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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: engelhardt h. 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.
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.
Engelhardt H, Böse D, Petronczki M, Scharn D, Bader G, Baum A, Bergner A, Chong E, Döbel S, Egger G, Engelhardt C, Ettmayer P, Fuchs JE, Gerstberger T, Gonnella N, Grimm A, Grondal E, Haddad N, Hopfgartner B, Kousek R, Krawiec M, Kriz M, Lamarre L, Leung J, Mayer M, Patel ND, Simov BP, Reeves JT, Schnitzer R, Schrenk A, Sharps B, Solca F, Stadtmüller H, Tan Z, Wunberg T, Zoephel A, McConnell DB. Engelhardt H, et al. Among authors: engelhardt c. J Med Chem. 2019 Nov 27;62(22):10272-10293. doi: 10.1021/acs.jmedchem.9b01169. Epub 2019 Nov 13. J Med Chem. 2019. PMID: 31689114 Free article.
Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance.
Hofmann MH, Mani R, Engelhardt H, Impagnatiello MA, Carotta S, Kerenyi M, Lorenzo-Herrero S, Böttcher J, Scharn D, Arnhof H, Zoephel A, Schnitzer R, Gerstberger T, Sanderson MP, Rajgolikar G, Goswami S, Vasu S, Ettmayer P, Gonzalez S, Pearson M, McConnell DB, Kraut N, Muthusamy N, Moll J. Hofmann MH, et al. Among authors: engelhardt h. Mol Cancer Ther. 2020 Apr;19(4):1018-1030. doi: 10.1158/1535-7163.MCT-19-0789. Epub 2020 Feb 5. Mol Cancer Ther. 2020. PMID: 32024684 Free PMC article.
Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling.
Wilding B, Scharn D, Böse D, Baum A, Santoro V, Chetta P, Schnitzer R, Botesteanu DA, Reiser C, Kornigg S, Knesl P, Hörmann A, Köferle A, Corcokovic M, Lieb S, Scholz G, Bruchhaus J, Spina M, Balla J, Peric-Simov B, Zimmer J, Mitzner S, Fett TN, Beran A, Lamarre L, Gerstberger T, Gerlach D, Bauer M, Bergner A, Schlattl A, Bader G, Treu M, Engelhardt H, Zahn S, Fuchs JE, Zuber J, Ettmayer P, Pearson M, Petronczki M, Kraut N, McConnell DB, Solca F, Neumüller RA. Wilding B, et al. Among authors: engelhardt h. Nat Cancer. 2022 Jul;3(7):821-836. doi: 10.1038/s43018-022-00412-y. Epub 2022 Jul 26. Nat Cancer. 2022. PMID: 35883003
381 results