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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: thoma nh. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
Crystal structure of the human COP9 signalosome.
Lingaraju GM, Bunker RD, Cavadini S, Hess D, Hassiepen U, Renatus M, Fischer ES, Thomä NH. Lingaraju GM, et al. Among authors: thoma nh. Nature. 2014 Aug 14;512(7513):161-5. doi: 10.1038/nature13566. Epub 2014 Jul 16. Nature. 2014. PMID: 25043011
Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide.
Fischer ES, Böhm K, Lydeard JR, Yang H, Stadler MB, Cavadini S, Nagel J, Serluca F, Acker V, Lingaraju GM, Tichkule RB, Schebesta M, Forrester WC, Schirle M, Hassiepen U, Ottl J, Hild M, Beckwith RE, Harper JW, Jenkins JL, Thomä NH. Fischer ES, et al. Among authors: thoma nh. Nature. 2014 Aug 7;512(7512):49-53. doi: 10.1038/nature13527. Epub 2014 Jul 16. Nature. 2014. PMID: 25043012 Free PMC article.
The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.
Słabicki M, Kozicka Z, Petzold G, Li YD, Manojkumar M, Bunker RD, Donovan KA, Sievers QL, Koeppel J, Suchyta D, Sperling AS, Fink EC, Gasser JA, Wang LR, Corsello SM, Sellar RS, Jan M, Gillingham D, Scholl C, Fröhling S, Golub TR, Fischer ES, Thomä NH, Ebert BL. Słabicki M, et al. Among authors: thoma nh. Nature. 2020 Sep;585(7824):293-297. doi: 10.1038/s41586-020-2374-x. Epub 2020 Jun 3. Nature. 2020. PMID: 32494016 Free PMC article.
Cullin-RING ubiquitin E3 ligase regulation by the COP9 signalosome.
Cavadini S, Fischer ES, Bunker RD, Potenza A, Lingaraju GM, Goldie KN, Mohamed WI, Faty M, Petzold G, Beckwith RE, Tichkule RB, Hassiepen U, Abdulrahman W, Pantelic RS, Matsumoto S, Sugasawa K, Stahlberg H, Thomä NH. Cavadini S, et al. Among authors: thoma nh. Nature. 2016 Mar 31;531(7596):598-603. doi: 10.1038/nature17416. Nature. 2016. PMID: 27029275
Structural mechanism of cGAS inhibition by the nucleosome.
Pathare GR, Decout A, Glück S, Cavadini S, Makasheva K, Hovius R, Kempf G, Weiss J, Kozicka Z, Guey B, Melenec P, Fierz B, Thomä NH, Ablasser A. Pathare GR, et al. Among authors: thoma nh. Nature. 2020 Nov;587(7835):668-672. doi: 10.1038/s41586-020-2750-6. Epub 2020 Sep 10. Nature. 2020. PMID: 32911482
Cooperation between bHLH transcription factors and histones for DNA access.
Michael AK, Stoos L, Crosby P, Eggers N, Nie XY, Makasheva K, Minnich M, Healy KL, Weiss J, Kempf G, Cavadini S, Kater L, Seebacher J, Vecchia L, Chakraborty D, Isbel L, Grand RS, Andersch F, Fribourgh JL, Schübeler D, Zuber J, Liu AC, Becker PB, Fierz B, Partch CL, Menet JS, Thomä NH. Michael AK, et al. Among authors: thoma nh. Nature. 2023 Jul;619(7969):385-393. doi: 10.1038/s41586-023-06282-3. Epub 2023 Jul 5. Nature. 2023. PMID: 37407816 Free PMC article.
BANP opens chromatin and activates CpG-island-regulated genes.
Grand RS, Burger L, Gräwe C, Michael AK, Isbel L, Hess D, Hoerner L, Iesmantavicius V, Durdu S, Pregnolato M, Krebs AR, Smallwood SA, Thomä N, Vermeulen M, Schübeler D. Grand RS, et al. Nature. 2021 Aug;596(7870):133-137. doi: 10.1038/s41586-021-03689-8. Epub 2021 Jul 7. Nature. 2021. PMID: 34234345
75 results