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Page 1
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: gerstberger t. Nat Cancer. 2022 Jul;3(7):821-836. doi: 10.1038/s43018-022-00412-y. Epub 2022 Jul 26. Nat Cancer. 2022. PMID: 35883003
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: gerstberger t. 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: gerstberger t. 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.
Discovery of Novel Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction.
Gollner A, Rudolph D, Arnhof H, Bauer M, Blake SM, Boehmelt G, Cockroft XL, Dahmann G, Ettmayer P, Gerstberger T, Karolyi-Oezguer J, Kessler D, Kofink C, Ramharter J, Rinnenthal J, Savchenko A, Schnitzer R, Weinstabl H, Weyer-Czernilofsky U, Wunberg T, McConnell DB. Gollner A, et al. Among authors: gerstberger t. J Med Chem. 2016 Nov 23;59(22):10147-10162. doi: 10.1021/acs.jmedchem.6b00900. Epub 2016 Nov 15. J Med Chem. 2016. PMID: 27775892
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: gerstberger t. Cell Rep. 2017 Sep 19;20(12):2860-2875. doi: 10.1016/j.celrep.2017.08.081. Cell Rep. 2017. PMID: 28930682 Free article.
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: gerstberger t. 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.
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: gerstberger t. 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: gerstberger t. Nat Chem Biol. 2019 Aug;15(8):846. doi: 10.1038/s41589-019-0329-z. Nat Chem Biol. 2019. PMID: 31267096
Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.
Böttcher J, Dilworth D, Reiser U, Neumüller RA, Schleicher M, Petronczki M, Zeeb M, Mischerikow N, Allali-Hassani A, Szewczyk MM, Li F, Kennedy S, Vedadi M, Barsyte-Lovejoy D, Brown PJ, Huber KVM, Rogers CM, Wells CI, Fedorov O, Rumpel K, Zoephel A, Mayer M, Wunberg T, Böse D, Zahn S, Arnhof H, Berger H, Reiser C, Hörmann A, Krammer T, Corcokovic M, Sharps B, Winkler S, Häring D, Cockcroft XL, Fuchs JE, Müllauer B, Weiss-Puxbaum A, Gerstberger T, Boehmelt G, Vakoc CR, Arrowsmith CH, Pearson M, McConnell DB. Böttcher J, et al. Among authors: gerstberger t. Nat Chem Biol. 2019 Aug;15(8):822-829. doi: 10.1038/s41589-019-0310-x. Epub 2019 Jul 8. Nat Chem Biol. 2019. PMID: 31285596
23 results