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659 results

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Page 1
Discovery of a Chemical Probe to Study Implications of BPTF Bromodomain Inhibition in Cellular and in vivo Experiments.
Martinelli P, Schaaf O, Mantoulidis A, Martin LJ, Fuchs JE, Bader G, Gollner A, Wolkerstorfer B, Rogers C, Balıkçı E, Lipp JJ, Mischerikow N, Doebel S, Gerstberger T, Sommergruber W, Huber KVM, Böttcher J. Martinelli P, et al. Among authors: bader g. ChemMedChem. 2023 Mar 14;18(6):e202200686. doi: 10.1002/cmdc.202200686. Epub 2023 Feb 6. ChemMedChem. 2023. PMID: 36649575
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.
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
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo.
Kofink C, Trainor N, Mair B, Wöhrle S, Wurm M, Mischerikow N, Roy MJ, Bader G, Greb P, Garavel G, Diers E, McLennan R, Whitworth C, Vetma V, Rumpel K, Scharnweber M, Fuchs JE, Gerstberger T, Cui Y, Gremel G, Chetta P, Hopf S, Budano N, Rinnenthal J, Gmaschitz G, Mayer M, Koegl M, Ciulli A, Weinstabl H, Farnaby W. Kofink C, et al. Among authors: bader g. Nat Commun. 2022 Oct 10;13(1):5969. doi: 10.1038/s41467-022-33430-6. Nat Commun. 2022. PMID: 36216795 Free PMC 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.
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: bader g. Nat Cancer. 2022 Jul;3(7):821-836. doi: 10.1038/s43018-022-00412-y. Epub 2022 Jul 26. Nat Cancer. 2022. PMID: 35883003
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: bader g. 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
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.
659 results