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(2017) Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors. Nat Commun 8:1527. https://doi.org/10.1038/s41467-017-01657-3
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M (2014) Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs).
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101. Furdas SD, Shekfeh S, Bissinger EM, Wagner JM, Schlimme S, Valkov V, Hendzel M,
Jung M, Sippl W (2011) Synthesis and biological testing of novel pyridoisothiazolones as
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1016/j.bmc.2011.01.063
102. Gajer JM, Furdas SD, Grunder A, Gothwal M, Heinicke U, Keller K, Colland F, Fulda S, Pahl
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103. Chimenti F, Bizzarri B, Maccioni E, Secci D, Bolasco A, Chimenti P, Fioravanti R, Granese A,
Carradori S, Tosi F, Ballario P, Vernarecci S, Filetici P (2009) A novel histone
acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4
0 -chlorophenyl)
thiazol-2-yl]hydrazone. J Med Chem 52:530–536. https://doi.org/10.1021/jm800885d
104. Trisciuoglio D, Ragazzoni Y, Pelosi A, Desideri M, Carradori S, Gabellini C, Maresca G,
Nescatelli R, Secci D, Bolasco A, Bizzarri B, Cavaliere C, D’Agnano I, Filetici P, RicciVitiani L, Rizzo MG, del Bufalo D (2012) CPTH6, a thiazole derivative, induces histone
hypoacetylation and apoptosis in human leukemia cells. Clin Cancer Res 18:475–486. https://
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105. Ragazzoni Y, Desideri M, Gabellini C, de Luca T, Carradori S, Secci D, Nescatelli R,
Candiloro A, Condello M, Meschini S, del Bufalo D, Trisciuoglio D (2013) The thiazole
derivative CPTH6 impairs autophagy. Cell Death Dis 4:e524. https://doi.org/10.1038/cddis.
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106. di Martile M, Desideri M, de Luca T, Gabellini C, Buglioni S, Eramo A, Sette G, Milella M,
Rotili D, Mai A, Carradori S, Secci D, de Maria R, del Bufalo D, Trisciuoglio D (2016)
Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells.
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107. Carradori S, Rotili D, de Monte C, Lenoci A, D’Ascenzio M, Rodriguez V, Filetici P,
Miceli M, Nebbioso A, Altucci L, Secci D, Mai A (2014) Evaluation of a large library of
(thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and
cellular studies. Eur J Med Chem 80:569–578. https://doi.org/10.1016/j.ejmech.2014.04.042
108. Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA,
Liszczak G, Yuan H, Larocca C, Saldanha SA, Abagyan R, Sun Y, Meyers DJ,
Marmorstein R, Mahadevan LC, Alani RM, Cole PA (2010) Virtual ligand screening of the
p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.
Chem Biol 17:471–482. https://doi.org/10.1016/j.chembiol.2010.03.006
109. Shrimp JH, Sorum AW, Garlick JM, Guasch L, Nicklaus MC, Meier JL (2015) Characterizing
the covalent targets of a small molecule inhibitor of the lysine acetyltransferase P300. ACS
Med Chem Lett 7:151–155. https://doi.org/10.1021/acsmedchemlett.5b00385
110. Dancy BM, Crump NT, Peterson DJ, Mukherjee C, Bowers EM, Ahn YH, Yoshida M,
Zhang J, Mahadevan LC, Meyers DJ, Boeke JD, Cole PA (2012) Live-cell studies of p300/
CBP histone acetyltransferase activity and inhibition. Chembiochem 13:2113–2121. https://
doi.org/10.1002/cbic.201200381
111. Gao XN, Lin J, Ning QY, Gao L, Yao YS, Zhou JH, Li YH, Wang LL, Yu L (2013) A histone
acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in
AML1-ETO-positive AML cells. PLoS One 8:e55481. https://doi.org/10.1371/journal.pone.
0055481
Histone Acetyltransferase Enzymes: From Biological Implications to Most. . .
121
Cancer Ther 4:1521–1532. https://doi.org/10.1158/1535-7163.MCT-05-0135
99. Dahlin JL, Nelson KM, Strasser JM, Barsyte-Lovejoy D, Szewczyk MM, Organ S, Cuellar M,
Singh G, Shrimp JH, Nguyen N, Meier JL, Arrowsmith CH, Brown PJ, Baell JB, Walters MA
(2017) Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors. Nat Commun 8:1527. https://doi.org/10.1038/s41467-017-01657-3
100. Furdas SD, Hoffmann I, Robaa D, Herquel B, Malinka W, Świątek P, Akhtar A, Sippl W, Jung
M (2014) Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs).
Med Chem Commun 5(12):1856
101. Furdas SD, Shekfeh S, Bissinger EM, Wagner JM, Schlimme S, Valkov V, Hendzel M,
Jung M, Sippl W (2011) Synthesis and biological testing of novel pyridoisothiazolones as
histone acetyltransferase inhibitors. Bioorg Med Chem 19:3678–3689. https://doi.org/10.
1016/j.bmc.2011.01.063
102. Gajer JM, Furdas SD, Grunder A, Gothwal M, Heinicke U, Keller K, Colland F, Fulda S, Pahl
HL, Fichtner I, Sippl W, Jung M (2015) Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogene 4:e137. https://doi.org/10.1038/oncsis.2014.51
103. Chimenti F, Bizzarri B, Maccioni E, Secci D, Bolasco A, Chimenti P, Fioravanti R, Granese A,
Carradori S, Tosi F, Ballario P, Vernarecci S, Filetici P (2009) A novel histone
acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4
0 -chlorophenyl)
thiazol-2-yl]hydrazone. J Med Chem 52:530–536. https://doi.org/10.1021/jm800885d
104. Trisciuoglio D, Ragazzoni Y, Pelosi A, Desideri M, Carradori S, Gabellini C, Maresca G,
Nescatelli R, Secci D, Bolasco A, Bizzarri B, Cavaliere C, D’Agnano I, Filetici P, RicciVitiani L, Rizzo MG, del Bufalo D (2012) CPTH6, a thiazole derivative, induces histone
hypoacetylation and apoptosis in human leukemia cells. Clin Cancer Res 18:475–486. https://
doi.org/10.1158/1078-0432.CCR-11-0579
105. Ragazzoni Y, Desideri M, Gabellini C, de Luca T, Carradori S, Secci D, Nescatelli R,
Candiloro A, Condello M, Meschini S, del Bufalo D, Trisciuoglio D (2013) The thiazole
derivative CPTH6 impairs autophagy. Cell Death Dis 4:e524. https://doi.org/10.1038/cddis.
2013.53
106. di Martile M, Desideri M, de Luca T, Gabellini C, Buglioni S, Eramo A, Sette G, Milella M,
Rotili D, Mai A, Carradori S, Secci D, de Maria R, del Bufalo D, Trisciuoglio D (2016)
Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells.
Oncotarget 7:11332–11348. https://doi.org/10.18632/oncotarget.7238
107. Carradori S, Rotili D, de Monte C, Lenoci A, D’Ascenzio M, Rodriguez V, Filetici P,
Miceli M, Nebbioso A, Altucci L, Secci D, Mai A (2014) Evaluation of a large library of
(thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and
cellular studies. Eur J Med Chem 80:569–578. https://doi.org/10.1016/j.ejmech.2014.04.042
108. Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA,
Liszczak G, Yuan H, Larocca C, Saldanha SA, Abagyan R, Sun Y, Meyers DJ,
Marmorstein R, Mahadevan LC, Alani RM, Cole PA (2010) Virtual ligand screening of the
p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.
Chem Biol 17:471–482. https://doi.org/10.1016/j.chembiol.2010.03.006
109. Shrimp JH, Sorum AW, Garlick JM, Guasch L, Nicklaus MC, Meier JL (2015) Characterizing
the covalent targets of a small molecule inhibitor of the lysine acetyltransferase P300. ACS
Med Chem Lett 7:151–155. https://doi.org/10.1021/acsmedchemlett.5b00385
110. Dancy BM, Crump NT, Peterson DJ, Mukherjee C, Bowers EM, Ahn YH, Yoshida M,
Zhang J, Mahadevan LC, Meyers DJ, Boeke JD, Cole PA (2012) Live-cell studies of p300/
CBP histone acetyltransferase activity and inhibition. Chembiochem 13:2113–2121. https://
doi.org/10.1002/cbic.201200381
111. Gao XN, Lin J, Ning QY, Gao L, Yao YS, Zhou JH, Li YH, Wang LL, Yu L (2013) A histone
acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in
AML1-ETO-positive AML cells. PLoS One 8:e55481. https://doi.org/10.1371/journal.pone.
0055481
Histone Acetyltransferase Enzymes: From Biological Implications to Most. . .
121