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55. Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H,
Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che
KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio
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doi.org/10.1038/nature13229
41. Hu P, Wang X, Zhang B, Zhang S, Wang Q, Wang Z (2014) Fluorescence polarization for
the evaluation of small-molecule inhibitors of PCAF BRD/Tat-AcK50 association.
ChemMedChem 9(5):928–931. https://doi.org/10.1002/cmdc.201300499
42. Moustakim M, Clark PGK, Trulli L, de Arriba ALF, Ehebauer MT, Chaikuad A, Murphy EJ,
Mendez-Johnson J, Daniels D, Hou CFD, Lin YH, Walker JR, Hui R, Yang HB, Dorrell L,
Rogers CM, Monteiro OP, Fedorov O, Huber KVM, Knapp S, Heer J, Dixon DJ, Brennan PE
(2017) Discovery of a PCAF bromodomain chemical probe. Angew Chem Int Ed
56(3):827–831. https://doi.org/10.1002/anie.201610816
43. Picaud S, Leonards K, Lambert J-P, Dovey O, Wells C, Fedorov O, Monteiro O, Fujisawa T,
Wang C-Y, Lingard H, Tallant C, Nikbin N, Guetzoyan L, Ingham R, Ley SV, Brennan P,
Muller S, Samsonova A, Gingras A-C, Schwaller J, Vassiliou G, Knapp S, Filippakopoulos P
(2016) Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as
master regulators of primary transcription response in leukemia. Sci Adv 2(10):e1600760.
https://doi.org/10.1126/sciadv.1600760
44. Humphreys PG, Bamborough P, Chung C-W, Crags PD, Gordon L, Grandi P, Hayhow TG,
Hussain J, Jones KL, Lindon M, Michon A-M, Renaux JF, Suckling CJ, Tough DF, Prinjha
RK (2017) Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor
(PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probe. J Med
Chem 60(2):695–709. https://doi.org/10.1021/acs.jmedchem.6b01566
45. Goodman RH, Smolik S (2000) CBP/p300 in cell growth, transformation, and development.
Genes Dev 14(13):1553–1577
46. Zhang ZW, Hofmann C, Casanova E, Schutz G, Lutz B (2004) Generation of a conditional
allele of the CBP gene in mouse. Genesis 40(2):82–89. https://doi.org/10.1002/gene.20068
47. Korzus E (2017) Rubinstein-Taybi syndrome and epigenetic alterations. Adv Exp Med Biol
978:39–62. https://doi.org/10.1007/978-3-319-53889-1_3
48. Sachchidanand, Resnick-Silverman L, Yan S, Mutjaba S, Liu WJ, Zeng L, Manfredi JJ, Zhou
MM (2006) Target structure-based discovery of small molecules that block human p53 and
CREB binding protein association. Chem Biol 13(1):81–90. https://doi.org/10.1016/j.
chembiol.2005.10.014
49. Shankar DB, Cheng JC, Sakamoto KM (2005) Role of cyclic AMP response element binding
protein in human leukemias. Cancer 104(9):1819–1824. https://doi.org/10.1002/cncr.21401
50. Iyer NG, Ozdag H, Caldas C (2004) p300/CBP and cancer. Oncogene 23(24):4225–4231.
https://doi.org/10.1038/sj.onc.1207118
51. Gerona-Navarro G, Yoel R, Mujtaba S, Frasca A, Patel J, Zeng L, Plotnikov AN, Osman R,
Zhou M-M (2011) Rational design of cyclic peptide modulators of the transcriptional
coactivator CBP: a new class of p53 inhibitors. J Am Chem Soc 133(7):2040–2043. https://
doi.org/10.1021/ja107761h
52. Borah JC, Mujtaba S, Karakikes I, Zeng L, Muller M, Patel J, Moshkina N, Morohashi K,
Zhang W, Gerona-Navarro G, Hajjar RJ, Zhou M-M (2011) A small molecule binding to
the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. Chem Biol
18(4):531–541. https://doi.org/10.1016/j.chembiol.2010.12.021
53. Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin
SJ, Felletar I, Marsden BD, Filippakopoulos P, Mueller S, Knapp S, Brennan PE (2014) 1,2,4
Triazolo 4,3-a phthalazines: inhibitors of diverse bromodomains. J Med Chem 57(2):462–476.
https://doi.org/10.1021/jm401568s
54. Rooney TPC, Filippakopoulos P, Fedorov O, Picaud S, Cortopassi WA, Hay DA, Martin S,
Tumber A, Rogers CM, Philpott M, Wang M, Thompson AL, Heightman TD, Pryde DC,
Cook A, Paton RS, Mueller S, Knapp S, Brennan PE, Conway SJ (2014) A series of potent
CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-pi interaction. Angew Chem Int Ed 53(24):6126–6130. https://doi.org/10.1002/anie.201402750
55. Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H,
Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che
KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio
330
W. C. K. Pomerantz et al.