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Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.
Gradl S, Steuber H, Weiske J, Szewczyk MM, Schmees N, Siegel S, Stoeckigt D, Christ CD, Li F, Organ S, Abbey M, Kennedy S, Chau I, Trush V, Barsyte-Lovejoy D, Brown PJ, Vedadi M, Arrowsmith C, Husemann M, Badock V, Bauser M, Haegebarth A, Hartung IV, Stresemann C. Gradl S, et al. Among authors: hartung iv. SLAS Discov. 2021 Sep;26(8):947-960. doi: 10.1177/24725552211019409. Epub 2021 Jun 21. SLAS Discov. 2021. PMID: 34154424 Free article.
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Eggert E, Hillig RC, Koehr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernandez-Montalvan AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C. Eggert E, et al. Among authors: hartung iv. J Med Chem. 2016 May 26;59(10):4578-600. doi: 10.1021/acs.jmedchem.5b01890. Epub 2016 May 3. J Med Chem. 2016. PMID: 27075367 Free PMC article.
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett J, Monteiro O, Díaz-Sáez L, Siejka P, Meier J, Pütter V, Weiske J, Müller S, Huber KVM, Hartung IV, Haendler B. Bouché L, et al. Among authors: hartung iv. J Med Chem. 2017 May 11;60(9):4002-4022. doi: 10.1021/acs.jmedchem.7b00306. Epub 2017 May 1. J Med Chem. 2017. PMID: 28402630 Free PMC article.
Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.
Fernández-Montalván AE, Berger M, Kuropka B, Koo SJ, Badock V, Weiske J, Puetter V, Holton SJ, Stöckigt D, Ter Laak A, Centrella PA, Clark MA, Dumelin CE, Sigel EA, Soutter HH, Troast DM, Zhang Y, Cuozzo JW, Keefe AD, Roche D, Rodeschini V, Chaikuad A, Díaz-Sáez L, Bennett JM, Fedorov O, Huber KVM, Hübner J, Weinmann H, Hartung IV, Gorjánácz M. Fernández-Montalván AE, et al. Among authors: hartung iv. ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24. ACS Chem Biol. 2017. PMID: 29043777 Free PMC article.
Rational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics*.
Sutherland M, Li A, Kaghad A, Panagopoulos D, Li F, Szewczyk M, Smil D, Scholten C, Bouché L, Stellfeld T, Arrowsmith CH, Barsyte D, Vedadi M, Hartung IV, Steuber H, Britton R, Santhakumar V. Sutherland M, et al. Among authors: hartung iv. ChemMedChem. 2021 Apr 8;16(7):1116-1125. doi: 10.1002/cmdc.202100018. Epub 2021 Mar 4. ChemMedChem. 2021. PMID: 33513288
Targeting the aryl hydrocarbon receptor (AhR) with BAY 2416964: a selective small molecule inhibitor for cancer immunotherapy.
Kober C, Roewe J, Schmees N, Roese L, Roehn U, Bader B, Stoeckigt D, Prinz F, Gorjánácz M, Roider HG, Olesch C, Leder G, Irlbacher H, Lesche R, Lefranc J, Oezcan-Wahlbrink M, Batra AS, Elmadany N, Carretero R, Sahm K, Oezen I, Cichon F, Baumann D, Sadik A, Opitz CA, Weinmann H, Hartung IV, Kreft B, Offringa R, Platten M, Gutcher I. Kober C, et al. Among authors: hartung iv. J Immunother Cancer. 2023 Nov;11(11):e007495. doi: 10.1136/jitc-2023-007495. J Immunother Cancer. 2023. PMID: 37963637 Free PMC article.
A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition.
Falkenstern L, Georgi V, Bunse S, Badock V, Husemann M, Roehn U, Stellfeld T, Fitzgerald M, Ferrara S, Stöckigt D, Stresemann C, Hartung IV, Fernández-Montalván A. Falkenstern L, et al. Among authors: hartung iv. Sci Rep. 2024 Jan 19;14(1):1739. doi: 10.1038/s41598-023-50964-x. Sci Rep. 2024. PMID: 38242973 Free PMC article.
34 results