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![]() Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs) (107 visite) Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2011 Jun 15; 19(12): 3690-3701. Tipo di articolo: Journal Article, Impact factor: 2.921, Impact factor a 5 anni: 3.157 Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-79958265044&partnerID=40&md5=60b1cedc8aacbaba9aa0db197b88db75 Parole chiave: Epigenetics, Histone Acetyltransferases Modulators, Kat, P300 Cbp, Pcaf Activator, 2 Dodecylmalonic Acid, 2 Tridecylmalonic Acid, 2 Undecylmalonic Acid, 2 Dimethyl 5 Pentadecyl 1, 3 Dioxane 4, 6 Dione, 2 Dimethyl 5 Pentadecylidene 1, Alkan 2 Ylidene Malonic Acid Derivative, Diethyl 2 (1 Aminopentadecylidene)malonic Acid, Diethyl 2 (1 Chloropentadecylidene)malonic Acid, Diethyl 2 (1 Hydroxyheptadecylidene)malonic Acid, Diethyl 2 (1 Hydroxyhexadecylidene)malonic Acid, Diethyl 2 (1 Hydroxypentadecylidene)malonic Acid, Diethyl 2 [(tridecylamino)methylene]malonic Acid Derivative, Diethyl 2 Pentadecylidenemalonic Acid, Diethyl 2 Tetradecylidenemalonic Acid, Diethyl 2 Tridecylmalonic Acid, Enzyme Inhibitor, Functional Group, Long Chain Alkylidenemalonic Acid Derivative, Myristyl Aldehyde, Pentadecanal, Pentadecylmalonic Acid, Tetradecylmalonic Acid, Unclassified Drug, Apoptosis, Article, Biological Activity, Cancer Cell, Cell Cycle, Concentration Response, Controlled Study, Drug Synthesis, Enzyme Activity, Enzyme Induction, Enzyme Inhibition, Enzyme Mechanism, Enzyme Regulation, Histone Acetylation, Human, Human Cell, Leukemia Cell, Protein Expression, Protein Interaction, Protein Modification, Protein Purification, Rigidity, Structure Activity Relation, Alkylation, Blotting, Western, Cell Line, Tumor, Enzyme Activation, Malonates, U937 Cells, Diethyl 2 (1 Aminopentadecylidene) Malonic Acid, Diethyl 2 (1 Chloropentadecylidene) Malonic Acid, Diethyl 2 (1 Hydroxyheptadecylidene) Malonic Acid, Diethyl 2 (1 Hydroxyhexadecylidene) Malonic Acid, Diethyl 2 (1 Hydroxypentadecylidene) Malonic Acid, Diethyl 2 [(tridecylamino) Methylene] Malonic Acid Derivative, Affiliazioni: *** IBB - CNR *** Dipartimento di Scienze Farmaceutiche, Università Degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy Dipartimento di Patologia Generale, Seconda Università Degli Studi di Napoli, Vico L. De Crecchio 7, 80138 Napoli, Italy Dipartimento di Fisica, Università di Napoli Federico II, Napoli, Italy IGB-CNR, Via Pietro Castellino, 80100, Napoli, Italy Dipartimento di Chimica e Tecnologie Del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza Università di Roma, P.le A. Moro 5, 00185 Roma, Italy Riferimenti: Kouzarides, T., (2007) Cell, 128, p. 69 Berger, S.L., (2007) Nature, 447, p. 407 Ruthenburg, A.J., Li, H., Patel, D.J., Allis, C.D., (2007) Nat. Rev. Mol. Cell Biol., 8, p. 983 Strahl, B.D., Allis, C.D., (2000) Nature, 403, p. 41 Allfrey, V.G., Faulkner, R., Mirsky, A.E., (1964) Proc. Natl. Acad. Sci. U.S.A., 51, p. 786 Roth, S.Y., Denu, J.M., Allis, C.D., (2001) Annu. Rev. Biochem., 70, p. 81 Yang, X.-J., Seto, E., (2008) Mol. Cell, 31, p. 449 Liu, Y., Colosimo, A.L., Yang, X.-J., Liao, D., (2000) Mol. Cell. 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Soc., 113, p. 7277 Haldar, J., Kondaiah, P., Bhattacharya, S., (2005) J. Med. Chem., 48, p. 3823 Ahlquist, L., Asselineau, C., Asselineau, J., Stallberg-Stenhagen, S., Stenhagen, E., (1958) Ark. Kemi, 31, p. 543 Comeau, D., Lai, R., Charlot, C., Ucciani, E., (1972) Bull. Soc. Chim. Fr., p. 4163 Actually, as noticeable in Figure 5B, a slight acetylation was observed for both compounds at 15 μM concentration. Yet, it was completely undetectable at 30 μMVarier, R.A., Swaminathan, V., Balasubramanyam, K., Kundu, T.K., (2004) Biochem. Pharmacol., 68, p. 1215 In these conditions, compound 2b caused excessive cell deathTurner, B.M., (2005) Nat. Struct. Mol. Biol., 12, p. 110 Mai, A., Esposito, M., Sbardella, G., Massa, S., (2001) Org. Prep. Proced. Int., 33, p. 391 Chang, Y.-H., Uang, B.-J., Wu, C.-M., Yu, T.-H., (1990) Synthesis, 1990, p. 1033 Sorg, G., Mengel, A., Jung, G., Rademann, J., (2001) Angew. Chem., Int. Ed., 40, p. 4395 Kraus, W.L., Kadonaga, J.T., (1998) Genes Dev., 12, p. 331 Nebbioso, A., Clarke, N., Voltz, E., Germain, E., Ambrosino, C., Bontempo, P., Alvarez, R., Altucci, L., (2005) Nat. Med., 11, p. 77 Cooper, M., (2003) Anal. Bioanal. Chem., 377, p. 834 Johnsson, B., Löfs, S., Lindquist, G., (1991) Anal. Biochem., 198, p. 268 A novel class of KAT modulators (long chain alkylidenemalonates, LoCAMs) has been identified. Variations of the alkyl chain length can change the activity profile from inhibition of both KAT3A/KAT2B (as derivative 2a) to the peculiar profile of pentadecylidenemalonate 1b, the first activator/inhibitor of histone acetyltransferases. Together with the powerful apoptotic effect (particularly notable if considering that anacardic acid and other KAT inhibitors are not cell permeable) appoint them as valuable biological tools to understand the mechanisms of lysine acetyltransferases. (C) 2011 Elsevier Ltd. All rights reserved.
Petraglia F, Singh AA, Carafa V, Nebbioso A, Conte M, Scisciola L, Valente S, Baldi A, Mandoli A, Petrizzi VB, Ingenito C, De Falco S, Cicatiello V, Apicella I, Janssen-megens EM, Kim B, Yi G, Logie C, Heath S, Ruvo M, Wierenga ATJ, Flicek P, Yaspo ML, Della Valle V, Bernard O, Tomassi S, Novellino E, Feoli A, Sbardella G, Gut I, Vellenga E, Stunnenberg HG, Mai A, Martens JHA, Altucci L * Combined HAT/EZH2 modulation leads to cancer-selective cell death (47 visite) Oncotarget (ISSN: 1949-2553electronic, 1949-2553linking), 2018 May 22; 9(39): 25630-25646. Impact Factor: 5.008 Dettagli Esporta in BibTeX Esporta in EndNote Garzia L, Andolfo I, Cusanelli E, Marino N, Petrosino G, De Martino D, Esposito V, Galeone A, Navas L, Esposito S, Gargiulo S, Fattet S, Donofrio V, Cinalli G, Brunetti A, Del Vecchio L, Northcott PA, Delattre O, Taylor MD, Iolascon A, Zollo M * MicroRNA-199b-5p Impairs Cancer Stem Cells through Negative Regulation of HES1 in Medulloblastoma (149 visite) Plosone (ISSN: 1932-6203, 1932-6203electronic), 2009 Mar 24; 4(3): e4998-e4998. Impact Factor: 4.351 Dettagli Esporta in BibTeX Esporta in EndNote Chiechio S, Zammataro M, Morales ME, Busceti CL, Drago F, Th Gereau RW, Copani A, Nicoletti F * Epigenetic modulation of mGlu2 receptors by histone deacetylase inhibitors in the treatment of inflammatory pain (109 visite) Mol Pharmacol (ISSN: 0026-895x), 2009; 75(5): 1014-1020. Impact Factor: 4.531 Dettagli Esporta in BibTeX Esporta in EndNote Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A * Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases (87 visite) Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 May 1; 18(9): 2788-2792. Impact Factor: 2.531 Dettagli Esporta in BibTeX Esporta in EndNote 4 Records (3 escludendo Abstract e Conferenze). Impact factor totale: 16.421 (12.07 escludendo Abstract e Conferenze). Impact factor a 5 anni totale: 16.901 (12.518 escludendo Abstract e Conferenze). Esporta in BibTeX Esporta in EndNote Ultima modifica di Massimiliano Sorbillo in data Thursday 12 March 2015, 8:11:32 107 visite. Ultima visita in data Monday 31 December 2018, 16:29:03 |
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