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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: labella d. J Med Chem. 2014 Jan 9;57(1):42-55. doi: 10.1021/jm4012802. Epub 2013 Dec 19. J Med Chem. 2014. PMID: 24325601
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
Valente S, Liu Y, Schnekenburger M, Zwergel C, Cosconati S, Gros C, Tardugno M, Labella D, Florean C, Minden S, Hashimoto H, Chang Y, Zhang X, Kirsch G, Novellino E, Arimondo PB, Miele E, Ferretti E, Gulino A, Diederich M, Cheng X, Mai A. Valente S, et al. Among authors: labella d. J Med Chem. 2014 Feb 13;57(3):701-13. doi: 10.1021/jm4012627. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24387159 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: labella d. 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
tert-Butylcarbamate-containing histone deacetylase inhibitors: apoptosis induction, cytodifferentiation, and antiproliferative activities in cancer cells.
Valente S, Trisciuoglio D, Tardugno M, Benedetti R, Labella D, Secci D, Mercurio C, Boggio R, Tomassi S, Di Maro S, Novellino E, Altucci L, Del Bufalo D, Mai A, Cosconati S. Valente S, et al. Among authors: labella d. ChemMedChem. 2013 May;8(5):800-11. doi: 10.1002/cmdc.201300005. Epub 2013 Mar 25. ChemMedChem. 2013. PMID: 23526814
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: labella d. 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.
Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity.
Rotili D, Tarantino D, Marrocco B, Gros C, Masson V, Poughon V, Ausseil F, Chang Y, Labella D, Cosconati S, Di Maro S, Novellino E, Schnekenburger M, Grandjenette C, Bouvy C, Diederich M, Cheng X, Arimondo PB, Mai A. Rotili D, et al. Among authors: labella d. PLoS One. 2014 May 8;9(5):e96941. doi: 10.1371/journal.pone.0096941. eCollection 2014. PLoS One. 2014. PMID: 24810902 Free PMC article.
New insights on the mechanism of quinoline-based DNA Methyltransferase inhibitors.
Gros C, Fleury L, Nahoum V, Faux C, Valente S, Labella D, Cantagrel F, Rilova E, Bouhlel MA, David-Cordonnier MH, Dufau I, Ausseil F, Mai A, Mourey L, Lacroix L, Arimondo PB. Gros C, et al. Among authors: labella d. J Biol Chem. 2015 Mar 6;290(10):6293-302. doi: 10.1074/jbc.M114.594671. Epub 2014 Dec 18. J Biol Chem. 2015. PMID: 25525263 Free PMC article.
38 results