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Page 1
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Eggert E, Hillig RC, Koehr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernandez-Montalvan AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C. Eggert E, et al. Among authors: hillig rc. J Med Chem. 2016 May 26;59(10):4578-600. doi: 10.1021/acs.jmedchem.5b01890. Epub 2016 May 3. J Med Chem. 2016. PMID: 27075367 Free PMC article.
Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo.
Pusch S, Krausert S, Fischer V, Balss J, Ott M, Schrimpf D, Capper D, Sahm F, Eisel J, Beck AC, Jugold M, Eichwald V, Kaulfuss S, Panknin O, Rehwinkel H, Zimmermann K, Hillig RC, Guenther J, Toschi L, Neuhaus R, Haegebart A, Hess-Stumpp H, Bauser M, Wick W, Unterberg A, Herold-Mende C, Platten M, von Deimling A. Pusch S, et al. Among authors: hillig rc. Acta Neuropathol. 2017 Apr;133(4):629-644. doi: 10.1007/s00401-017-1677-y. Epub 2017 Jan 25. Acta Neuropathol. 2017. PMID: 28124097
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, Werbeck ND, Briem H, Boemer U, Weiske J, Badock V, Mastouri J, Petersen K, Siemeister G, Kahmann JD, Wegener D, Böhnke N, Eis K, Graham K, Wortmann L, von Nussbaum F, Bader B. Hillig RC, et al. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. doi: 10.1073/pnas.1812963116. Epub 2019 Jan 25. Proc Natl Acad Sci U S A. 2019. PMID: 30683722 Free PMC article.
Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles.
Eaton JK, Furst L, Ruberto RA, Moosmayer D, Hilpmann A, Ryan MJ, Zimmermann K, Cai LL, Niehues M, Badock V, Kramm A, Chen S, Hillig RC, Clemons PA, Gradl S, Montagnon C, Lazarski KE, Christian S, Bajrami B, Neuhaus R, Eheim AL, Viswanathan VS, Schreiber SL. Eaton JK, et al. Among authors: hillig rc. Nat Chem Biol. 2020 May;16(5):497-506. doi: 10.1038/s41589-020-0501-5. Epub 2020 Mar 30. Nat Chem Biol. 2020. PMID: 32231343 Free PMC article.
Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRASG12C.
Mortier J, Friberg A, Badock V, Moosmayer D, Schroeder J, Steigemann P, Siegel F, Gradl S, Bauser M, Hillig RC, Briem H, Eis K, Bader B, Nguyen D, Christ CD. Mortier J, et al. Among authors: hillig rc. ChemMedChem. 2020 May 19;15(10):827-832. doi: 10.1002/cmdc.201900727. Epub 2020 Apr 1. ChemMedChem. 2020. PMID: 32237114 Free PMC article.
BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe.
Günther J, Hillig RC, Zimmermann K, Kaulfuss S, Lemos C, Nguyen D, Rehwinkel H, Habgood M, Lechner C, Neuhaus R, Ganzer U, Drewes M, Chai J, Bouché L. Günther J, et al. Among authors: hillig rc. J Med Chem. 2022 Nov 10;65(21):14366-14390. doi: 10.1021/acs.jmedchem.2c00441. Epub 2022 Oct 19. J Med Chem. 2022. PMID: 36261130 Free PMC article.
Discovery and Characterization of BAY-184: A New Potent and Selective Acylsulfonamide-Benzofuran In Vivo-Active KAT6AB Inhibitor.
Ter Laak A, Hillig RC, Ferrara SJ, Korr D, Barak N, Lienau P, Herbert S, Fernández-Montalván AE, Neuhaus R, Gorjánácz M, Puetter V, Badock V, Bone W, Strathdee C, Siegel F, Schatz C, Nowak-Reppel K, Doehr O, Gradl S, Hartung IV, Meyerson M, Bouché L. Ter Laak A, et al. Among authors: hillig rc. J Med Chem. 2024 Nov 14;67(21):19282-19303. doi: 10.1021/acs.jmedchem.4c01709. Epub 2024 Oct 25. J Med Chem. 2024. PMID: 39450890 Free PMC article.
37 results