GP.

Neurochem Res. 2016 Feb;41(1-2):231-42. doi: 10.1007/s11064-015-1765-0. Epub 2015 Dec 31.

PMID:
26721513
23.

Small molecules with anti-inflammatory properties in clinical development.

Hanke T, Merk D, Steinhilber D, Geisslinger G, Schubert-Zsilavecz M.

Pharmacol Ther. 2016 Jan;157:163-87. doi: 10.1016/j.pharmthera.2015.11.011. Epub 2015 Nov 26. Review.

PMID:
26627986
24.

N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.

Blöcher R, Lamers C, Wittmann SK, Merk D, Hartmann M, Weizel L, Diehl O, Brüggerhoff A, Boß M, Kaiser A, Schader T, Göbel T, Grundmann M, Angioni C, Heering J, Geisslinger G, Wurglics M, Kostenis E, Brüne B, Steinhilber D, Schubert-Zsilavecz M, Kahnt AS, Proschak E.

J Med Chem. 2016 Jan 14;59(1):61-81. doi: 10.1021/acs.jmedchem.5b01239. Epub 2015 Dec 25.

PMID:
26595749
25.

NSAIDs Ibuprofen, Indometacin, and Diclofenac do not interact with Farnesoid X Receptor.

Schmidt J, Klingler FM, Proschak E, Steinhilber D, Schubert-Zsilavecz M, Merk D.

Sci Rep. 2015 Oct 1;5:14782. doi: 10.1038/srep14782.

26.
27.

Detection of oxidative hair treatment using fluorescence microscopy.

Witt S, Wunder C, Paulke A, Verhoff MA, Schubert-Zsilavecz M, Toennes SW.

Drug Test Anal. 2016 Aug;8(8):826-31. doi: 10.1002/dta.1854. Epub 2015 Sep 11.

PMID:
26359937
28.

Pirinixic acids: flexible fatty acid mimetics with various biological activities.

Merk D, Zettl M, Steinhilber D, Werz O, Schubert-Zsilavecz M.

Future Med Chem. 2015 Aug;7(12):1597-616. doi: 10.4155/fmc.15.87. Epub 2015 Aug 27. Review.

PMID:
26313377
29.

Dosing Accuracy of Two Disposable Insulin Pens According to New ISO 11608-1: 2012 Requirements.

Abdel-Tawab M, Schmitz M, Kamlot S, Schubert-Zsilavecz M.

J Diabetes Sci Technol. 2015 Jul 17;10(1):157-61. doi: 10.1177/1932296815595983.

30.

Natural compound renews hope for diabetes and obesity therapeutic target.

Merk D, Schubert-Zsilavecz M.

Future Med Chem. 2015;7(7):833-5. doi: 10.4155/fmc.15.40. No abstract available.

PMID:
26061101
31.

Detection of pyrrolizidine alkaloids in German licensed herbal medicinal teas.

Schulz M, Meins J, Diemert S, Zagermann-Muncke P, Goebel R, Schrenk D, Schubert-Zsilavecz M, Abdel-Tawab M.

Phytomedicine. 2015 Jun 1;22(6):648-56. doi: 10.1016/j.phymed.2015.03.020. Epub 2015 Apr 29.

PMID:
26055130
32.

Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties.

Flesch D, Gabler M, Lill A, Gomez RC, Steri R, Schneider G, Stark H, Schubert-Zsilavecz M, Merk D.

Bioorg Med Chem. 2015 Jul 1;23(13):3490-8. doi: 10.1016/j.bmc.2015.04.035. Epub 2015 Apr 18.

PMID:
25934227
33.

Studies on the alkaloid composition of the Hawaiian Baby Woodrose Argyreia nervosa, a common legal high.

Paulke A, Kremer C, Wunder C, Wurglics M, Schubert-Zsilavecz M, Toennes SW.

Forensic Sci Int. 2015 Apr;249:281-93. doi: 10.1016/j.forsciint.2015.02.011. Epub 2015 Feb 19.

PMID:
25747328
34.

Identification and characterisation of a prototype for a new class of competitive PPARγ antagonists.

Knape T, Flesch D, Kuchler L, Sha LK, Giegerich AK, Labocha S, Ferreirós N, Schmid T, Wurglics M, Schubert-Zsilavecz M, Proschak E, Brüne B, Parnham MJ, von Knethen A.

Eur J Pharmacol. 2015 May 15;755:16-26. doi: 10.1016/j.ejphar.2015.02.034. Epub 2015 Mar 5.

PMID:
25746464
35.

Anthranilic acid derivatives as nuclear receptor modulators--development of novel PPAR selective and dual PPAR/FXR ligands.

Merk D, Lamers C, Weber J, Flesch D, Gabler M, Proschak E, Schubert-Zsilavecz M.

Bioorg Med Chem. 2015 Feb 1;23(3):499-514. doi: 10.1016/j.bmc.2014.12.013. Epub 2014 Dec 19.

PMID:
25583100
36.

SAR-studies of γ-secretase modulators with PPARγ-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease.

Flesch D, Ness J, Lamers C, Dehm F, Popella S, Steri R, Ogorek I, Hieke M, Dannhardt G, Werz O, Weggen S, Schubert-Zsilavecz M.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):841-6. doi: 10.1016/j.bmcl.2014.12.073. Epub 2014 Dec 30.

PMID:
25575659
37.

Pharmacokinetic properties of MH84, a γ-secretase modulator with PPARγ agonistic activity.

Pellowska M, Stein C, Pohland M, Merk D, Klein J, Eckert GP, Schubert-Zsilavecz M, Wurglics M.

J Pharm Biomed Anal. 2015 Jan;102:417-24. doi: 10.1016/j.jpba.2014.10.001. Epub 2014 Oct 13.

PMID:
25459941
38.

Revealing the macromolecular targets of complex natural products.

Reker D, Perna AM, Rodrigues T, Schneider P, Reutlinger M, Mönch B, Koeberle A, Lamers C, Gabler M, Steinmetz H, Müller R, Schubert-Zsilavecz M, Werz O, Schneider G.

Nat Chem. 2014 Dec;6(12):1072-8. doi: 10.1038/nchem.2095. Epub 2014 Nov 2.

PMID:
25411885
39.

Medicinal chemistry and pharmacological effects of Farnesoid X Receptor (FXR) antagonists.

Lamers C, Schubert-Zsilavecz M, Merk D.

Curr Top Med Chem. 2014;14(19):2188-205. Review.

PMID:
25388533
40.

Vanillin-derived antiproliferative compounds influence Plk1 activity.

Carrasco-Gomez R, Keppner-Witter S, Hieke M, Lange L, Schneider G, Schubert-Zsilavecz M, Proschak E, Spänkuch B.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5063-9. doi: 10.1016/j.bmcl.2014.09.015. Epub 2014 Sep 16.

PMID:
25304894
41.

Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist.

Merk D, Lamers C, Ahmad K, Carrasco Gomez R, Schneider G, Steinhilber D, Schubert-Zsilavecz M.

J Med Chem. 2014 Oct 9;57(19):8035-55. doi: 10.1021/jm500937v. Epub 2014 Sep 25.

PMID:
25255039
42.

Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition.

Hanke T, Lamers C, Gomez RC, Schneider G, Werz O, Schubert-Zsilavecz M.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3757-63. doi: 10.1016/j.bmcl.2014.06.077. Epub 2014 Jul 3.

PMID:
25037914
43.

Identification of legal highs--ergot alkaloid patterns in two Argyreia nervosa products.

Paulke A, Kremer C, Wunder C, Wurglics M, Schubert-Zsilavecz M, Toennes SW.

Forensic Sci Int. 2014 Sep;242:62-71. doi: 10.1016/j.forsciint.2014.06.025. Epub 2014 Jun 30.

PMID:
25036782
44.

Molecular determinants for improved activity at PPARα: structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARα.

Lamers C, Dittrich M, Steri R, Proschak E, Schubert-Zsilavecz M.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):4048-52. doi: 10.1016/j.bmcl.2014.05.058. Epub 2014 Jun 11.

PMID:
25022880
45.

Anthranilic acid derivatives as novel ligands for farnesoid X receptor (FXR).

Merk D, Gabler M, Gomez RC, Flesch D, Hanke T, Kaiser A, Lamers C, Werz O, Schneider G, Schubert-Zsilavecz M.

Bioorg Med Chem. 2014 Apr 15;22(8):2447-60. doi: 10.1016/j.bmc.2014.02.053. Epub 2014 Mar 15.

PMID:
24685112
46.

Characterizing ligands for farnesoid X receptor--available in vitro test systems for farnesoid X receptor modulator development.

Merk D, Steinhilber D, Schubert-Zsilavecz M.

Expert Opin Drug Discov. 2014 Jan;9(1):27-37. doi: 10.1517/17460441.2014.860129. Epub 2013 Nov 21. Review.

PMID:
24261510
47.

Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.

Hanke T, Rörsch F, Thieme TM, Ferreiros N, Schneider G, Geisslinger G, Proschak E, Grösch S, Schubert-Zsilavecz M.

Bioorg Med Chem. 2013 Dec 15;21(24):7874-83. doi: 10.1016/j.bmc.2013.10.006. Epub 2013 Oct 16.

PMID:
24183739
48.

Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.

Hanke T, Dehm F, Liening S, Popella SD, Maczewsky J, Pillong M, Kunze J, Weinigel C, Barz D, Kaiser A, Wurglics M, Lämmerhofer M, Schneider G, Sautebin L, Schubert-Zsilavecz M, Werz O.

J Med Chem. 2013 Nov 27;56(22):9031-44. doi: 10.1021/jm401557w. Epub 2013 Nov 15.

PMID:
24171493
49.

Dose accuracy and injection force of different insulin glargine pens.

Friedrichs A, Bohnet J, Korger V, Adler S, Schubert-Zsilavecz M, Abdel-Tawab M.

J Diabetes Sci Technol. 2013 Sep 1;7(5):1346-53.

50.

Advances in personalized medicine - medicinal chemistry and pharmacology of vemurafenib and ivacaftor.

Pellowska M, Merk D, Schubert-Zsilavecz M.

Pharmazie. 2013 Jul;68(7):484-91. Review.

PMID:
23923627

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