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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: hilpmann a. 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.
Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162.
Moosmayer D, Hilpmann A, Hoffmann J, Schnirch L, Zimmermann K, Badock V, Furst L, Eaton JK, Viswanathan VS, Schreiber SL, Gradl S, Hillig RC. Moosmayer D, et al. Among authors: hilpmann a. Acta Crystallogr D Struct Biol. 2021 Feb 1;77(Pt 2):237-248. doi: 10.1107/S2059798320016125. Epub 2021 Jan 26. Acta Crystallogr D Struct Biol. 2021. PMID: 33559612 Free PMC article.
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. Among authors: hilpmann a. 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.