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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: furst l. 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.
Structure-activity relationships of GPX4 inhibitor warheads.
Eaton JK, Furst L, Cai LL, Viswanathan VS, Schreiber SL. Eaton JK, et al. Among authors: furst l. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127538. doi: 10.1016/j.bmcl.2020.127538. Epub 2020 Sep 11. Bioorg Med Chem Lett. 2020. PMID: 32920142 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: furst l. 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.
Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments.
Haftchenary S, Nelson SD Jr, Furst L, Dandapani S, Ferrara SJ, Bošković ŽV, Figueroa Lazú S, Guerrero AM, Serrano JC, Crews DK, Brackeen C, Mowat J, Brumby T, Bauser M, Schreiber SL, Phillips AJ. Haftchenary S, et al. Among authors: furst l. ACS Comb Sci. 2016 Sep 12;18(9):569-74. doi: 10.1021/acscombsci.6b00050. Epub 2016 Aug 12. ACS Comb Sci. 2016. PMID: 27518324 Free PMC article.
Reaction design: Nature-inspired total synthesis.
Furst L, Stephenson CR. Furst L, et al. Nat Chem Biol. 2011 Aug 17;7(9):582-3. doi: 10.1038/nchembio.637. Nat Chem Biol. 2011. PMID: 21849998 No abstract available.
33 results