메뉴 건너뛰기




Volumn 6, Issue 5, 2014, Pages 473-476

Epigenetic drug therapy based on bromodomain inhibition

Author keywords

BET family; bromodomain; epigenetic inhibitors; histone acetylation; small molecule therapies

Indexed keywords

2 MORPHOLINO 8 PHENYLCHROMONE; 4 (4 CHLOROPHENYL) 2,3,9 TRIMETHYL 6H THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE 6 ACETIC ACID TERT BUTYL ESTER; 6 (4 CHLOROPHENYL) N ETHYL 8 METHOXY 1 METHYL 4H [1,2,4]TRIAZOLO[4,3 A][1,4]BENZODIAZEPINE 4 ACETAMIDE; 7 (3,5 DIMETHYL 4 ISOXAZOLYL) 1,3 DIHYDRO 8 METHOXY 1 [1 (2 PYRIDINYL)ETHYL] 2H IMIDAZO[4,5 C]QUINOLIN 2 ONE; APABETALONE; BROMODOMAIN INHIBITOR; UNCLASSIFIED DRUG; ZINC01411240; ZINC04818522; ZINC19632618; NUCLEAR PROTEIN;

EID: 84913610674     PISSN: 17501911     EISSN: 1750192X     Source Type: Journal    
DOI: 10.2217/epi.14.45     Document Type: Note
Times cited : (1)

References (39)
  • 1
    • 84899973908 scopus 로고    scopus 로고
    • Targeting bromodomains: Epigenetic readers of lysine acetylation
    • Filippakopoulos P, Knapp S. Targeting bromodomains: epigenetic readers of lysine acetylation. Nat. Rev. Drug Discov. 13(5), 337-356 (2014).
    • (2014) Nat. Rev. Drug Discov. , vol.13 , Issue.5 , pp. 337-356
    • Filippakopoulos, P.1    Knapp, S.2
  • 2
    • 84896697426 scopus 로고    scopus 로고
    • Bromodomains and their pharmacological inhibitors
    • Gallenkamp D, Gelato KA, Haendler B et al. Bromodomains and their pharmacological inhibitors. Chem. Med. Chem. 9(3), 438-464 (2014).
    • (2014) Chem. Med. Chem. , vol.9 , Issue.3 , pp. 438-464
    • Gallenkamp, D.1    Gelato, K.A.2    Haendler, B.3
  • 3
    • 84901821841 scopus 로고    scopus 로고
    • The mechanisms behind the therapeutic activity of BET bromodomain inhibition
    • Shi J, Vakoc CR. The mechanisms behind the therapeutic activity of BET bromodomain inhibition. Mol. Cell 54(5), 728-736 (2014).
    • (2014) Mol. Cell , vol.54 , Issue.5 , pp. 728-736
    • Shi, J.1    Vakoc, C.R.2
  • 4
    • 84876222028 scopus 로고    scopus 로고
    • Selective inhibition of tumor oncogenes by disruption of super-enhancers
    • Lovén J, Hoke HA, Lin CY et al. Selective inhibition of tumor oncogenes by disruption of super-enhancers. Cell 153(2), 320-334 (2013).
    • (2013) Cell , vol.153 , Issue.2 , pp. 320-334
    • Lovén, J.1    Hoke, H.A.2    Lin, C.Y.3
  • 5
    • 84888015137 scopus 로고    scopus 로고
    • Super-enhancers in the control of cell identity and disease
    • Hnisz D, Abraham BJ, Lee TI et al. Super-enhancers in the control of cell identity and disease. Cell 155(4), 934-947 (2013).
    • (2013) Cell , vol.155 , Issue.4 , pp. 934-947
    • Hnisz, D.1    Abraham, B.J.2    Lee, T.I.3
  • 6
    • 84903954080 scopus 로고    scopus 로고
    • BET inhibitor JQ1 blocks infammation and bone destruction
    • Meng S, Zhang L, Tang Y et al. BET inhibitor JQ1 blocks infammation and bone destruction. J. Dent. Res. 93(7), 657-662 (2014).
    • (2014) J. Dent. Res. , vol.93 , Issue.7 , pp. 657-662
    • Meng, S.1    Zhang, L.2    Tang, Y.3
  • 7
    • 84880588126 scopus 로고    scopus 로고
    • Assessment of Brd4 inhibition in idiopathic pulmonary fbrosis lung fbroblasts and in vivo models of lung fbrosis
    • Tang X, Peng R, Phillips JE et al. Assessment of Brd4 inhibition in idiopathic pulmonary fbrosis lung fbroblasts and in vivo models of lung fbrosis. Am. J. Pathol. 183(2), 470-479 (2013).
    • (2013) Am. J. Pathol. , vol.183 , Issue.2 , pp. 470-479
    • Tang, X.1    Peng, R.2    Phillips, J.E.3
  • 8
    • 84903744128 scopus 로고    scopus 로고
    • Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle
    • Lamoureux F, Baud'huin M, Rodriguez Calleja L et al. Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle. Nat. Commun. 5, 355 (2014).
    • (2014) Nat. Commun. , vol.5 , pp. 355
    • Lamoureux, F.1    Baud'Huin, M.2    Rodriguez Calleja, L.3
  • 9
    • 84901256398 scopus 로고    scopus 로고
    • Bromodomain and extraterminal proteins suppress NF-E2-related factor 2-mediated antioxidant gene expression
    • Michaeloudes C, Mercado N, Clarke C et al. Bromodomain and extraterminal proteins suppress NF-E2-related factor 2-mediated antioxidant gene expression. J. Immunol. 192(10), 4913-4920 (2014).
    • (2014) J. Immunol. , vol.192 , Issue.10 , pp. 4913-4920
    • Michaeloudes, C.1    Mercado, N.2    Clarke, C.3
  • 10
    • 84901004504 scopus 로고    scopus 로고
    • The bromodomain protein BRD4 regulates the KEAP1/NRF2-dependent oxidative stress response
    • Hussong M, Börno ST, Kerick M et al. The bromodomain protein BRD4 regulates the KEAP1/NRF2-dependent oxidative stress response. Cell Death Dis. 5, e1195 (2014).
    • (2014) Cell Death Dis. , vol.5 , pp. e1195
    • Hussong, M.1    Börno, S.T.2    Kerick, M.3
  • 11
    • 84897486329 scopus 로고    scopus 로고
    • Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis
    • Ray S, Zhao Y, Jamaluddin M et al. Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis. Cell Signal. 26(7), 1445-1455 (2014).
    • (2014) Cell Signal. , vol.26 , Issue.7 , pp. 1445-1455
    • Ray, S.1    Zhao, Y.2    Jamaluddin, M.3
  • 12
    • 84899840925 scopus 로고    scopus 로고
    • Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2
    • Liu S, Walker SR, Nelson EA et al. Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2. Mol. Cancer Ther. 13(5), 1194-1205 (2014).
    • (2014) Mol. Cancer Ther. , vol.13 , Issue.5 , pp. 1194-1205
    • Liu, S.1    Walker, S.R.2    Nelson, E.A.3
  • 13
    • 84913617113 scopus 로고    scopus 로고
    • Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma
    • In Press)
    • Trabucco SE, Gerstein RM, Evens AM et al. Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma. Clin. Cancer Res. (2014) (In Press).
    • (2014) Clin. Cancer Res
    • Trabucco, S.E.1    Gerstein, R.M.2    Evens, A.M.3
  • 14
    • 84899948906 scopus 로고    scopus 로고
    • BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1
    • Stewart HJ, Horne GA, Bastow S et al. BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1. Cancer Med. 2(6), 826-835 (2013).
    • (2013) Cancer Med. , vol.2 , Issue.6 , pp. 826-835
    • Stewart, H.J.1    Horne, G.A.2    Bastow, S.3
  • 15
    • 84906968200 scopus 로고    scopus 로고
    • BET bromodomain protein inhibition is a therapeutic option for medulloblastoma
    • Henssen A, Thor T, Odersky A et al. BET bromodomain protein inhibition is a therapeutic option for medulloblastoma. Oncotarget 4(11), 2080-2095 (2013).
    • (2013) Oncotarget , vol.4 , Issue.11 , pp. 2080-2095
    • Henssen, A.1    Thor, T.2    Odersky, A.3
  • 16
    • 84880894039 scopus 로고    scopus 로고
    • BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia
    • Da Costa D, Agathanggelou A, Perry T et al. BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia. Blood Cancer J. 3, e126 (2013).
    • (2013) Blood Cancer J. , vol.3 , pp. e126
    • Da Costa, D.1    Agathanggelou, A.2    Perry, T.3
  • 17
    • 84896076685 scopus 로고    scopus 로고
    • C-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells
    • Roderick JE, Tesell J, Shultz LD et al. c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells. Blood 123(7), 1040-1050 (2014).
    • (2014) Blood , vol.123 , Issue.7 , pp. 1040-1050
    • Roderick, J.E.1    Tesell, J.2    Shultz, L.D.3
  • 18
    • 84902075847 scopus 로고    scopus 로고
    • Therapeutic targeting of c-Myc in T-Cell acute lymphoblastic leukemia, T-ALL
    • Loosveld M, Castellano R, Gon S et al. Therapeutic targeting of c-Myc in T-Cell acute lymphoblastic leukemia, T-ALL. Oncotarget 5 (10), 3168-3172 (2014).
    • (2014) Oncotarget , vol.5 , Issue.10 , pp. 3168-3172
    • Loosveld, M.1    Castellano, R.2    Gon, S.3
  • 19
    • 84899893338 scopus 로고    scopus 로고
    • Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells
    • Fiskus W, Sharma S, Qi J et al. Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells. Mol. Cancer Ther. 13(5), 1142-1154 (2014).
    • (2014) Mol. Cancer Ther. , vol.13 , Issue.5 , pp. 1142-1154
    • Fiskus, W.1    Sharma, S.2    Qi, J.3
  • 20
    • 84904036266 scopus 로고    scopus 로고
    • Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition
    • Tang Y, Gholamin S, Schubert S et al. Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition. Nat. Med. 20(7), 732-740 (2014).
    • (2014) Nat. Med. , vol.20 , Issue.7 , pp. 732-740
    • Tang, Y.1    Gholamin, S.2    Schubert, S.3
  • 21
    • 84913607582 scopus 로고    scopus 로고
    • Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151
    • In Press)
    • Gallagher SJ, Mijatov B, Gunatilake D et al. Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151. Pigment Cell Melanoma Res. (2014) (In Press).
    • (2014) Pigment Cell Melanoma Res
    • Gallagher, S.J.1    Mijatov, B.2    Gunatilake, D.3
  • 22
    • 84903716389 scopus 로고    scopus 로고
    • I-BET 151 selectively regulates IL-6 production
    • Barrett E, Brothers S, Wahlestedt C et al. I-BET 151 selectively regulates IL-6 production. Biochim. Biophys. Acta 1842(9), 1549-1555 (2014).
    • (2014) Biochim. Biophys. Acta , vol.1842 , Issue.9 , pp. 1549-1555
    • Barrett, E.1    Brothers, S.2    Wahlestedt, C.3
  • 23
    • 84897024898 scopus 로고    scopus 로고
    • Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762
    • Chaidos A, Caputo V, Gouvedenou K et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood 123(5), 697-705 (2014).
    • (2014) Blood , vol.123 , Issue.5 , pp. 697-705
    • Chaidos, A.1    Caputo, V.2    Gouvedenou, K.3
  • 24
    • 84891879120 scopus 로고    scopus 로고
    • BET protein inhibition shows effcacy against JAK2V617F-driven neoplasms
    • Wyspiańska BS, Bannister AJ, Barbieri I et al. BET protein inhibition shows effcacy against JAK2V617F-driven neoplasms. Leukemia 28(1), 88-97 (2014).
    • (2014) Leukemia , vol.28 , Issue.1 , pp. 88-97
    • Wyspiańska, B.S.1    Bannister, A.J.2    Barbieri, I.3
  • 25
    • 84899131911 scopus 로고    scopus 로고
    • BET bromodomain proteins are required for glioblastoma cell proliferation
    • Pastori C, Daniel M, Penas C et al. BET bromodomain proteins are required for glioblastoma cell proliferation. Epigenetics 9(4), 611-620 (2014).
    • (2014) Epigenetics , vol.9 , Issue.4 , pp. 611-620
    • Pastori, C.1    Daniel, M.2    Penas, C.3
  • 26
    • 84891921969 scopus 로고    scopus 로고
    • Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer
    • Wyce A, Degenhardt Y, Bai Y et al. Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer. Oncotarget 4(12), 2419-2429 (2013).
    • (2013) Oncotarget , vol.4 , Issue.12 , pp. 2419-2429
    • Wyce, A.1    Degenhardt, Y.2    Bai, Y.3
  • 27
    • 84885623316 scopus 로고    scopus 로고
    • The making of I-BET762, a BET bromodomain inhibitor now in clinical development
    • Zhao Y, Yang CY, Wang S. The making of I-BET762, a BET bromodomain inhibitor now in clinical development. J. Med. Chem. 56(19), 7498-7500 (2013).
    • (2013) J. Med. Chem. , vol.56 , Issue.19 , pp. 7498-7500
    • Zhao, Y.1    Yang, C.Y.2    Wang, S.3
  • 28
    • 84889663966 scopus 로고    scopus 로고
    • RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
    • Picaud S, Wells C, Felletar I et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc. Natl Acad. Sci. USA 110 (49), 19754-19759 (2013).
    • (2013) Proc. Natl Acad. Sci. USA , vol.110 , Issue.49 , pp. 19754-19759
    • Picaud, S.1    Wells, C.2    Felletar, I.3
  • 29
    • 84905842525 scopus 로고    scopus 로고
    • A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE defcient mice
    • Jahagirdar R, Zhang H, Azhar S et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE defcient mice. Atherosclerosis 236(1), 91-100 (2014).
    • (2014) Atherosclerosis , vol.236 , Issue.1 , pp. 91-100
    • Jahagirdar, R.1    Zhang, H.2    Azhar, S.3
  • 30
    • 84904538380 scopus 로고    scopus 로고
    • Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression
    • Gacias M, Gerona-Navarro G, Plotnikov AN et al. Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression. Chem. Biol. 21(7), 841-854 (2014).
    • (2014) Chem. Biol. , vol.21 , Issue.7 , pp. 841-854
    • Gacias, M.1    Gerona-Navarro, G.2    Plotnikov, A.N.3
  • 31
    • 84903712622 scopus 로고    scopus 로고
    • BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma
    • Bhadury J, Nilsson LM, Veppil Muralidharan S et al. BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma. Proc. Natl Acad. Sci. USA 111(26), E2721-E2730 (2014).
    • (2014) Proc. Natl Acad. Sci. USA , vol.111 , Issue.26 , pp. E2721-E2730
    • Bhadury, J.1    Nilsson, L.M.2    Veppil Muralidharan, S.3
  • 32
    • 84860832960 scopus 로고    scopus 로고
    • BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain
    • Devaiah BN, Lewis BA, Cherman N et al. BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc. Natl Acad. Sci. USA 109(18), 6927-6932 (2012).
    • (2012) Proc. Natl Acad. Sci. USA , vol.109 , Issue.18 , pp. 6927-6932
    • Devaiah, B.N.1    Lewis, B.A.2    Cherman, N.3
  • 33
    • 84859479811 scopus 로고    scopus 로고
    • Bromodomain protein Brd4 associated with acetylated chromatin is important for maintenance of higher-order chromatin structure
    • Wang R, Li Q, Helfer CM et al. Bromodomain protein Brd4 associated with acetylated chromatin is important for maintenance of higher-order chromatin structure. J. Biol. Chem. 287, 10738-10752 (2012).
    • (2012) J. Biol. Chem. , vol.287 , pp. 10738-10752
    • Wang, R.1    Li, Q.2    Helfer, C.M.3
  • 34
    • 84887940786 scopus 로고    scopus 로고
    • Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains
    • Martin MP, Olesen SH, Georg GI et al. Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chem. Biol. 8(11), 2360-2365 (2013).
    • (2013) ACS Chem. Biol. , vol.8 , Issue.11 , pp. 2360-2365
    • Martin, M.P.1    Olesen, S.H.2    Georg, G.I.3
  • 35
    • 84899936534 scopus 로고    scopus 로고
    • Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors
    • Ember SW, Zhu JY, Olesen SH et al. Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. ACS Chem. Biol. 9(5), 1160-1171 (2014).
    • (2014) ACS Chem. Biol. , vol.9 , Issue.5 , pp. 1160-1171
    • Ember, S.W.1    Zhu, J.Y.2    Olesen, S.H.3
  • 36
    • 84896701144 scopus 로고    scopus 로고
    • The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains
    • Dittmann A, Werner T, Chung CW et al. The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains. ACS Chem. Biol. 9, 495-502 (2014).
    • (2014) ACS Chem. Biol. , vol.9 , pp. 495-502
    • Dittmann, A.1    Werner, T.2    Chung, C.W.3
  • 37
    • 84905269946 scopus 로고    scopus 로고
    • Structure-based virtual screening of novel, high-affnity BRD4 inhibitors
    • Muvva C, Singam ER, Raman SS et al. Structure-based virtual screening of novel, high-affnity BRD4 inhibitors. Mol. Biosyst. 10(9), 2384-2397 (2014).
    • (2014) Mol. Biosyst. , vol.10 , Issue.9 , pp. 2384-2397
    • Muvva, C.1    Singam, E.R.2    Raman, S.S.3
  • 38
    • 84903133687 scopus 로고    scopus 로고
    • Role of transcription factor acetylation in diabetic kidney disease
    • Liu R, Zhong Y, Li X et al. Role of transcription factor acetylation in diabetic kidney disease. Diabetes 63(7), 2440-2453 (2014).
    • (2014) Diabetes , vol.63 , Issue.7 , pp. 2440-2453
    • Liu, R.1    Zhong, Y.2    Li, X.3
  • 39
    • 84921725084 scopus 로고    scopus 로고
    • Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma
    • Epub ahead of print
    • Moros A, Rodríguez V, Saborit-Villarroya I et al. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia doi:10.1038/eu.2014.106 (2014) (Epub ahead of print).
    • (2014) Leukemia
    • Moros, A.1    Rodríguez, V.2    Saborit-Villarroya, I.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.