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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.
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.
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.
Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions.
Popow J, Arnhof H, Bader G, Berger H, Ciulli A, Covini D, Dank C, Gmaschitz T, Greb P, Karolyi-Özguer J, Koegl M, McConnell DB, Pearson M, Rieger M, Rinnenthal J, Roessler V, Schrenk A, Spina M, Steurer S, Trainor N, Traxler E, Wieshofer C, Zoephel A, Ettmayer P. Popow J, et al. Among authors: bader g. J Med Chem. 2019 Mar 14;62(5):2508-2520. doi: 10.1021/acs.jmedchem.8b01826. Epub 2019 Feb 22. J Med Chem. 2019. PMID: 30739444
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.
Publisher Correction: 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 Aug;15(8):846. doi: 10.1038/s41589-019-0329-z. Nat Chem Biol. 2019. PMID: 31267096
Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis.
Weinstabl H, Treu M, Rinnenthal J, Zahn SK, Ettmayer P, Bader G, Dahmann G, Kessler D, Rumpel K, Mischerikow N, Savarese F, Gerstberger T, Mayer M, Zoephel A, Schnitzer R, Sommergruber W, Martinelli P, Arnhof H, Peric-Simov B, Hofbauer KS, Garavel G, Scherbantin Y, Mitzner S, Fett TN, Scholz G, Bruchhaus J, Burkard M, Kousek R, Ciftci T, Sharps B, Schrenk A, Harrer C, Haering D, Wolkerstorfer B, Zhang X, Lv X, Du A, Li D, Li Y, Quant J, Pearson M, McConnell DB. Weinstabl H, et al. Among authors: bader g. J Med Chem. 2019 Sep 12;62(17):7976-7997. doi: 10.1021/acs.jmedchem.9b00718. Epub 2019 Aug 14. J Med Chem. 2019. PMID: 31365252
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: bader g. 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.
PI by NMR: Probing CH-π Interactions in Protein-Ligand Complexes by NMR Spectroscopy.
Platzer G, Mayer M, Beier A, Brüschweiler S, Fuchs JE, Engelhardt H, Geist L, Bader G, Schörghuber J, Lichtenecker R, Wolkerstorfer B, Kessler D, McConnell DB, Konrat R. Platzer G, et al. Among authors: bader g. Angew Chem Int Ed Engl. 2020 Aug 24;59(35):14861-14868. doi: 10.1002/anie.202003732. Epub 2020 Jul 15. Angew Chem Int Ed Engl. 2020. PMID: 32421895 Free PMC article.
659 results