 |
 |
 |
|
Progetti in evidenza
 INCIPIT ISTAPCA Fondo Europeo Pesca Euro-BioImaging Fondazione Veronesi LightDyNAmics INMiND Instruct-IT PRIN eHealthNet Ponrec MFAG Grant MERITCollegamenti
|
 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. Biol., 20, p. 5540 Hubbert, C., Guardiola, A., Shao, R., Kawaguchi, Y., Ito, A., Nixon, A., Yoshida, M., Yao, T.-P., (2002) Nature, 417, p. 455 Glozak, M.A., Sengupta, N., Zhang, X., Seto, E., (2005) Gene, 363, p. 15 Matthias, P., Yoshida, M., Khochbin, S., (2008) Cell Cycle, 7, p. 7 Arif, M., Selvi, B.R., Kundu, T.K., (2010) ChemBioChem, 11, p. 1501 Von Wantoch Rekowski, M., Giannis, A., (2010) Biochim. Biophys. Acta, Gene Regul. Mech., 1799, p. 760 Zhao, S., Xu, W., Jiang, W., Yu, W., Lin, Y., Zhang, T., Yao, J., Guan, K.-L., (2010) Science, 327, p. 1000 Wang, Q., Zhang, Y., Yang, C., Xiong, H., Lin, Y., Yao, J., Li, H., Zhao, G.-P., (2010) Science, 327, p. 1004 Allis, C.D., Berger, S.L., Cote, J., Dent, S., Jenuwien, T., Kouzarides, T., Pillus, L., Zhang, Y., (2007) Cell, 131, p. 633 Lysine acetylation was initially identified in histones, so many KATs and KDACs are often referred to as histone acetyltransferases (HATs) and deacetylases (HDACs), respectivelyDekker, F.J., Haisma, H.J., (2009) Drug Discovery Today, 14, p. 942 Manzo, F., Tambaro, F.P., Mai, A., Altucci, L., (2009) Expert Opin. Ther. Pat., 19, p. 761 Howe, L., Auston, D., Grant, P., John, S., Cook, R.G., Workman, J.L., Pillus, L., (2001) Genes Dev., 15, p. 3144 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 Bandyopadhyay, D., Okan, N.A., Bales, E., Nascimento, L., Cole, P.A., Medrano, E.E., (2002) Cancer Res., 62, p. 6231 Giordano, A., Avantaggiati, M.L., (1999) J. Cell. Physiol., 181, p. 218 Pfister, S., Rea, S., Taipale, M., Mendrzyk, F., Straub, B., Ittrich, C., Thuerigen, O., Lichter, P., (2008) Int. J. Cancer, 122, p. 1207 Katsumoto, T., Yoshida, N., Kitabayashi, I., (2008) Cancer Sci., 99, p. 1523 Iyer, N.G., Xian, J., Chin, S.F., Bannister, A.J., Daigo, Y., Aparicio, S., Kouzarides, T., Caldas, C., (2007) Oncogene, 26, p. 21 Kitabayashi, I., Aikawa, Y., Yokoyama, A., Hosoda, F., Nagai, M., Kakazu, N., Abe, T., Ohki, M., (2001) Leukemia, 15, p. 89 Ait-Si-Ali, S., Polesskaya, A., Filleur, S., Ferreira, R., Duquet, A., Robin, P., Vervish, A., Harel-Bellan, A., (2000) Oncogene, 19, p. 2430 Adcock, I.M., Tsaprouni, L., Bhavsar, P., Ito, K., (2007) Curr. Opin. Immunol., 19, p. 694 Yang, X.J., (2004) Nucleic Acids Res., 32, p. 959 Mantelingu, K., Reddy, B.A.A., Swaminathan, V., Kishore, A.H., Siddappa, N.B., Kumar, G.V.P., Nagashankar, G., Kundu, T.K., (2007) Chem. Biol., 14, p. 645 Barnes, P.J., Adcock, I.M., Ito, K., (2005) Eur. Resp. J., 25, p. 552 Lau, O.D., Kundu, T.K., Soccio, R.E., Ait-Si-Ali, S., Khalil, E.M., Vassilev, A., Wolffe, A.P., Cole, P.A., (2000) Mol. Cell, 5, p. 589 Saha, R.N., Pahan, K., (2005) Cell Death Differ., 13, p. 539 Rouaux, C., Jokic, N., Mbebi, C., Boutillier, S., Loeffler, J.-P., Boutillier, A.-L., (2003) EMBO J., 22, p. 6537 Barrett, R.M., Wood, M.A., (2008) Learn. Memory, 15, p. 460 Maurice, T., Duclot, F., Meunier, J., Naert, G., Givalois, L., Meffre, J., Celerier, A., Gongora, C., (2007) Neuropsychopharmacology, 33, p. 1584 Mai, A., Massa, S., Rotili, D., Cerbara, I., Valente, S., Pezzi, R., Simeoni, S., Ragno, R., (2005) Med. Res. Rev., 25, p. 261 Minucci, S., Pelicci, P.G., (2006) Nat. Rev. Cancer, 6, p. 38 Richon, V.M., Emiliani, S., Verdin, E., Webb, Y., Breslow, R., Rifkind, R.A., Marks, P.A., (1998) Proc. Natl. Acad. Sci. U.S.A., 95, p. 3003 Nakajima, H., Kim, Y.B., Terano, H., Yoshida, M., Horinouchi, S., (1998) Exp. Cell. Res., 241, p. 126 Nagy, Z., Tora, L., (2007) Oncogene, 26, p. 5341 Marmorstein, R., Trievel, R.C., (2009) Biochim. Biophys. Acta, Gene Regul. Mech., 1789, p. 58 Lee, K.K., Workman, J.L., (2007) Nat. Rev. Mol. Cell Biol., 8, p. 284 Hodawadekar, S.C., Marmorstein, R., (2007) Oncogene, 26, p. 5528 Brownell, J.E., Zhou, J., Ranalli, T., Kobayashi, R., Edmondson, D.G., Roth, S.Y., Allis, C.D., (1996) Cell, 84, p. 843 Stockwell, B.R., (2000) Nat. Rev. Genet., 1, p. 116 Bowers, E.M., Yan, G., Mukherjee, C., Orry, A., Wang, L., Holbert, M.A., Crump, N.T., Cole, P.A., (2010) Chem. Biol., 17, p. 471 Cebrat, M., Kim, C.M., Thompson, P.R., Daugherty, M., Cole, P.A., (2003) Bioorg. Med. Chem., 11, p. 3307 Balasubramanyam, K., Swaminathan, V., Ranganathan, A., Kundu, T.K., (2003) J. Biol. Chem., 278, p. 19134 Ravindra, K.C., Selvi, B.R., Arif, M., Reddy, B.A.A., Thanuja, G.R., Agrawal, S., Pradhan, S.K., Kundu, T.K., (2009) J. Biol. Chem., 284, p. 24453 Dal Piaz, F., Tosco, A., Eletto, D., Piccinelli, A.L., Moltedo, O., Franceschelli, S., Sbardella, G., De Tommasi, N., (2010) ChemBioChem, 11, p. 818 Eliseeva, E.D., Valkov, V., Jung, M., Jung, M.O., (2007) Mol. Cancer Ther., 6, p. 2391 Ghizzoni, M., Boltjes, A., Graaf, C.D., Haisma, H.J., Dekker, F.J., (2010) Bioorg. Med. Chem., 18, p. 5826 Souto, J.A., Conte, M., Álvarez, R., Nebbioso, A., Carafa, V., Altucci, L., De Lera, A.R., (2008) ChemMedChem, 3, p. 1435 Costi, R., Di Santo, R., Artico, M., Miele, G., Valentini, P., Novellino, E., Cereseto, A., (2007) J. Med. Chem., 50, p. 1973 Mai, A., Cheng, D., Bedford, M.T., Valente, S., Nebbioso, A., Perrone, A., Brosch, G., Altucci, L., (2008) J. Med. Chem., 51, p. 2279 Dekker, F.J., Ghizzoni, M., Van Der Meer, N., Wisastra, R., Haisma, H.J., (2009) Bioorg. Med. Chem., 17, p. 460 Ghizzoni, M., Haisma, H.J., Dekker, F.J., (2009) Eur. J. Med. Chem., 44, p. 4855 Gorsuch, S., Bavetsias, V., Rowlands, M.G., Aherne, G.W., Workman, P., Jarman, M., McDonald, E., (2009) Bioorg. Med. Chem., 17, p. 467 Stimson, L., Rowlands, M.G., Newbatt, Y.M., Smith, N.F., Raynaud, F.I., Rogers, P., Bavetsias, V., Aherne, G.W., (2005) Mol. Cancer Ther., 4, p. 1521 Biel, M., Kretsovali, A., Karatzali, E., Papamatheakis, J., Giannis, A., (2004) Angew. Chem., Int. Ed., 43, p. 3974 Mai, A., Rotili, D., Tarantino, D., Ornaghi, P., Tosi, F., Vicidomini, C., Sbardella, G., Filetici, P., (2006) J. Med. Chem., 49, p. 6897 Sbardella, G., Castellano, S., Vicidomini, C., Rotili, D., Nebbioso, A., Miceli, M., Altucci, L., Mai, A., (2008) Bioorg. Med. Chem. Lett., 18, p. 2788 Dess, D.B., Martin, J.C., (1991) J. Am. Chem. 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 |
Notizie
 Post Doctoral fellowship w2019 award Fondazione Umberto Veronesi  Innova S@lute 2017Bambini Liberi progetto coordinato dal Cnr, vince il premio Innova S@lute 2017 (161 visite)  Sperimentato su pazienti pediatrici un esoscheletro personalizzato progettato da ricercatori Cnr (485 visite)SmartCity Radio24-Sole 24 Ore Intervista il Dott. Alessandro Soluri sulla Pocket Gamma Camera (272 visite) Accordo cooperazione tra IBB ed il Dipartimento di Ingegneria Biomedica dell’Università di Pechino (567 visite) Archivio Notizie>>> (766 visite) Post Doctoral fellowship w2019 award Fondazione Umberto Veronesi Innova S@lute 2017Bambini Liberi progetto coordinato dal Cnr, vince il premio Innova S@lute 2017 (161 visite) Sperimentato su pazienti pediatrici un esoscheletro personalizzato progettato da ricercatori Cnr (485 visite)SmartCity Radio24-Sole 24 Ore Intervista il Dott. Alessandro Soluri sulla Pocket Gamma Camera (272 visite) Accordo cooperazione tra IBB ed il Dipartimento di Ingegneria Biomedica dell’Università di Pechino (567 visite) Archivio Notizie>>> (766 visite) Post Doctoral fellowship w2019 award Fondazione Umberto Veronesi Innova S@lute 2017Bambini Liberi progetto coordinato dal Cnr, vince il premio Innova S@lute 2017 (161 visite) Sperimentato su pazienti pediatrici un esoscheletro personalizzato progettato da ricercatori Cnr (485 visite)SmartCity Radio24-Sole 24 Ore Intervista il Dott. Alessandro Soluri sulla Pocket Gamma Camera (272 visite) Accordo cooperazione tra IBB ed il Dipartimento di Ingegneria Biomedica dell’Università di Pechino (567 visite) Archivio Notizie>>> (766 visite) Concorsi
Apparecchiature
Eventi
Altre risorse
|
Webmaster and developer: Marco Comerci
Per problemi e suggerimenti: admin
ibb.cnr.it
Ultimo aggiornamento: Friday 15 February 2019, 13:06:47
Per problemi e suggerimenti: admin
ibb.cnr.itUltimo aggiornamento: Friday 15 February 2019, 13:06:47