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Page 1
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
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J. Lorthiois E, et al. Among authors: vulpetti a. J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30. J Med Chem. 2017. PMID: 28621538
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Karki RG, Powers J, Mainolfi N, Anderson K, Belanger DB, Liu D, Ji N, Jendza K, Gelin CF, Mac Sweeney A, Solovay C, Delgado O, Crowley M, Liao SM, Argikar UA, Flohr S, La Bonte LR, Lorthiois EL, Vulpetti A, Brown A, Long D, Prentiss M, Gradoux N, de Erkenez A, Cumin F, Adams C, Jaffee B, Mogi M. Karki RG, et al. Among authors: vulpetti a. J Med Chem. 2019 May 9;62(9):4656-4668. doi: 10.1021/acs.jmedchem.9b00271. Epub 2019 Apr 30. J Med Chem. 2019. PMID: 30995036
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.
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
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.
Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches.
Vulpetti A, Rondeau JM, Bellance MH, Blank J, Boesch R, Boettcher A, Bornancin F, Buhr S, Connor LE, Dumelin CE, Esser O, Hediger M, Hintermann S, Hommel U, Koch E, Lapointe G, Leder L, Lehmann S, Lehr P, Meier P, Muller L, Ostermeier D, Ramage P, Schiebel-Haddad S, Smith AB, Stojanovic A, Velcicky J, Yamamoto R, Hurth K. Vulpetti A, et al. J Med Chem. 2024 May 10. doi: 10.1021/acs.jmedchem.4c00240. Online ahead of print. J Med Chem. 2024. PMID: 38728572
70 results