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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: hofmann mh. 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: hofmann mh. 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
BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.
Sanderson MP, Apgar J, Garin-Chesa P, Hofmann MH, Kessler D, Quant J, Savchenko A, Schaaf O, Treu M, Tye H, Zahn SK, Zoephel A, Haaksma E, Adolf GR, Kraut N. Sanderson MP, et al. Among authors: hofmann mh. Mol Cancer Ther. 2015 Dec;14(12):2762-72. doi: 10.1158/1535-7163.MCT-15-0539. Epub 2015 Oct 5. Mol Cancer Ther. 2015. PMID: 26438154
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, Rogers C, Rumpel K, Schaaf O, Steurer S, Tallant C, Vakoc CR, Zeeb M, Zoephel A, Pearson M, Boehmelt G, McConnell D. Martin LJ, et al. Among authors: hofmann mh. J Med Chem. 2016 May 26;59(10):4462-75. doi: 10.1021/acs.jmedchem.5b01865. Epub 2016 Mar 10. J Med Chem. 2016. PMID: 26914985 Free PMC article.
The IGF1R/INSR Inhibitor BI 885578 Selectively Inhibits Growth of IGF2-Overexpressing Colorectal Cancer Tumors and Potentiates the Efficacy of Anti-VEGF Therapy.
Sanderson MP, Hofmann MH, Garin-Chesa P, Schweifer N, Wernitznig A, Fischer S, Jeschko A, Meyer R, Moll J, Pecina T, Arnhof H, Weyer-Czernilofsky U, Zahn SK, Adolf GR, Kraut N. Sanderson MP, et al. Among authors: hofmann mh. Mol Cancer Ther. 2017 Oct;16(10):2223-2233. doi: 10.1158/1535-7163.MCT-17-0336. Epub 2017 Jul 20. Mol Cancer Ther. 2017. PMID: 28729397
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. 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.
Antitumor Activity of the IGF-1/IGF-2-Neutralizing Antibody Xentuzumab (BI 836845) in Combination with Enzalutamide in Prostate Cancer Models.
Weyer-Czernilofsky U, Hofmann MH, Friedbichler K, Baumgartinger R, Adam PJ, Solca F, Kraut N, Nguyen HM, Corey E, Liu G, Sprenger CC, Plymate SR, Bogenrieder T. Weyer-Czernilofsky U, et al. Among authors: hofmann mh. Mol Cancer Ther. 2020 Apr;19(4):1059-1069. doi: 10.1158/1535-7163.MCT-19-0378. Epub 2020 Feb 13. Mol Cancer Ther. 2020. PMID: 32054790 Free PMC article.
BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition.
Hofmann MH, Gmachl M, Ramharter J, Savarese F, Gerlach D, Marszalek JR, Sanderson MP, Kessler D, Trapani F, Arnhof H, Rumpel K, Botesteanu DA, Ettmayer P, Gerstberger T, Kofink C, Wunberg T, Zoephel A, Fu SC, Teh JL, Böttcher J, Pototschnig N, Schachinger F, Schipany K, Lieb S, Vellano CP, O'Connell JC, Mendes RL, Moll J, Petronczki M, Heffernan TP, Pearson M, McConnell DB, Kraut N. Hofmann MH, et al. Cancer Discov. 2021 Jan;11(1):142-157. doi: 10.1158/2159-8290.CD-20-0142. Epub 2020 Aug 19. Cancer Discov. 2021. PMID: 32816843 Free PMC article.
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.
Ramharter J, Kessler D, Ettmayer P, Hofmann MH, Gerstberger T, Gmachl M, Wunberg T, Kofink C, Sanderson M, Arnhof H, Bader G, Rumpel K, Zöphel A, Schnitzer R, Böttcher J, O'Connell JC, Mendes RL, Richard D, Pototschnig N, Weiner I, Hela W, Hauer K, Haering D, Lamarre L, Wolkerstorfer B, Salamon C, Werni P, Munico-Martinez S, Meyer R, Kennedy MD, Kraut N, McConnell DB. Ramharter J, et al. Among authors: hofmann mh. J Med Chem. 2021 May 27;64(10):6569-6580. doi: 10.1021/acs.jmedchem.0c01949. Epub 2021 Mar 15. J Med Chem. 2021. PMID: 33719426
71 results