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Cormier-Daire V, Bainbridge MN, Yang XJ, Gingras MC, Gibbs RA, Rosenblatt DS,
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cause Genitopatellar syndrome. Am J Hum Genet 90:282–289. https://doi.org/10.1016/j.
ajhg.2011.11.023
69. Wang Y, Miao X, Liu Y, Li F, Liu Q, Sun J, Cai L (2014) Dysregulation of histone
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70. Yanazume T, Hasegawa K, Morimoto T, Kawamura T, Wada H, Matsumori A, Kawase Y,
Hirai M, Kita T (2003) Cardiac p300 is involved in myocyte growth with decompensated heart
failure. Mol Cell Biol 23:3593–3606
71. Iyer A, Fairlie DP, Brown L (2012) Lysine acetylation in obesity, diabetes and metabolic
disease. Immunol Cell Biol 90:39–46. https://doi.org/10.1038/icb.2011.99
72. Lau OD, Kundu TK, Soccio RE, Ait-Si-Ali S, Khalil EM, Vassilev A, Wolffe AP, Nakatani Y,
Roeder RG, Cole PA (2000) HATs off: selective synthetic inhibitors of the histone
acetyltransferases p300 and PCAF. Mol Cell 5:589–595
73. Liu X, Wang L, Zhao K, Thompson PR, Hwang Y, Marmorstein R, Cole PA (2008) The
structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature
451:846–850. https://doi.org/10.1038/nature06546
74. Wu J, Xie N, Wu Z, Zhang Y, Zheng YG (2009) Bisubstrate inhibitors of the MYST HATs
Esa1 and Tip60. Bioorg Med Chem 17:1381–1386. https://doi.org/10.1016/j.bmc.2008.12.
014
75. Cullis PM, Wolfenden R, Cousens LS, Alberts BM (1982) Inhibition of histone acetylation by
N-[2-(S-coenzyme A)acetyl] spermidine amide, a multisubstrate analog. J Biol Chem
257:12165–12169
76. Bandyopadhyay K, Baneres JL, Martin A, Blonski C, Parello J, Gjerset RA (2009)
Spermidinyl-CoA-based HAT inhibitors block DNA repair and provide cancer-specific
chemo- and radiosensitization. Cell Cycle 8:2779–2788
77. Balasubramanyam K, Swaminathan V, Ranganathan A, Kundu TK (2003) Small molecule
modulators of histone acetyltransferase p300. J Biol Chem 278:19134–19140. https://doi.org/
10.1074/jbc.M301580200
78. Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y (2012) 6-alkylsalicylates
are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem
47:337–344. https://doi.org/10.1016/j.ejmech.2011.11.001
79. Wapenaar H, van der Wouden PE, Groves MR, Rotili D, Mai A, Dekker FJ (2015) Enzyme
kinetics and inhibition of histone acetyltransferase KAT8. Eur J Med Chem 105:289–296.
https://doi.org/10.1016/j.ejmech.2015.10.016
80. Hemshekhar M, Sebastin Santhosh M, Kemparaju K, Girish KS (2012) Emerging roles of
anacardic acid and its derivatives: a pharmacological overview. Basic Clin Pharmacol Toxicol
110:122–132. https://doi.org/10.1111/j.1742-7843.2011.00833.x
81. Ornaghi P, Rotili D, Sbardella G, Mai A, Filetici P (2005) A novel Gcn5p inhibitor represses
cell growth, gene transcription and histone acetylation in budding yeast. Biochem Pharmacol
70:911–917. https://doi.org/10.1016/j.bcp.2005.06.013
82. Mai A, Rotili D, Tarantino D, Ornaghi P, Tosi F, Vicidomini C, Sbardella G, Nebbioso A,
Miceli M, Altucci L, Filetici P (2006) Small-molecule inhibitors of histone acetyltransferase
activity: identification and biological properties. J Med Chem 49:6897–6907. https://doi.org/
10.1021/jm060601m
83. Mai A, Rotili D, Tarantino D, Nebbioso A, Castellano S, Sbardella G, Tini M, Altucci L (2009)
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases.
Bioorg Med Chem Lett 19:1132–1135. https://doi.org/10.1016/j.bmcl.2008.12.097
84. Lenoci A, Tomassi S, Conte M, Benedetti R, Rodriguez V, Carradori S, Secci D, Castellano S,
Sbardella G, Filetici P, Novellino E, Altucci L, Rotili D, Mai A (2014) Quinoline-based p300
Histone Acetyltransferase Enzymes: From Biological Implications to Most. . .
119
Murdock DM, Jiang MM, Lammer EJ, Enns GM, Rhead WJ, Rowland J, Robertson SP,
Cormier-Daire V, Bainbridge MN, Yang XJ, Gingras MC, Gibbs RA, Rosenblatt DS,
Majewski J, Lee BH (2012) Mutations in KAT6B, encoding a histone acetyltransferase,
cause Genitopatellar syndrome. Am J Hum Genet 90:282–289. https://doi.org/10.1016/j.
ajhg.2011.11.023
69. Wang Y, Miao X, Liu Y, Li F, Liu Q, Sun J, Cai L (2014) Dysregulation of histone
acetyltransferases and deacetylases in cardiovascular diseases. Oxid Med Cell Longev
2014:641979. https://doi.org/10.1155/2014/641979
70. Yanazume T, Hasegawa K, Morimoto T, Kawamura T, Wada H, Matsumori A, Kawase Y,
Hirai M, Kita T (2003) Cardiac p300 is involved in myocyte growth with decompensated heart
failure. Mol Cell Biol 23:3593–3606
71. Iyer A, Fairlie DP, Brown L (2012) Lysine acetylation in obesity, diabetes and metabolic
disease. Immunol Cell Biol 90:39–46. https://doi.org/10.1038/icb.2011.99
72. Lau OD, Kundu TK, Soccio RE, Ait-Si-Ali S, Khalil EM, Vassilev A, Wolffe AP, Nakatani Y,
Roeder RG, Cole PA (2000) HATs off: selective synthetic inhibitors of the histone
acetyltransferases p300 and PCAF. Mol Cell 5:589–595
73. Liu X, Wang L, Zhao K, Thompson PR, Hwang Y, Marmorstein R, Cole PA (2008) The
structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature
451:846–850. https://doi.org/10.1038/nature06546
74. Wu J, Xie N, Wu Z, Zhang Y, Zheng YG (2009) Bisubstrate inhibitors of the MYST HATs
Esa1 and Tip60. Bioorg Med Chem 17:1381–1386. https://doi.org/10.1016/j.bmc.2008.12.
014
75. Cullis PM, Wolfenden R, Cousens LS, Alberts BM (1982) Inhibition of histone acetylation by
N-[2-(S-coenzyme A)acetyl] spermidine amide, a multisubstrate analog. J Biol Chem
257:12165–12169
76. Bandyopadhyay K, Baneres JL, Martin A, Blonski C, Parello J, Gjerset RA (2009)
Spermidinyl-CoA-based HAT inhibitors block DNA repair and provide cancer-specific
chemo- and radiosensitization. Cell Cycle 8:2779–2788
77. Balasubramanyam K, Swaminathan V, Ranganathan A, Kundu TK (2003) Small molecule
modulators of histone acetyltransferase p300. J Biol Chem 278:19134–19140. https://doi.org/
10.1074/jbc.M301580200
78. Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y (2012) 6-alkylsalicylates
are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem
47:337–344. https://doi.org/10.1016/j.ejmech.2011.11.001
79. Wapenaar H, van der Wouden PE, Groves MR, Rotili D, Mai A, Dekker FJ (2015) Enzyme
kinetics and inhibition of histone acetyltransferase KAT8. Eur J Med Chem 105:289–296.
https://doi.org/10.1016/j.ejmech.2015.10.016
80. Hemshekhar M, Sebastin Santhosh M, Kemparaju K, Girish KS (2012) Emerging roles of
anacardic acid and its derivatives: a pharmacological overview. Basic Clin Pharmacol Toxicol
110:122–132. https://doi.org/10.1111/j.1742-7843.2011.00833.x
81. Ornaghi P, Rotili D, Sbardella G, Mai A, Filetici P (2005) A novel Gcn5p inhibitor represses
cell growth, gene transcription and histone acetylation in budding yeast. Biochem Pharmacol
70:911–917. https://doi.org/10.1016/j.bcp.2005.06.013
82. Mai A, Rotili D, Tarantino D, Ornaghi P, Tosi F, Vicidomini C, Sbardella G, Nebbioso A,
Miceli M, Altucci L, Filetici P (2006) Small-molecule inhibitors of histone acetyltransferase
activity: identification and biological properties. J Med Chem 49:6897–6907. https://doi.org/
10.1021/jm060601m
83. Mai A, Rotili D, Tarantino D, Nebbioso A, Castellano S, Sbardella G, Tini M, Altucci L (2009)
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases.
Bioorg Med Chem Lett 19:1132–1135. https://doi.org/10.1016/j.bmcl.2008.12.097
84. Lenoci A, Tomassi S, Conte M, Benedetti R, Rodriguez V, Carradori S, Secci D, Castellano S,
Sbardella G, Filetici P, Novellino E, Altucci L, Rotili D, Mai A (2014) Quinoline-based p300
Histone Acetyltransferase Enzymes: From Biological Implications to Most. . .
119