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Items: 1 to 50 of 123

1.

2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.

Giroud M, Kuhn B, Saint-Auret S, Kuratli C, Martin RE, Schuler F, Diederich F, Kaiser M, Brun R, Schirmeister T, Haap W.

J Med Chem. 2018 Apr 26;61(8):3370-3388. doi: 10.1021/acs.jmedchem.7b01870. Epub 2018 Apr 6.

PMID:
29590751
2.

Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.

Giroud M, Dietzel U, Anselm L, Banner D, Kuglstatter A, Benz J, Blanc JB, Gaufreteau D, Liu H, Lin X, Stich A, Kuhn B, Schuler F, Kaiser M, Brun R, Schirmeister T, Kisker C, Diederich F, Haap W.

J Med Chem. 2018 Apr 26;61(8):3350-3369. doi: 10.1021/acs.jmedchem.7b01869. Epub 2018 Apr 13.

PMID:
29590750
3.

A Sensitive In Vitro Approach to Assess the Hybridization-Dependent Toxic Potential of High Affinity Gapmer Oligonucleotides.

Dieckmann A, Hagedorn PH, Burki Y, Brügmann C, Berrera M, Ebeling M, Singer T, Schuler F.

Mol Ther Nucleic Acids. 2018 Mar 2;10:45-54. doi: 10.1016/j.omtn.2017.11.004. Epub 2017 Nov 14.

4.

Checkpoint kinase 1 is essential for normal B cell development and lymphomagenesis.

Schuler F, Weiss JG, Lindner SE, Lohmüller M, Herzog S, Spiegl SF, Menke P, Geley S, Labi V, Villunger A.

Nat Commun. 2017 Nov 22;8(1):1697. doi: 10.1038/s41467-017-01850-4.

5.

The resurrection of the PIDDosome - emerging roles in the DNA-damage response and centrosome surveillance.

Sladky V, Schuler F, Fava LL, Villunger A.

J Cell Sci. 2017 Nov 15;130(22):3779-3787. doi: 10.1242/jcs.203448. Review.

6.

Signalling strength determines proapoptotic functions of STING.

Gulen MF, Koch U, Haag SM, Schuler F, Apetoh L, Villunger A, Radtke F, Ablasser A.

Nat Commun. 2017 Sep 5;8(1):427. doi: 10.1038/s41467-017-00573-w.

7.

The miR-15 family reinforces the transition from proliferation to differentiation in pre-B cells.

Lindner SE, Lohmüller M, Kotkamp B, Schuler F, Knust Z, Villunger A, Herzog S.

EMBO Rep. 2017 Sep;18(9):1604-1617. doi: 10.15252/embr.201643735. Epub 2017 Jul 13.

PMID:
28705801
8.

Electro-mechanical conditioning of human iPSC-derived cardiomyocytes for translational research.

Kroll K, Chabria M, Wang K, Häusermann F, Schuler F, Polonchuk L.

Prog Biophys Mol Biol. 2017 Nov;130(Pt B):212-222. doi: 10.1016/j.pbiomolbio.2017.07.003. Epub 2017 Jul 6.

PMID:
28688751
9.

Toward in vitro-to-in vivo translation of monoclonal antibody pharmacokinetics: Application of a neonatal Fc receptor-mediated transcytosis assay to understand the interplaying clearance mechanisms.

Jaramillo CAC, Belli S, Cascais AC, Dudal S, Edelmann MR, Haak M, Brun ME, Otteneder MB, Ullah M, Funk C, Schuler F, Simon S.

MAbs. 2017 Jul;9(5):781-791. doi: 10.1080/19420862.2017.1320008. Epub 2017 Apr 25.

10.

Application of Imaging Techniques to Cases of Drug-Induced Crystal Nephropathy in Preclinical Studies.

Lenz B, Brink A, Siam M, De Paepe A, Bassett S, Eichinger-Chapelon A, Maliver P, Neff R, Niederhauser U, Steinhuber B, Zurbach R, Singer T, Funk C, Schuler F, Albassam M, Schadt S.

Toxicol Sci. 2018 Jun 1;163(2):409-419. doi: 10.1093/toxsci/kfx044.

PMID:
28329870
11.

Inhibition of EGF Uptake by Nephrotoxic Antisense Drugs In Vitro and Implications for Preclinical Safety Profiling.

Moisan A, Gubler M, Zhang JD, Tessier Y, Dumong Erichsen K, Sewing S, Gérard R, Avignon B, Huber S, Benmansour F, Chen X, Villaseñor R, Braendli-Baiocco A, Festag M, Maunz A, Singer T, Schuler F, Roth AB.

Mol Ther Nucleic Acids. 2017 Mar 17;6:89-105. doi: 10.1016/j.omtn.2016.11.006. Epub 2016 Dec 10.

12.

The PIDDosome activates p53 in response to supernumerary centrosomes.

Fava LL, Schuler F, Sladky V, Haschka MD, Soratroi C, Eiterer L, Demetz E, Weiss G, Geley S, Nigg EA, Villunger A.

Genes Dev. 2017 Jan 1;31(1):34-45. doi: 10.1101/gad.289728.116.

13.

From the Cover: The Minipig is a Suitable Non-Rodent Model in the Safety Assessment of Single Stranded Oligonucleotides.

Braendli-Baiocco A, Festag M, Dumong Erichsen K, Persson R, Mihatsch MJ, Fisker N, Funk J, Mohr S, Constien R, Ploix C, Brady K, Berrera M, Altmann B, Lenz B, Albassam M, Schmitt G, Weiser T, Schuler F, Singer T, Tessier Y.

Toxicol Sci. 2017 May 1;157(1):112-128. doi: 10.1093/toxsci/kfx025.

14.

Crossed cerebellar diaschisis in acute ischemic stroke: Impact on morphologic and functional outcome.

Kunz WG, Sommer WH, Höhne C, Fabritius MP, Schuler F, Dorn F, Othman AE, Meinel FG, von Baumgarten L, Reiser MF, Ertl-Wagner B, Thierfelder KM.

J Cereb Blood Flow Metab. 2017 Nov;37(11):3615-3624. doi: 10.1177/0271678X16686594. Epub 2017 Jan 13.

PMID:
28084869
15.

Metabolic Profiling of Human Long-Term Liver Models and Hepatic Clearance Predictions from In Vitro Data Using Nonlinear Mixed-Effects Modeling.

Kratochwil NA, Meille C, Fowler S, Klammers F, Ekiciler A, Molitor B, Simon S, Walter I, McGinnis C, Walther J, Leonard B, Triyatni M, Javanbakht H, Funk C, Schuler F, Lavé T, Parrott NJ.

AAPS J. 2017 Mar;19(2):534-550. doi: 10.1208/s12248-016-0019-7. Epub 2017 Jan 3.

PMID:
28050713
16.

Minimizing the risk of chemically reactive metabolite formation of new drug candidates: implications for preclinical drug design.

Brink A, Pähler A, Funk C, Schuler F, Schadt S.

Drug Discov Today. 2017 May;22(5):751-756. doi: 10.1016/j.drudis.2016.11.018. Epub 2016 Nov 27.

PMID:
27903430
17.

Wavelet-Based Angiographic Reconstruction of Computed Tomography Perfusion Data: Diagnostic Value in Cerebral Venous Sinus Thrombosis.

Kunz WG, Schuler F, Sommer WH, Fabritius MP, Havla L, Meinel FG, Reiser MF, Ertl-Wagner B, Thierfelder KM.

Invest Radiol. 2017 May;52(5):302-309. doi: 10.1097/RLI.0000000000000337.

PMID:
27861231
18.

MYC selects against reduced BCL2A1/A1 protein expression during B cell lymphomagenesis.

Sochalska M, Schuler F, Weiss JG, Prchal-Murphy M, Sexl V, Villunger A.

Oncogene. 2017 Apr;36(15):2066-2073. doi: 10.1038/onc.2016.362. Epub 2016 Oct 3.

19.

Extension of the dissolution-precipitation model for kinetic elucidation of solvent-mediated polymorphic transformations.

Jakubiak P, Schuler F, Alvarez-Sánchez R.

Eur J Pharm Biopharm. 2016 Dec;109:43-48. doi: 10.1016/j.ejpb.2016.08.019. Epub 2016 Sep 17.

PMID:
27648958
20.

Simplified development of multiplex real-time PCR through master mix augmented by universal fluorogenic reporters.

Wadle S, Lehnert M, Schuler F, Köppel R, Serr A, Zengerle R, von Stetten F.

Biotechniques. 2016 Sep 1;61(3):123-8. doi: 10.2144/000114443. eCollection 2016.

21.

Establishment of a Predictive In Vitro Assay for Assessment of the Hepatotoxic Potential of Oligonucleotide Drugs.

Sewing S, Boess F, Moisan A, Bertinetti-Lapatki C, Minz T, Hedtjaern M, Tessier Y, Schuler F, Singer T, Roth AB.

PLoS One. 2016 Jul 21;11(7):e0159431. doi: 10.1371/journal.pone.0159431. eCollection 2016.

22.

Janus Kinase 1 Is Essential for Inflammatory Cytokine Signaling and Mammary Gland Remodeling.

Sakamoto K, Wehde BL, Yoo KH, Kim T, Rajbhandari N, Shin HY, Triplett AA, Rädler PD, Schuler F, Villunger A, Kang K, Hennighausen L, Wagner KU.

Mol Cell Biol. 2016 May 16;36(11):1673-90. doi: 10.1128/MCB.00999-15. Print 2016 Jun 1.

23.

Recent developments in using mechanistic cardiac modelling for drug safety evaluation.

Davies MR, Wang K, Mirams GR, Caruso A, Noble D, Walz A, Lavé T, Schuler F, Singer T, Polonchuk L.

Drug Discov Today. 2016 Jun;21(6):924-38. doi: 10.1016/j.drudis.2016.02.003. Epub 2016 Feb 15. Review.

24.

Monochrome Multiplexing in Polymerase Chain Reaction by Photobleaching of Fluorogenic Hydrolysis Probes.

Schuler F, Trotter M, Zengerle R, von Stetten F.

Anal Chem. 2016 Mar 1;88(5):2590-5. doi: 10.1021/acs.analchem.5b02960. Epub 2016 Feb 16.

PMID:
26840905
25.

Development of a Unified Dissolution and Precipitation Model and Its Use for the Prediction of Oral Drug Absorption.

Jakubiak P, Wagner B, Grimm HP, Petrig-Schaffland J, Schuler F, Alvarez-Sánchez R.

Mol Pharm. 2016 Feb 1;13(2):586-98. doi: 10.1021/acs.molpharmaceut.5b00808. Epub 2016 Jan 5.

PMID:
26674605
26.

Digital droplet PCR on disk.

Schuler F, Trotter M, Geltman M, Schwemmer F, Wadle S, Domínguez-Garrido E, López M, Cervera-Acedo C, Santibáñez P, von Stetten F, Zengerle R, Paust N.

Lab Chip. 2016 Jan 7;16(1):208-16. doi: 10.1039/c5lc01068c.

PMID:
26610263
27.

Estimation of Drug Binding to Brain Tissue: Methodology and in Vivo Application of a Distribution Assay in Brain Polar Lipids.

Belli S, Assmus F, Wagner B, Honer M, Fischer H, Schuler F, Alvarez-Sánchez R.

Mol Pharm. 2015 Dec 7;12(12):4529-41. doi: 10.1021/acs.molpharmaceut.5b00717. Epub 2015 Nov 23.

PMID:
26560069
28.

Minimizing DILI risk in drug discovery - A screening tool for drug candidates.

Schadt S, Simon S, Kustermann S, Boess F, McGinnis C, Brink A, Lieven R, Fowler S, Youdim K, Ullah M, Marschmann M, Zihlmann C, Siegrist YM, Cascais AC, Di Lenarda E, Durr E, Schaub N, Ang X, Starke V, Singer T, Alvarez-Sanchez R, Roth AB, Schuler F, Funk C.

Toxicol In Vitro. 2015 Dec 25;30(1 Pt B):429-37. doi: 10.1016/j.tiv.2015.09.019. Epub 2015 Sep 25.

PMID:
26407524
29.

Shedding light on minipig drug metabolism - elevated amide hydrolysis in vitro.

Jones R, Marschmann M, Keller M, Qiu NH, Fowler S, Singer T, Schuler F, Funk C, Schadt S.

Xenobiotica. 2016;46(6):483-94. doi: 10.3109/00498254.2015.1089452. Epub 2015 Sep 25.

PMID:
26405846
30.

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
31.

The BH3-only protein BIM contributes to late-stage involution in the mouse mammary gland.

Schuler F, Baumgartner F, Klepsch V, Chamson M, Müller-Holzner E, Watson CJ, Oh S, Hennighausen L, Tymoszuk P, Doppler W, Villunger A.

Cell Death Differ. 2016 Jan;23(1):41-51. doi: 10.1038/cdd.2015.61. Epub 2015 Jun 5.

32.

Centrifugal step emulsification applied for absolute quantification of nucleic acids by digital droplet RPA.

Schuler F, Schwemmer F, Trotter M, Wadle S, Zengerle R, von Stetten F, Paust N.

Lab Chip. 2015 Jul 7;15(13):2759-66. doi: 10.1039/c5lc00291e. Epub 2015 May 7.

PMID:
25947077
33.

Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.

Ratni H, Rogers-Evans M, Bissantz C, Grundschober C, Moreau JL, Schuler F, Fischer H, Alvarez Sanchez R, Schnider P.

J Med Chem. 2015 Mar 12;58(5):2275-89. doi: 10.1021/jm501745f. Epub 2015 Feb 18.

PMID:
25654260
34.

Death of p53-defective cells triggered by forced mitotic entry in the presence of DNA damage is not uniquely dependent on Caspase-2 or the PIDDosome.

Manzl C, Fava LL, Krumschnabel G, Peintner L, Tanzer MC, Soratroi C, Bock FJ, Schuler F, Luef B, Geley S, Villunger A.

Cell Death Dis. 2013 Dec 5;4:e942. doi: 10.1038/cddis.2013.470.

35.

A liposomal fluorescence assay to study permeation kinetics of drug-like weak bases across the lipid bilayer.

Eyer K, Paech F, Schuler F, Kuhn P, Kissner R, Belli S, Dittrich PS, Krämer SD.

J Control Release. 2014 Jan 10;173:102-9. doi: 10.1016/j.jconrel.2013.10.037. Epub 2013 Nov 6.

PMID:
24211703
36.

Circulating t(14;18)-positive cells in healthy individuals: association with age and sex but not with smoking.

Hirt C, Weitmann K, Schüler F, Kiefer T, Rabkin CS, Hoffmann W, Dölken G.

Leuk Lymphoma. 2013 Dec;54(12):2678-84. doi: 10.3109/10428194.2013.788177. Epub 2013 May 7.

37.

Possible pitfalls investigating cell death responses in genetically engineered mouse models and derived cell lines.

Manzl C, Baumgartner F, Peintner L, Schuler F, Villunger A.

Methods. 2013 Jun 1;61(2):130-7. doi: 10.1016/j.ymeth.2013.02.012. Epub 2013 Feb 27.

38.

PK/PD assessment in CNS drug discovery: Prediction of CSF concentration in rodents for P-glycoprotein substrates and application to in vivo potency estimation.

Caruso A, Alvarez-Sánchez R, Hillebrecht A, Poirier A, Schuler F, Lavé T, Funk C, Belli S.

Biochem Pharmacol. 2013 Jun 1;85(11):1684-99. doi: 10.1016/j.bcp.2013.02.021. Epub 2013 Feb 27.

PMID:
23454189
39.

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
40.

Personalized chemotherapy profiling using cancer cell lines from selectable mice.

Kamiyama H, Rauenzahn S, Shim JS, Karikari CA, Feldmann G, Hua L, Kamiyama M, Schuler FW, Lin MT, Beaty RM, Karanam B, Liang H, Mullendore ME, Mo G, Hidalgo M, Jaffee E, Hruban RH, Jinnah HA, Roden RB, Jimeno A, Liu JO, Maitra A, Eshleman JR.

Clin Cancer Res. 2013 Mar 1;19(5):1139-46. doi: 10.1158/1078-0432.CCR-12-2127. Epub 2013 Jan 22.

41.

Hyperbranched polymeric ionic liquids with onion-like topology as transporters and compartmentalized systems.

Schüler F, Kerscher B, Beckert F, Thomann R, Mülhaupt R.

Angew Chem Int Ed Engl. 2013 Jan 2;52(1):455-8. doi: 10.1002/anie.201205130. Epub 2012 Nov 4.

PMID:
23125048
42.

Statistical analysis of results obtained by real-time PCR for improvement of absolute quantification of target sequences.

Kiefer T, Hirt C, Schüler F, Busemann C, Wodny M, Jaeger B, Dölken G.

Clin Lab. 2012;58(5-6):465-70.

PMID:
22783576
43.

Expression profiles of metabolic enzymes and drug transporters in the liver and along the intestine of beagle dogs.

Haller S, Schuler F, Lazic SE, Bachir-Cherif D, Krämer SD, Parrott NJ, Steiner G, Belli S.

Drug Metab Dispos. 2012 Aug;40(8):1603-10. doi: 10.1124/dmd.112.045443. Epub 2012 May 17.

44.

Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.

Poirier A, Belli S, Funk C, Otteneder MB, Portmann R, Heinig K, Prinssen E, Lazic SE, Rayner CR, Hoffmann G, Singer T, Smith DE, Schuler F.

Drug Metab Dispos. 2012 Aug;40(8):1556-65. doi: 10.1124/dmd.112.044990. Epub 2012 May 14.

45.

Delayed processing of bone marrow samples reveals a prognostic pattern of NME mRNA expression in cytogenetically normal acute myeloid leukemia.

Bach E, Krahl R, Lange T, Schüler F, Al-Ali H, Büchner T, Haferlach T, Dölken G, Niederwieser D, Cross M.

Leuk Lymphoma. 2012 Aug;53(8):1561-8. doi: 10.3109/10428194.2012.676176. Epub 2012 Apr 23.

PMID:
22421058
46.

Synthesis of macroporous polystyrene by the polymerization of foamed emulsions.

Schüler F, Schamel D, Salonen A, Drenckhan W, Gilchrist MD, Stubenrauch C.

Angew Chem Int Ed Engl. 2012 Feb 27;51(9):2213-7. doi: 10.1002/anie.201107806. Epub 2012 Jan 20. No abstract available.

47.

Long-term follow-up of high-dose chemotherapy with autologous stem-cell transplantation and response-adapted whole-brain radiotherapy for newly diagnosed primary CNS lymphoma: results of the multicenter Ostdeutsche Studiengruppe Hamatologie und Onkologie OSHO-53 phase II study.

Kiefer T, Hirt C, Späth C, Schüler F, Al-Ali HK, Wolf HH, Herbst R, Maschmeyer G, Helke K, Kessler C, Niederwieser D, Busemann C, Schroeder H, Vogelgesang S, Kirsch M, Montemurro M, Krüger WH, Dölken G; Ostdeutsche Studiengruppe Hämatologie und Onkologie.

Ann Oncol. 2012 Jul;23(7):1809-12. doi: 10.1093/annonc/mdr553. Epub 2011 Nov 24.

PMID:
22115927
48.

Characterization of post-surgical alterations in the bile duct-cannulated rat.

Bachir-Cherif D, Blum D, Braendli-Baiocco A, Chaput E, Pacheco GC, Flint N, Haiker M, Hoflack JC, Justies N, Neff R, Starke V, Steiner G, Tournillac CA, Singer T, Ubeaud-Séquier G, Schuler F.

Xenobiotica. 2011 Aug;41(8):701-11. doi: 10.3109/00498254.2011.565819. Epub 2011 Apr 27.

PMID:
21521079
49.

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
50.

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

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