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Page 1
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: fuchs je. 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.
Targeted Synthesis of Complex Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors.
Gollner A, Weinstabl H, Fuchs JE, Rudolph D, Garavel G, Hofbauer KS, Karolyi-Oezguer J, Gmaschitz G, Hela W, Kerres N, Grondal E, Werni P, Ramharter J, Broeker J, McConnell DB. Gollner A, et al. Among authors: fuchs je. ChemMedChem. 2019 Jan 8;14(1):88-93. doi: 10.1002/cmdc.201800617. Epub 2018 Dec 11. ChemMedChem. 2019. PMID: 30458062 Free PMC article.
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: fuchs je. 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
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: fuchs je. 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.
Getting a Grip on the Undrugged: Targeting β-Catenin with Fragment-Based Methods.
Kessler D, Mayer M, Zahn SK, Zeeb M, Wöhrle S, Bergner A, Bruchhaus J, Ciftci T, Dahmann G, Dettling M, Döbel S, Fuchs JE, Geist L, Hela W, Kofink C, Kousek R, Moser F, Puchner T, Rumpel K, Scharnweber M, Werni P, Wolkerstorfer B, Breitsprecher D, Baaske P, Pearson M, McConnell DB, Böttcher J. Kessler D, et al. Among authors: fuchs je. ChemMedChem. 2021 May 6;16(9):1420-1424. doi: 10.1002/cmdc.202000839. Epub 2021 Jan 14. ChemMedChem. 2021. PMID: 33275320 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: fuchs je. Nat Cancer. 2022 Jul;3(7):821-836. doi: 10.1038/s43018-022-00412-y. Epub 2022 Jul 26. Nat Cancer. 2022. PMID: 35883003
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: fuchs je. Nat Commun. 2022 Oct 10;13(1):5969. doi: 10.1038/s41467-022-33430-6. Nat Commun. 2022. PMID: 36216795 Free PMC article.
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: fuchs je. ChemMedChem. 2023 Mar 14;18(6):e202200686. doi: 10.1002/cmdc.202200686. Epub 2023 Feb 6. ChemMedChem. 2023. PMID: 36649575
102 results