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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: vulpetti a. 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. 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
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.
Hoegenauer K, An S, Axford J, Benander C, Bergsdorf C, Botsch J, Chau S, Fernández C, Gleim S, Hassiepen U, Hunziker J, Joly E, Keller A, Lopez Romero S, Maher R, Mangold AS, Mickanin C, Mihalic M, Neuner P, Patterson AW, Perruccio F, Roggo S, Scesa J, Schröder M, Shkoza D, Thai B, Vulpetti A, Renatus M, Reece-Hoyes JS. Hoegenauer K, et al. Among authors: vulpetti a. ACS Med Chem Lett. 2023 Nov 13;14(12):1631-1639. doi: 10.1021/acsmedchemlett.3c00259. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116426
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. Among authors: vulpetti a. Bioconjug Chem. 2024 Feb 21;35(2):140-146. doi: 10.1021/acs.bioconjchem.3c00535. Epub 2024 Jan 24. Bioconjug Chem. 2024. PMID: 38265691
Discovery of a selective and biologically active low-molecular weight antagonist of human interleukin-1β.
Hommel U, Hurth K, Rondeau JM, Vulpetti A, Ostermeier D, Boettcher A, Brady JP, Hediger M, Lehmann S, Koch E, Blechschmidt A, Yamamoto R, Tundo Dottorello V, Haenni-Holzinger S, Kaiser C, Lehr P, Lingel A, Mureddu L, Schleberger C, Blank J, Ramage P, Freuler F, Eder J, Bornancin F. Hommel U, et al. Among authors: vulpetti a. Nat Commun. 2023 Sep 7;14(1):5497. doi: 10.1038/s41467-023-41190-0. Nat Commun. 2023. PMID: 37679328 Free PMC article.
Small-molecule factor D inhibitors targeting the alternative complement pathway.
Maibaum J, Liao SM, Vulpetti A, Ostermann N, Randl S, Rüdisser S, Lorthiois E, Erbel P, Kinzel B, Kolb FA, Barbieri S, Wagner J, Durand C, Fettis K, Dussauge S, Hughes N, Delgado O, Hommel U, Gould T, Mac Sweeney A, Gerhartz B, Cumin F, Flohr S, Schubart A, Jaffee B, Harrison R, Risitano AM, Eder J, Anderson K. Maibaum J, et al. Among authors: vulpetti a. Nat Chem Biol. 2016 Dec;12(12):1105-1110. doi: 10.1038/nchembio.2208. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775713
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
Pulz R, Angst D, Dawson J, Gessier F, Gutmann S, Hersperger R, Hinniger A, Janser P, Koch G, Revesz L, Vulpetti A, Waelchli R, Zimmerlin A, Cenni B. Pulz R, et al. Among authors: vulpetti a. ACS Med Chem Lett. 2019 Sep 6;10(10):1467-1472. doi: 10.1021/acsmedchemlett.9b00317. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620235 Free PMC article.
69 results