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23 results

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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 cr. 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: thoma cr. 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
Design, Synthesis, and In Vitro and In Vivo Evaluation of Cereblon Binding Bruton's Tyrosine Kinase (BTK) Degrader CD79b Targeted Antibody-Drug Conjugates.
Zhang A, Seiss K, Laborde L, Palacio-Ramirez S, Guthy D, Lanter M, Lorber J, Vulpetti A, Arista L, Zoller T, Radimerski T, Thoma C, Hebach C, Tschantz WR, Karpov A, Hollingworth GJ, D'Alessio JA, Ferretti S, Burger MT. Zhang A, et al. Bioconjug Chem. 2024 Feb 21;35(2):140-146. doi: 10.1021/acs.bioconjchem.3c00535. Epub 2024 Jan 24. Bioconjug Chem. 2024. PMID: 38265691
BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma.
Weisberg E, Chowdhury B, Meng C, Case AE, Ni W, Garg S, Sattler M, Azab AK, Sun J, Muz B, Sanchez D, Toure A, Stone RM, Galinsky I, Winer E, Gleim S, Gkountela S, Kedves A, Harrington E, Abrams T, Zoller T, Vaupel A, Manley P, Faller M, Chung B, Chen X, Busenhart P, Stephan C, Calkins K, Bonenfant D, Thoma CR, Forrester W, Griffin JD. Weisberg E, et al. Among authors: thoma cr. Blood Cancer J. 2022 Jul 19;12(7):110. doi: 10.1038/s41408-022-00704-7. Blood Cancer J. 2022. PMID: 35853853 Free PMC article.
Structure of the MRAS-SHOC2-PP1C phosphatase complex.
Hauseman ZJ, Fodor M, Dhembi A, Viscomi J, Egli D, Bleu M, Katz S, Park E, Jang DM, Porter KA, Meili F, Guo H, Kerr G, Mollé S, Velez-Vega C, Beyer KS, Galli GG, Maira SM, Stams T, Clark K, Eck MJ, Tordella L, Thoma CR, King DA. Hauseman ZJ, et al. Among authors: thoma cr. Nature. 2022 Sep;609(7926):416-423. doi: 10.1038/s41586-022-05086-1. Epub 2022 Jul 13. Nature. 2022. PMID: 35830882 Free PMC article.
A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes.
Pinch BJ, Buckley DL, Gleim S, Brittain SM, Tandeske L, D'Alessandro PL, Hauseman ZJ, Lipps J, Xu L, Harvey EP, Schirle M, Sprague ER, Forrester WC, Dovala D, McGregor LM, Thoma CR. Pinch BJ, et al. Among authors: thoma cr. Cell Chem Biol. 2022 Jan 20;29(1):57-66.e6. doi: 10.1016/j.chembiol.2021.08.007. Epub 2021 Sep 8. Cell Chem Biol. 2022. PMID: 34499862 Free article.
Tumor suppressor NF2/Merlin is a microtubule stabilizer.
Smole Z, Thoma CR, Applegate KT, Duda M, Gutbrodt KL, Danuser G, Krek W. Smole Z, et al. Among authors: thoma cr. Cancer Res. 2014 Jan 1;74(1):353-62. doi: 10.1158/0008-5472.CAN-13-1334. Epub 2013 Nov 26. Cancer Res. 2014. PMID: 24282279 Free PMC article.
23 results