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Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S.
Lategahn J, Keul M, Klövekorn P, Tumbrink HL, Niggenaber J, Müller MP, Hodson L, Flaßhoff M, Hardick J, Grabe T, Engel J, Schultz-Fademrecht C, Baumann M, Ketzer J, Mühlenberg T, Hiller W, Günther G, Unger A, Müller H, Heimsoeth A, Golz C, Blank-Landeshammer B, Kollipara L, Zahedi RP, Strohmann C, Hengstler JG, van Otterlo WAL, Bauer S, Rauh D. Lategahn J, et al. Among authors: schultz fademrecht c. Chem Sci. 2019 Oct 4;10(46):10789-10801. doi: 10.1039/c9sc03445e. eCollection 2019 Dec 14. Chem Sci. 2019. PMID: 31857889 Free PMC article.
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.
Engel J, Smith S, Lategahn J, Tumbrink HL, Goebel L, Becker C, Hennes E, Keul M, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Hengstler JG, Rauh D. Engel J, et al. Among authors: schultz fademrecht c. J Med Chem. 2017 Sep 28;60(18):7725-7744. doi: 10.1021/acs.jmedchem.7b00515. Epub 2017 Sep 18. J Med Chem. 2017. PMID: 28853575
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.
Lategahn J, Tumbrink HL, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, Russ N, Müller F, Lorenz C, Brägelmann J, Spille I, Grabe T, Müller MP, Heuckmann JM, Klebl BM, Nussbaumer P, Sos ML, Rauh D. Lategahn J, et al. Among authors: schultz fademrecht c. J Med Chem. 2022 May 12;65(9):6643-6655. doi: 10.1021/acs.jmedchem.1c02080. Epub 2022 Apr 29. J Med Chem. 2022. PMID: 35486541
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
Engel J, Richters A, Getlik M, Tomassi S, Keul M, Termathe M, Lategahn J, Becker C, Mayer-Wrangowski S, Grütter C, Uhlenbrock N, Krüll J, Schaumann N, Eppmann S, Kibies P, Hoffgaard F, Heil J, Menninger S, Ortiz-Cuaran S, Heuckmann JM, Tinnefeld V, Zahedi RP, Sos ML, Schultz-Fademrecht C, Thomas RK, Kast SM, Rauh D. Engel J, et al. J Med Chem. 2015 Sep 10;58(17):6844-63. doi: 10.1021/acs.jmedchem.5b01082. Epub 2015 Aug 31. J Med Chem. 2015. PMID: 26275028
Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer.
Weisner J, Landel I, Reintjes C, Uhlenbrock N, Trajkovic-Arsic M, Dienstbier N, Hardick J, Ladigan S, Lindemann M, Smith S, Quambusch L, Scheinpflug R, Depta L, Gontla R, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Maghnouj A, Müller MP, Pohl M, Teschendorf C, Wolters H, Viebahn R, Tannapfel A, Uhl W, Hengstler JG, Hahn SA, Siveke JT, Rauh D. Weisner J, et al. Among authors: schultz fademrecht c. Cancer Res. 2019 May 1;79(9):2367-2378. doi: 10.1158/0008-5472.CAN-18-2861. Epub 2019 Mar 11. Cancer Res. 2019. PMID: 30858154
Cellular model system to dissect the isoform-selectivity of Akt inhibitors.
Quambusch L, Depta L, Landel I, Lubeck M, Kirschner T, Nabert J, Uhlenbrock N, Weisner J, Kostka M, Levy LM, Schultz-Fademrecht C, Glanemann F, Althoff K, Müller MP, Siveke JT, Rauh D. Quambusch L, et al. Among authors: schultz fademrecht c. Nat Commun. 2021 Sep 6;12(1):5297. doi: 10.1038/s41467-021-25512-8. Nat Commun. 2021. PMID: 34489430 Free PMC article.
Potent anti-leukemic activity of a specific cyclin-dependent kinase 9 inhibitor in mouse models of chronic lymphocytic leukemia.
Göthert JR, Imsak R, Möllmann M, Kesper S, Göbel M, Dührsen U, Scholz A, Lücking U, Baumann M, Unger A, Schultz-Fademrecht C, Klebl B, Eickhoff J, Choidas A, Dürig J. Göthert JR, et al. Among authors: schultz fademrecht c. Oncotarget. 2018 May 29;9(41):26353-26369. doi: 10.18632/oncotarget.25293. eCollection 2018 May 29. Oncotarget. 2018. PMID: 29899864 Free PMC article.
35 results