Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases(313 views) Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A
Keywords: Anacardic Acid, Antitumor Agents, Epigenetics, Hat, Histone Acetyltransferase Modulators, Antineoplastic Agent, Histone Acetyltransferase Pcaf, Pentadecylidenemalonate, Apoptosis, Article, Controlled Study, Drug Activity, Drug Identification, Drug Inhibition, Drug Mechanism, Human, Human Cell, Acetylation, Alkadienes, Cell Cycle, Enzyme Inhibitors, Models, Chemical, P300-Cbp Transcription Factors, U937 Cells,
Affiliations: *** IBB - CNR ***
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano, SA, Italy
Dipartimento di Studi Farmaceutici, Istituto Pasteur-Fondazione Cenci Bolognetti, Università degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Roma, Italy
Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. De Crecchio 7, 80138 Napoli, Italy
References: Allis, C.D., Berger, S.L., Cote, J., Dent, S., Jenuwein, T., Kouzarides, T., Pillus, L., Zhang, Y., (2007) Cell, 131, p. 633. , A number of scientists have recently proposed to rationalize the nomenclature for all the characterized members of the families of lysine demethylases, acetyltransferases, and lysine methyltransferases. We agree with the reasons supporting this proposal, yet, to avoid confusion, in this paper we preferred to use the current nomenclature. For the new one see
Sakakura, C., Hagiwara, A., Yasuoka, R., Fujita, Y., Nakanishi, M., Masuda, K., Kimura, A., Yamagishi, H., (2000) Int. J. Cancer, 89, p. 217
Aguiar, R.C., Chase, A., Coulthard, S., Macdonald, D.H., Carapeti, M., Reiter, A., Sohal, J., Cross, N.C., (1997) Blood, 90, p. 3130
Panagopoulos, I., Fioretos, T., Isaksson, M., Isaksson, M., Samuelsson, U., Billstrom, R., Strombeck, B., Johansson, B., (2001) Hum. Mol. Genet., 10, p. 395
Muraoka, M., Konishi, M., Kikuchi-Yanoshita, R., Tanaka, K., Shitara, N., Chong, J.M., Iwama, T., Miyaki, M., (1996) Oncogene, 12, p. 1565
Gayther, S.A., Batley, S.J., Linger, L., Bannister, A., Thorpe, K., Chin, S.F., Daigo, Y., Caldas, C., (2000) Nat. Genet., 24, p. 300
Ionov, Y., Matsui, S., Cowell, J.K., (2004) Proc. Natl. Acad. Sci. U.S.A., 101, p. 1273
Lehrmann, H., Pritchard, L.L., Harel-Bellan, A., (2002) Adv. Cancer Res., 86, p. 41
Zheng, Y., Thompson, P.R., Cebrat, M., Wang, L., Devlin, M., Alani, R.M., Cole, P.A., (2004) Methods Enzymol., 376, p. 188
Massa, S., Mai, A., Sbardella, G., Esposito, M., Ragno, R., Loidl, P., Brosch, G., (2001) J. Med. Chem., 44, p. 2069
Bartolini, S., Mai, A., Artico, M., Paesano, N., Rotili, D., Spadafora, C., Sbardella, G., (2005) J. Med. Chem., 48, p. 6776
Sbardella, G., Bartolini, S., Castellano, S., Artico, M., Paesano, N., Rotili, D., Spadafora, C., Mai, A., (2006) ChemMedChem, 1, p. 1073
Ragno, R., Simeoni, S., Castellano, S., Vicidomini, C., Mai, A., Caroli, A., Tramontano, A., Sbardella, G., (2007) J. Med. Chem., 50, p. 1241
Varier, R.A., Swaminathan, V., Balasubramanyam, K., Kundu, T.K., (2004) Biochem. Pharmacol., 68, p. 1215
Dess, D.B., Martin, J.C., (1991) J. Am. Chem. Soc., 113, p. 7277
Allinson, G., Bushby, R.J., Jesudason, M.V., Paillaud, J.-L., Taylor, N., (1997) J. Chem. Soc., Perkin Trans. 2, 2, p. 147
Glozak, M.A., Sengupta, N., Zhang, X., Seto, E., (2005) Gene, 363, p. 15
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs. (c) 2008 Elsevier Ltd. All rights reserved.
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
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Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
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(284 views) Oncotarget (ISSN: 1949-2553electronic, 1949-2553linking), 2018 May 22; 9(39): 25630-25646. Impact Factor:5.008 ViewExport to BibTeXExport to EndNote