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Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors.
Kalin JH, Wu M, Gomez AV, Song Y, Das J, Hayward D, Adejola N, Wu M, Panova I, Chung HJ, Kim E, Roberts HJ, Roberts JM, Prusevich P, Jeliazkov JR, Roy Burman SS, Fairall L, Milano C, Eroglu A, Proby CM, Dinkova-Kostova AT, Hancock WW, Gray JJ, Bradner JE, Valente S, Mai A, Anders NM, Rudek MA, Hu Y, Ryu B, Schwabe JWR, Mattevi A, Alani RM, Cole PA. Kalin JH, et al. Among authors: mattevi a. Nat Commun. 2018 Jan 4;9(1):53. doi: 10.1038/s41467-017-02242-4. Nat Commun. 2018. PMID: 29302039 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
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.
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
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.
Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.
Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Monaldi D, Ruoppolo G, Tilset M, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A. Valente S, et al. Among authors: mattevi a. Eur J Med Chem. 2015 Apr 13;94:163-74. doi: 10.1016/j.ejmech.2015.02.060. Epub 2015 Mar 3. Eur J Med Chem. 2015. PMID: 25768700
233 results