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DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance.
Schröder M, Renatus M, Liang X, Meili F, Zoller T, Ferrand S, Gauter F, Li X, Sigoillot F, Gleim S, Stachyra TM, Thomas JR, Begue D, Khoshouei M, Lefeuvre P, Andraos-Rey R, Chung B, Ma R, Pinch B, Hofmann A, Schirle M, Schmiedeberg N, Imbach P, Gorses D, Calkins K, Bauer-Probst B, Maschlej M, Niederst M, Maher R, Henault M, Alford J, Ahrne E, Tordella L, Hollingworth G, Thomä NH, Vulpetti A, Radimerski T, Holzer P, Carbonneau S, Thoma CR. Schröder M, et al. Among authors: gorses d. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
Benzimidazolyl-pyrazolo[3,4-b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest.
Lichitsky BV, Komogortsev AN, Dudinov AA, Krayushkin MM, Khodot EN, Samet AV, Silyanova EA, Konyushkin LD, Karpov AS, Gorses D, Radimerski T, Semenova MN, Kiselyov AS, Semenov VV. Lichitsky BV, et al. Among authors: gorses d. ACS Comb Sci. 2019 Dec 9;21(12):805-816. doi: 10.1021/acscombsci.9b00135. Epub 2019 Nov 14. ACS Comb Sci. 2019. PMID: 31689077