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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: schmiedeberg n. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field.
Vulpetti A, Holzer P, Schmiedeberg N, Imbach-Weese P, Pissot-Soldermann C, Hollingworth GJ, Radimerski T, Thoma CR, Stachyra TM, Wojtynek M, Maschlej M, Chau S, Schuffenhauer A, Fernández C, Schröder M, Renatus M. Vulpetti A, et al. Among authors: schmiedeberg n. ACS Med Chem Lett. 2023 Jun 2;14(7):949-954. doi: 10.1021/acsmedchemlett.3c00104. eCollection 2023 Jul 13. ACS Med Chem Lett. 2023. PMID: 37465299
Drug-induced eRF1 degradation promotes readthrough and reveals a new branch of ribosome quality control.
Gurzeler LA, Link M, Ibig Y, Schmidt I, Galuba O, Schoenbett J, Gasser-Didierlaurant C, Parker CN, Mao X, Bitsch F, Schirle M, Couttet P, Sigoillot F, Ziegelmüller J, Uldry AC, Teodorowicz W, Schmiedeberg N, Mühlemann O, Reinhardt J. Gurzeler LA, et al. Among authors: schmiedeberg n. Cell Rep. 2023 Sep 26;42(9):113056. doi: 10.1016/j.celrep.2023.113056. Epub 2023 Aug 30. Cell Rep. 2023. PMID: 37651229 Free article.
Drug-induced eRF1 degradation promotes readthrough and reveals a new branch of ribosome quality control.
Gurzeler LA, Link M, Ibig Y, Schmidt I, Galuba O, Schoenbett J, Gasser-Didierlaurant C, Parker CN, Mao X, Bitsch F, Schirle M, Couttet P, Sigoillot F, Ziegelmüller J, Uldry AC, Teodorowicz W, Schmiedeberg N, Mühlemann O, Reinhardt J. Gurzeler LA, et al. Among authors: schmiedeberg n. Cell Rep. 2023 Sep 26;42(9):113159. doi: 10.1016/j.celrep.2023.113159. Epub 2023 Sep 13. Cell Rep. 2023. PMID: 37708027 Free article. No abstract available.
The Crystal Structure of Cancer Osaka Thyroid Kinase Reveals an Unexpected Kinase Domain Fold.
Gutmann S, Hinniger A, Fendrich G, Drückes P, Antz S, Mattes H, Möbitz H, Ofner S, Schmiedeberg N, Stojanovic A, Rieffel S, Strauss A, Troxler T, Glatthar R, Sparrer H. Gutmann S, et al. Among authors: schmiedeberg n. J Biol Chem. 2015 Jun 12;290(24):15210-8. doi: 10.1074/jbc.M115.648097. Epub 2015 Apr 27. J Biol Chem. 2015. PMID: 25918157 Free PMC article.
G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonists reduce the production of proinflammatory cytokines and stabilize the alternative macrophage phenotype.
Högenauer K, Arista L, Schmiedeberg N, Werner G, Jaksche H, Bouhelal R, Nguyen DG, Bhat BG, Raad L, Rauld C, Carballido JM. Högenauer K, et al. Among authors: schmiedeberg n. J Med Chem. 2014 Dec 26;57(24):10343-54. doi: 10.1021/jm501052c. Epub 2014 Dec 9. J Med Chem. 2014. PMID: 25411721
13 results