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Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
Rotili D, Tomassi S, Conte M, Benedetti R, Tortorici M, Ciossani G, Valente S, Marrocco B, Labella D, Novellino E, Mattevi A, Altucci L, Tumber A, Yapp C, King ON, Hopkinson RJ, Kawamura A, Schofield CJ, Mai A. Rotili D, et al. Among authors: mattevi a. J Med Chem. 2014 Jan 9;57(1):42-55. doi: 10.1021/jm4012802. Epub 2013 Dec 19. J Med Chem. 2014. PMID: 24325601
A novel mammalian flavin-dependent histone demethylase.
Karytinos A, Forneris F, Profumo A, Ciossani G, Battaglioli E, Binda C, Mattevi A. Karytinos A, et al. Among authors: mattevi a. J Biol Chem. 2009 Jun 26;284(26):17775-82. doi: 10.1074/jbc.M109.003087. Epub 2009 Apr 30. J Biol Chem. 2009. PMID: 19407342 Free PMC article.
Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase.
Tortorici M, Borrello MT, Tardugno M, Chiarelli LR, Pilotto S, Ciossani G, Vellore NA, Bailey SG, Cowan J, O'Connell M, Crabb SJ, Packham G, Mai A, Baron R, Ganesan A, Mattevi A. Tortorici M, et al. Among authors: mattevi a. ACS Chem Biol. 2013 Aug 16;8(8):1677-82. doi: 10.1021/cb4001926. Epub 2013 Jun 11. ACS Chem Biol. 2013. PMID: 23721412
Expanding the druggable space of the LSD1/CoREST epigenetic target: new potential binding regions for drug-like molecules, peptides, protein partners, and chromatin.
Robertson JC, Hurley NC, Tortorici M, Ciossani G, Borrello MT, Vellore NA, Ganesan A, Mattevi A, Baron R. Robertson JC, et al. Among authors: mattevi a. PLoS Comput Biol. 2013;9(7):e1003158. doi: 10.1371/journal.pcbi.1003158. Epub 2013 Jul 18. PLoS Comput Biol. 2013. PMID: 23874194 Free PMC article.
Phosphorylation of neuronal Lysine-Specific Demethylase 1LSD1/KDM1A impairs transcriptional repression by regulating interaction with CoREST and histone deacetylases HDAC1/2.
Toffolo E, Rusconi F, Paganini L, Tortorici M, Pilotto S, Heise C, Verpelli C, Tedeschi G, Maffioli E, Sala C, Mattevi A, Battaglioli E. Toffolo E, et al. Among authors: mattevi a. J Neurochem. 2014 Mar;128(5):603-16. doi: 10.1111/jnc.12457. Epub 2013 Oct 23. J Neurochem. 2014. PMID: 24111946 Free article.
Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.
Vianello P, Botrugno OA, Cappa A, Ciossani G, Dessanti P, Mai A, Mattevi A, Meroni G, Minucci S, Thaler F, Tortorici M, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C. Vianello P, et al. Among authors: mattevi a. Eur J Med Chem. 2014 Oct 30;86:352-63. doi: 10.1016/j.ejmech.2014.08.068. Epub 2014 Aug 27. Eur J Med Chem. 2014. PMID: 25173853
Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.
Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Ruoppolo G, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A. Valente S, et al. Among authors: mattevi a. ACS Med Chem Lett. 2014 Dec 8;6(2):173-7. doi: 10.1021/ml500424z. eCollection 2015 Feb 12. ACS Med Chem Lett. 2014. PMID: 25699146 Free PMC article.
234 results