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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: holton sj. 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.
Coordination of Di-Acetylated Histone Ligands by the ATAD2 Bromodomain.
Evans CM, Phillips M, Malone KL, Tonelli M, Cornilescu G, Cornilescu C, Holton SJ, Gorjánácz M, Wang L, Carlson S, Gay JC, Nix JC, Demeler B, Markley JL, Glass KC. Evans CM, et al. Among authors: holton sj. Int J Mol Sci. 2021 Aug 24;22(17):9128. doi: 10.3390/ijms22179128. Int J Mol Sci. 2021. PMID: 34502039 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: holton sj. 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.
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: holton sj. 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
Functional and Structural Characterization of Bub3·BubR1 Interactions Required for Spindle Assembly Checkpoint Signaling in Human Cells.
Prinz F, Puetter V, Holton SJ, Andres D, Stegmann CM, Kwiatkowski D, Prechtl S, Petersen K, Beckmann G, Kreft B, Mumberg D, Fernández-Montalván A. Prinz F, et al. Among authors: holton sj. J Biol Chem. 2016 May 20;291(21):11252-67. doi: 10.1074/jbc.M115.702142. Epub 2016 Mar 30. J Biol Chem. 2016. PMID: 27030009 Free PMC article.
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: holton sj. 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
The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models.
Lemos C, Schulze VK, Baumgart SJ, Nevedomskaya E, Heinrich T, Lefranc J, Bader B, Christ CD, Briem H, Kuhnke LP, Holton SJ, Bömer U, Lienau P, von Nussbaum F, Nising CF, Bauser M, Hägebarth A, Mumberg D, Haendler B. Lemos C, et al. Among authors: holton sj. Cell Oncol (Dordr). 2021 Jun;44(3):581-594. doi: 10.1007/s13402-020-00584-8. Epub 2021 Jan 25. Cell Oncol (Dordr). 2021. PMID: 33492659
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A. Nguyen D, et al. Among authors: holton sj. J Med Chem. 2019 Jan 24;62(2):928-940. doi: 10.1021/acs.jmedchem.8b01606. Epub 2019 Jan 9. J Med Chem. 2019. PMID: 30563338
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.
Lücking U, Wortmann L, Wengner AM, Lefranc J, Lienau P, Briem H, Siemeister G, Bömer U, Denner K, Schäfer M, Koppitz M, Eis K, Bartels F, Bader B, Bone W, Moosmayer D, Holton SJ, Eberspächer U, Grudzinska-Goebel J, Schatz C, Deeg G, Mumberg D, von Nussbaum F. Lücking U, et al. Among authors: holton sj. J Med Chem. 2020 Jul 9;63(13):7293-7325. doi: 10.1021/acs.jmedchem.0c00369. Epub 2020 Jun 28. J Med Chem. 2020. PMID: 32502336
38 results