Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs) (225 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
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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
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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
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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.
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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
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