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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. 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: fernandez montalvan ae. 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.
Super-enhancers define a proliferative PGC-1α-expressing melanoma subgroup sensitive to BET inhibition.
Gelato KA, Schöckel L, Klingbeil O, Rückert T, Lesche R, Toedling J, Kalfon E, Héroult M, Lejeune P, Mönning U, Fernández-Montalván AE, Bäurle S, Siegel S, Haendler B. Gelato KA, et al. Among authors: fernandez montalvan ae. Oncogene. 2018 Jan 25;37(4):512-521. doi: 10.1038/onc.2017.325. Epub 2017 Oct 9. Oncogene. 2018. PMID: 28991225 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. 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.
Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo.
Siemeister G, Mengel A, Fernández-Montalván AE, Bone W, Schröder J, Zitzmann-Kolbe S, Briem H, Prechtl S, Holton SJ, Mönning U, von Ahsen O, Johanssen S, Cleve A, Pütter V, Hitchcock M, von Nussbaum F, Brands M, Ziegelbauer K, Mumberg D. Siemeister G, et al. Among authors: fernandez montalvan ae. Clin Cancer Res. 2019 Feb 15;25(4):1404-1414. doi: 10.1158/1078-0432.CCR-18-0628. Epub 2018 Nov 14. Clin Cancer Res. 2019. PMID: 30429199
Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase.
Schulze VK, Klar U, Kosemund D, Wengner AM, Siemeister G, Stöckigt D, Neuhaus R, Lienau P, Bader B, Prechtl S, Holton SJ, Briem H, Marquardt T, Schirok H, Jautelat R, Bohlmann R, Nguyen D, Fernández-Montalván AE, Bömer U, Eberspaecher U, Brüning M, Döhr O, Raschke M, Kreft B, Mumberg D, Ziegelbauer K, Brands M, von Nussbaum F, Koppitz M. Schulze VK, et al. Among authors: fernandez montalvan ae. J Med Chem. 2020 Aug 13;63(15):8025-8042. doi: 10.1021/acs.jmedchem.9b02035. Epub 2020 Apr 27. J Med Chem. 2020. PMID: 32338514
Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis.
Sugawara T, Nevedomskaya E, Heller S, Böhme A, Lesche R, von Ahsen O, Grünewald S, Nguyen HM, Corey E, Baumgart SJ, Georgi V, Pütter V, Fernández-Montalván A, Vasta JD, Robers MB, Politz O, Mumberg D, Haendler B. Sugawara T, et al. Mol Oncol. 2024 Mar;18(3):726-742. doi: 10.1002/1878-0261.13577. Epub 2024 Jan 15. Mol Oncol. 2024. PMID: 38225213 Free PMC article.
36 results