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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: schirle m. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
Enhancing the Small-Scale Screenable Biological Space beyond Known Chemogenomics Libraries with Gray Chemical Matter─Compounds with Novel Mechanisms from High-Throughput Screening Profiles.
Thomas JR, Shelton C 4th, Murphy J, Brittain S, Bray MA, Aspesi P, Concannon J, King FJ, Ihry RJ, Ho DJ, Henault M, Hadjikyriacou A, Neri M, Sigoillot FD, Pham HT, Shum M, Barys L, Jones MD, Martin EJ, Blechschmidt A, Rieffel S, Troxler TJ, Mapa FA, Jenkins JL, Jain RK, Kutchukian PS, Schirle M, Renner S. Thomas JR, et al. Among authors: schirle m. ACS Chem Biol. 2024 Apr 19;19(4):938-952. doi: 10.1021/acschembio.3c00737. Epub 2024 Apr 2. ACS Chem Biol. 2024. PMID: 38565185 Free PMC article.
Activation of human STING by a molecular glue-like compound.
Li J, Canham SM, Wu H, Henault M, Chen L, Liu G, Chen Y, Yu G, Miller HR, Hornak V, Brittain SM, Michaud GA, Tutter A, Broom W, Digan ME, McWhirter SM, Sivick KE, Pham HT, Chen CH, Tria GS, McKenna JM, Schirle M, Mao X, Nicholson TB, Wang Y, Jenkins JL, Jain RK, Tallarico JA, Patel SJ, Zheng L, Ross NT, Cho CY, Zhang X, Bai XC, Feng Y. Li J, et al. Among authors: schirle m. Nat Chem Biol. 2024 Mar;20(3):365-372. doi: 10.1038/s41589-023-01434-y. Epub 2023 Oct 12. Nat Chem Biol. 2024. PMID: 37828400 Free PMC 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: schirle m. 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.
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: schirle m. 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.
Correction to "Rational Chemical Design of Molecular Glue Degraders".
Toriki ES, Papatzimas JW, Nishikawa K, Dovala D, Frank AO, Hesse MJ, Dankova D, Song JG, Bruce-Smythe M, Struble H, Garcia FJ, Brittain SM, Kile AC, McGregor LM, McKenna JM, Tallarico JA, Schirle M, Nomura DK. Toriki ES, et al. Among authors: schirle m. ACS Cent Sci. 2023 Jul 21;9(8):1702. doi: 10.1021/acscentsci.3c00844. eCollection 2023 Aug 23. ACS Cent Sci. 2023. PMID: 37637749 Free PMC article.
Rational Chemical Design of Molecular Glue Degraders.
Toriki ES, Papatzimas JW, Nishikawa K, Dovala D, Frank AO, Hesse MJ, Dankova D, Song JG, Bruce-Smythe M, Struble H, Garcia FJ, Brittain SM, Kile AC, McGregor LM, McKenna JM, Tallarico JA, Schirle M, Nomura DK. Toriki ES, et al. Among authors: schirle m. ACS Cent Sci. 2023 Apr 11;9(5):915-926. doi: 10.1021/acscentsci.2c01317. eCollection 2023 May 24. ACS Cent Sci. 2023. PMID: 37252349 Free PMC article.
89 results