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The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML.
Gerlach D, Tontsch-Grunt U, Baum A, Popow J, Scharn D, Hofmann MH, Engelhardt H, Kaya O, Beck J, Schweifer N, Gerstberger T, Zuber J, Savarese F, Kraut N. Gerlach D, et al. Among authors: tontsch grunt u. Oncogene. 2018 May;37(20):2687-2701. doi: 10.1038/s41388-018-0150-2. Epub 2018 Mar 1. Oncogene. 2018. PMID: 29491412 Free PMC article.
Efficacy and mechanism of action of volasertib, a potent and selective inhibitor of Polo-like kinases, in preclinical models of acute myeloid leukemia.
Rudolph D, Impagnatiello MA, Blaukopf C, Sommer C, Gerlich DW, Roth M, Tontsch-Grunt U, Wernitznig A, Savarese F, Hofmann MH, Albrecht C, Geiselmann L, Reschke M, Garin-Chesa P, Zuber J, Moll J, Adolf GR, Kraut N. Rudolph D, et al. Among authors: tontsch grunt u. J Pharmacol Exp Ther. 2015 Mar;352(3):579-89. doi: 10.1124/jpet.114.221150. Epub 2015 Jan 9. J Pharmacol Exp Ther. 2015. PMID: 25576074
Transcriptional plasticity promotes primary and acquired resistance to BET inhibition.
Rathert P, Roth M, Neumann T, Muerdter F, Roe JS, Muhar M, Deswal S, Cerny-Reiterer S, Peter B, Jude J, Hoffmann T, Boryń ŁM, Axelsson E, Schweifer N, Tontsch-Grunt U, Dow LE, Gianni D, Pearson M, Valent P, Stark A, Kraut N, Vakoc CR, Zuber J. Rathert P, et al. Among authors: tontsch grunt u. Nature. 2015 Sep 24;525(7570):543-547. doi: 10.1038/nature14898. Epub 2015 Sep 14. Nature. 2015. PMID: 26367798 Free PMC article.
Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases.
Sini P, Gürtler U, Zahn SK, Baumann C, Rudolph D, Baumgartinger R, Strauss E, Haslinger C, Tontsch-Grunt U, Waizenegger IC, Solca F, Bader G, Zoephel A, Treu M, Reiser U, Garin-Chesa P, Boehmelt G, Kraut N, Quant J, Adolf GR. Sini P, et al. Among authors: tontsch grunt u. Mol Cancer Ther. 2016 Oct;15(10):2388-2398. doi: 10.1158/1535-7163.MCT-16-0066. Epub 2016 Aug 5. Mol Cancer Ther. 2016. PMID: 27496137
Triple Angiokinase Inhibitor Nintedanib Directly Inhibits Tumor Cell Growth and Induces Tumor Shrinkage via Blocking Oncogenic Receptor Tyrosine Kinases.
Hilberg F, Tontsch-Grunt U, Baum A, Le AT, Doebele RC, Lieb S, Gianni D, Voss T, Garin-Chesa P, Haslinger C, Kraut N. Hilberg F, et al. Among authors: tontsch grunt u. J Pharmacol Exp Ther. 2018 Mar;364(3):494-503. doi: 10.1124/jpet.117.244129. Epub 2017 Dec 20. J Pharmacol Exp Ther. 2018. PMID: 29263244 Free PMC article.
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