histone acetyltransferase inhibitors with pro-apoptotic activity in human leukemia U937 cells.
ChemMedChem 9:542–548. https://doi.org/10.1002/cmdc.201300536
85. Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A
(2008) Identification of long chain alkylidenemalonates as novel small molecule modulators of
histone acetyltransferases. Bioorg Med Chem Lett 18:2788–2792. https://doi.org/10.1016/j.
bmcl.2008.04.017
86. Castellano S, Milite C, Feoli A, Viviano M, Mai A, Novellino E, Tosco A, Sbardella G (2015)
Identification of structural features of 2-alkylidene-1,3-dicarbonyl derivatives that induce
inhibition and/or activation of histone acetyltransferases KAT3B/p300 and KAT2B/PCAF.
ChemMedChem 10:144–157. https://doi.org/10.1002/cmdc.201402371
87. Balasubramanyam K, Varier RA, Altaf M, Swaminathan V, Siddappa NB, Ranga U, Kundu TK
(2004) Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase,
represses the acetylation of histone/nonhistone proteins and histone acetyltransferasedependent chromatin transcription. J Biol Chem 279:51163–51171. https://doi.org/10.1074/
jbc.M409024200
88. Marcu MG, Jung YJ, Lee S, Chung EJ, Lee MJ, Trepel J, Neckers L (2006) Curcumin is an
inhibitor of p300 histone acetylatransferase. Med Chem 2:169–174
89. Fu S, Kurzrock R (2010) Development of curcumin as an epigenetic agent. Cancer
116:4670–4676. https://doi.org/10.1002/cncr.25414
90. Ingolfsson HI, Thakur P, Herold KF, Hobart EA, Ramsey NB, Periole X, de Jong DH,
Zwama M, Yilmaz D, Hall K, Maretzky T, Hemmings HC Jr, Blobel C, Marrink SJ,
Kocer A, Sack JT, Andersen OS (2014) Phytochemicals perturb membranes and promiscuously alter protein function. ACS Chem Biol 9:1788–1798. https://doi.org/10.1021/
cb500086e
91. Nelson KM, Dahlin JL, Bisson J, Graham J, Pauli GF, Walters MA (2017) The essential
medicinal chemistry of curcumin. J Med Chem 60:1620–1637. https://doi.org/10.1021/acs.
jmedchem.6b00975
92. Arif M, Vedamurthy BM, Choudhari R, Ostwal YB, Mantelingu K, Kodaganur GS, Kundu
TK (2010) Nitric oxide-mediated histone hyperacetylation in oral cancer: target for a watersoluble HAT inhibitor, CTK7A. Chem Biol 17:903–913. https://doi.org/10.1016/j.chembiol.
2010.06.014
93. Balasubramanyam K, Altaf M, Varier RA, Swaminathan V, Ravindran A, Sadhale PP, Kundu
TK (2004) Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase
inhibitor, represses chromatin transcription and alters global gene expression. J Biol Chem
279:33716–33726. https://doi.org/10.1074/jbc.M402839200
94. Mantelingu K, Reddy BA, Swaminathan V, Kishore AH, Siddappa NB, Kumar GV,
Nagashankar G, Natesh N, Roy S, Sadhale PP, Ranga U, Narayana C, Kundu TK (2007)
Specific inhibition of p300-HAT alters global gene expression and represses HIV replication.
Chem Biol 14:645–657. https://doi.org/10.1016/j.chembiol.2007.04.011
95. Arif M, Pradhan SK, Thanuja GR, Vedamurthy BM, Agrawal S, Dasgupta D, Kundu TK
(2009) Mechanism of p300 specific histone acetyltransferase inhibition by small molecules. J
Med Chem 52:267–277. https://doi.org/10.1021/jm800657z
96. Milite C, Feoli A, Sasaki K, La Pietra V, Balzano AL, Marinelli L, Mai A, Novellino E,
Castellano S, Tosco A, Sbardella G (2015) A novel cell-permeable, selective, and
noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular
pruning/classical isosterism approach. J Med Chem 58:2779–2798. https://doi.org/10.1021/
jm5019687
97. Tohyama S, Tomura A, Ikeda N, Hatano M, Odanaka J, Kubota Y, Umekita M, Igarashi M,
Sawa R, Morino T (2012) Discovery and characterization of NK13650s, naturally occurring
p300-selective histone acetyltransferase inhibitors. J Org Chem 77:9044–9052. https://doi.org/
10.1021/jo301534b
98. Stimson L, Rowlands MG, Newbatt YM, Smith NF, Raynaud FI, Rogers P, Bavetsias V,
Gorsuch S, Jarman M, Bannister A, Kouzarides T, McDonald E, Workman P, Aherne GW
120
D. Trisciuoglio and D. Rotili
ChemMedChem 9:542–548. https://doi.org/10.1002/cmdc.201300536
85. Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A
(2008) Identification of long chain alkylidenemalonates as novel small molecule modulators of
histone acetyltransferases. Bioorg Med Chem Lett 18:2788–2792. https://doi.org/10.1016/j.
bmcl.2008.04.017
86. Castellano S, Milite C, Feoli A, Viviano M, Mai A, Novellino E, Tosco A, Sbardella G (2015)
Identification of structural features of 2-alkylidene-1,3-dicarbonyl derivatives that induce
inhibition and/or activation of histone acetyltransferases KAT3B/p300 and KAT2B/PCAF.
ChemMedChem 10:144–157. https://doi.org/10.1002/cmdc.201402371
87. Balasubramanyam K, Varier RA, Altaf M, Swaminathan V, Siddappa NB, Ranga U, Kundu TK
(2004) Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase,
represses the acetylation of histone/nonhistone proteins and histone acetyltransferasedependent chromatin transcription. J Biol Chem 279:51163–51171. https://doi.org/10.1074/
jbc.M409024200
88. Marcu MG, Jung YJ, Lee S, Chung EJ, Lee MJ, Trepel J, Neckers L (2006) Curcumin is an
inhibitor of p300 histone acetylatransferase. Med Chem 2:169–174
89. Fu S, Kurzrock R (2010) Development of curcumin as an epigenetic agent. Cancer
116:4670–4676. https://doi.org/10.1002/cncr.25414
90. Ingolfsson HI, Thakur P, Herold KF, Hobart EA, Ramsey NB, Periole X, de Jong DH,
Zwama M, Yilmaz D, Hall K, Maretzky T, Hemmings HC Jr, Blobel C, Marrink SJ,
Kocer A, Sack JT, Andersen OS (2014) Phytochemicals perturb membranes and promiscuously alter protein function. ACS Chem Biol 9:1788–1798. https://doi.org/10.1021/
cb500086e
91. Nelson KM, Dahlin JL, Bisson J, Graham J, Pauli GF, Walters MA (2017) The essential
medicinal chemistry of curcumin. J Med Chem 60:1620–1637. https://doi.org/10.1021/acs.
jmedchem.6b00975
92. Arif M, Vedamurthy BM, Choudhari R, Ostwal YB, Mantelingu K, Kodaganur GS, Kundu
TK (2010) Nitric oxide-mediated histone hyperacetylation in oral cancer: target for a watersoluble HAT inhibitor, CTK7A. Chem Biol 17:903–913. https://doi.org/10.1016/j.chembiol.
2010.06.014
93. Balasubramanyam K, Altaf M, Varier RA, Swaminathan V, Ravindran A, Sadhale PP, Kundu
TK (2004) Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase
inhibitor, represses chromatin transcription and alters global gene expression. J Biol Chem
279:33716–33726. https://doi.org/10.1074/jbc.M402839200
94. Mantelingu K, Reddy BA, Swaminathan V, Kishore AH, Siddappa NB, Kumar GV,
Nagashankar G, Natesh N, Roy S, Sadhale PP, Ranga U, Narayana C, Kundu TK (2007)
Specific inhibition of p300-HAT alters global gene expression and represses HIV replication.
Chem Biol 14:645–657. https://doi.org/10.1016/j.chembiol.2007.04.011
95. Arif M, Pradhan SK, Thanuja GR, Vedamurthy BM, Agrawal S, Dasgupta D, Kundu TK
(2009) Mechanism of p300 specific histone acetyltransferase inhibition by small molecules. J
Med Chem 52:267–277. https://doi.org/10.1021/jm800657z
96. Milite C, Feoli A, Sasaki K, La Pietra V, Balzano AL, Marinelli L, Mai A, Novellino E,
Castellano S, Tosco A, Sbardella G (2015) A novel cell-permeable, selective, and
noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular
pruning/classical isosterism approach. J Med Chem 58:2779–2798. https://doi.org/10.1021/
jm5019687
97. Tohyama S, Tomura A, Ikeda N, Hatano M, Odanaka J, Kubota Y, Umekita M, Igarashi M,
Sawa R, Morino T (2012) Discovery and characterization of NK13650s, naturally occurring
p300-selective histone acetyltransferase inhibitors. J Org Chem 77:9044–9052. https://doi.org/
10.1021/jo301534b
98. Stimson L, Rowlands MG, Newbatt YM, Smith NF, Raynaud FI, Rogers P, Bavetsias V,
Gorsuch S, Jarman M, Bannister A, Kouzarides T, McDonald E, Workman P, Aherne GW
120
D. Trisciuoglio and D. Rotili