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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design.
Farnaby W, Koegl M, Roy MJ, Whitworth C, Diers E, Trainor N, Zollman D, Steurer S, Karolyi-Oezguer J, Riedmueller C, Gmaschitz T, Wachter J, Dank C, Galant M, Sharps B, Rumpel K, Traxler E, Gerstberger T, Schnitzer R, Petermann O, Greb P, Weinstabl H, Bader G, Zoephel A, Weiss-Puxbaum A, Ehrenhöfer-Wölfer K, Wöhrle S, Boehmelt G, Rinnenthal J, Arnhof H, Wiechens N, Wu MY, Owen-Hughes T, Ettmayer P, Pearson M, McConnell DB, Ciulli A. Farnaby W, et al. Among authors: bader g. Nat Chem Biol. 2019 Jul;15(7):672-680. doi: 10.1038/s41589-019-0294-6. Epub 2019 Jun 10. Nat Chem Biol. 2019. PMID: 31178587 Free PMC article.
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: bader g. 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.
A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation.
Waizenegger IC, Baum A, Steurer S, Stadtmüller H, Bader G, Schaaf O, Garin-Chesa P, Schlattl A, Schweifer N, Haslinger C, Colbatzky F, Mousa S, Kalkuhl A, Kraut N, Adolf GR. Waizenegger IC, et al. Among authors: bader g. Mol Cancer Ther. 2016 Mar;15(3):354-65. doi: 10.1158/1535-7163.MCT-15-0617. Epub 2016 Feb 25. Mol Cancer Ther. 2016. PMID: 26916115
Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition.
Hohmann AF, Martin LJ, Minder JL, Roe JS, Shi J, Steurer S, Bader G, McConnell D, Pearson M, Gerstberger T, Gottschamel T, Thompson D, Suzuki Y, Koegl M, Vakoc CR. Hohmann AF, et al. Among authors: bader g. Nat Chem Biol. 2016 Sep;12(9):672-9. doi: 10.1038/nchembio.2115. Epub 2016 Jul 4. Nat Chem Biol. 2016. PMID: 27376689 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: bader g. 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
Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6.
Kerres N, Steurer S, Schlager S, Bader G, Berger H, Caligiuri M, Dank C, Engen JR, Ettmayer P, Fischerauer B, Flotzinger G, Gerlach D, Gerstberger T, Gmaschitz T, Greb P, Han B, Heyes E, Iacob RE, Kessler D, Kölle H, Lamarre L, Lancia DR, Lucas S, Mayer M, Mayr K, Mischerikow N, Mück K, Peinsipp C, Petermann O, Reiser U, Rudolph D, Rumpel K, Salomon C, Scharn D, Schnitzer R, Schrenk A, Schweifer N, Thompson D, Traxler E, Varecka R, Voss T, Weiss-Puxbaum A, Winkler S, Zheng X, Zoephel A, Kraut N, McConnell D, Pearson M, Koegl M. Kerres N, et al. Among authors: bader g. Cell Rep. 2017 Sep 19;20(12):2860-2875. doi: 10.1016/j.celrep.2017.08.081. Cell Rep. 2017. PMID: 28930682 Free article.
Expansion of DUB functionality generated by alternative isoforms - USP35, a case study.
Leznicki P, Natarajan J, Bader G, Spevak W, Schlattl A, Abdul Rehman SA, Pathak D, Weidlich S, Zoephel A, Bordone MC, Barbosa-Morais NL, Boehmelt G, Kulathu Y. Leznicki P, et al. Among authors: bader g. J Cell Sci. 2018 May 16;131(10):jcs212753. doi: 10.1242/jcs.212753. J Cell Sci. 2018. PMID: 29685892 Free PMC article.
RIOK1 kinase activity is required for cell survival irrespective of MTAP status.
Hörmann A, Hopfgartner B, Köcher T, Corcokovic M, Krammer T, Reiser C, Bader G, Shi J, Ehrenhöfer K, Wöhrle S, Schweifer N, Vakoc CR, Kraut N, Pearson M, Petronczki M, Neumüller RA. Hörmann A, et al. Among authors: bader g. Oncotarget. 2018 Jun 19;9(47):28625-28637. doi: 10.18632/oncotarget.25586. eCollection 2018 Jun 19. Oncotarget. 2018. PMID: 29983885 Free PMC article.
658 results