References
- Waddington CH. Preliminary notes on the development of the wings in normal and mutant strains of Drosophila. Proc Natl Acad Sci USA 1939; 25(7):299-307; PMID:16577903; https://doi.org/10.1073/pnas.25.7.299
- Holliday R. The inheritance of epigenetic defects. Science 1987; 238(4824):163-70; PMID:3310230; https://doi.org/10.1126/science.3310230
- Esteller M. Epigenetics in cancer. N Engl J Med 2008; 358(11):1148-59; PMID:18337604; https://doi.org/10.1056/NEJMra072067
- Kouzarides T. Chromatin modifications and their function. Cell 2007; 128(4):693-705; PMID:17320507; https://doi.org/10.1016/j.cell.2007.02.005
- Berger SL, Kouzarides T, Shiekhattar R, Shilatifard A. An operational definition of epigenetics. Genes Dev 2009; 23(7):781-783; PMID:19339683; https://doi.org/10.1101/gad.1787609
- Shogren-Knaak M, Ishii H, Sun JM, Pazin MJ, Davie JR, Peterson CL. Histone H4-K16 acetylation controls chromatin structure and protein interactions. Science 2006; 311(5762):844-7; PMID:16469925; https://doi.org/10.1126/science.1124000
- Pasqualucci L, Dominguez-Sola D, Chiarenza A, Fabbri G, Grunn A, Trifonov V, Kasper LH, Lerach S, Tang H, Ma J, et al. Inactivating mutations of acetyltransferase genes in B-cell lymphoma. Nature 2011; 471(7337):189-95; PMID:21390126; https://doi.org/10.1038/nature09730
- Gorrini C, Squatrito M, Luise C, Syed N, Perna D, Wark L, Martinato F, Sardella D, Verrecchia A, Bennett S, et al. Tip60 is a haplo-insufficient tumour suppressor required for an oncogene-induced DNA damage response. Nature 2007; 448(7157):1063-7; PMID:17728759; https://doi.org/10.1038/nature06055
- Simo-Riudalbas L, Perez-Salvia M, Setien F, Villanueva A, Moutinho C, Martinez-Cardus A, Moran S, Berdasco M, Gomez A, Vidal E, et al. KAT6B Is a tumor suppressor histone H3 lysine 23 acetyltransferase undergoing genomic loss in small cell lung cancer. Cancer Res 2015; 75(18):3936-45; PMID:26208904; https://doi.org/10.1158/0008-5472.CAN-14-3702
- Bolden JE, Peart MJ, Johnstone RW. Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov 2006; 5(9):769-84; PMID:16955068; https://doi.org/10.1038/nrd2133
- Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H, et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol 2010; 17(5):471-82; PMID:20534345
- Tamkun JW, Deuring R, Scott MP, Kissinger M, Pattatucci AM, Kaufman TC, Kennison JA. brahma: a regulator of Drosophila homeotic genes structurally related to the yeast transcriptional activator SNF2/SWI2. Cell 1992; 68(3):561-72; PMID:1346755; https://doi.org/10.1016/0092-8674(92)90191-E
- Filippakopoulos P, Picaud S, Mangos M, Keates T, Lambert JP, Barsyte-Lovejoy D, Felletar I, Volkmer R, Muller S, Pawson T, et al. Histone recognition and large-scale structural analysis of the human bromodomain family. Cell 2012; 149(1):214-31; PMID:22464331; https://doi.org/10.1016/j.cell.2012.02.013
- Mujtaba S, Zeng L, Zhou MM. Structure and acetyl-lysine recognition of the bromodomain. Oncogene 2007; 26(37):5521-7; PMID:17694091; https://doi.org/10.1038/sj.onc.1210618
- Moriniere J, Rousseaux S, Steuerwald U, Soler-Lopez M, Curtet S, Vitte AL, Govin J, Gaucher J, Sadoul K, Hart DJ, et al. Cooperative binding of two acetylation marks on a histone tail by a single bromodomain. Nature 2009; 461(7264):664-8; PMID:19794495; https://doi.org/10.1038/nature08397
- Filippakopoulos P, Knapp S. The bromodomain interaction module. FEBS Lett 2012; 586(17):2692-704; PMID:22710155; https://doi.org/10.1016/j.febslet.2012.04.045
- Filippakopoulos P, Knapp S. Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov 2014; 13(5):337-56; PMID:24751816; https://doi.org/10.1038/nrd4286
- Yang Z, Yik JH, Chen R, He N, Jang MK, Ozato K, Zhou Q. Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein Brd4. Mol Cell 2005; 19(4):535-45; PMID:16109377; https://doi.org/10.1016/j.molcel.2005.06.029
- Delmore JE, Issa GC, Lemieux ME, Rahl PB, Shi J, Jacobs HM, Kastritis E, Gilpatrick T, Paranal RM, Qi J, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell 146(6):904; PMID:21889194; https://doi.org/10.1016/j.cell.2011.08.017
- Zou Z, Huang B, Wu X, Zhang H, Qi J, Bradner J, Nair S, Chen LF. Brd4 maintains constitutively active NF-kappaB in cancer cells by binding to acetylated RelA. Oncogene 2014; 33(18):2395-404; PMID:23686307; https://doi.org/10.1038/onc.2013.179
- Feng Q, Zhang Z, Shea MJ, Creighton CJ, Coarfa C, Hilsenbeck SG, Lanz R, He B, Wang L, Fu X, et al. An epigenomic approach to therapy for tamoxifen-resistant breast cancer. Cell Res 2014; 24(7):809-19; PMID:24874954; https://doi.org/10.1038/cr.2014.71
- Yang Z, He N, Zhou Q. Brd4 recruits P-TEFb to chromosomes at late mitosis to promote G1 gene expression and cell cycle progression. Mol Cell Biol 2008; 28(3):967-76; PMID:18039861; https://doi.org/10.1128/MCB.01020-07
- Loven J, Hoke HA, Lin CY, Lau A, Orlando DA, Vakoc CR, Bradner JE, Lee TI, Young RA. Selective inhibition of tumor oncogenes by disruption of super-enhancers. Cell 2013; 153(2):320-34; PMID:23582323; https://doi.org/10.1016/j.cell.2013.03.036
- Mohan M, Lin C, Guest E, Shilatifard A. Licensed to elongate: a molecular mechanism for MLL-based leukaemogenesis. Nat Rev Cancer 2010; 10(10):721-8; PMID:20844554; https://doi.org/10.1038/nrc2915
- Hou M, Huang R, Song Y, Feng D, Jiang Y, Liu M. ATAD2 overexpression is associated with progression and prognosis in colorectal cancer. Jpn J Clin Oncol 2016; 46(3):222-7; PMID:26819280; https://doi.org/10.1093/jjco/hyv195
- Zhang M, Zhang C, Du W, Yang X, Chen Z. ATAD2 is overexpressed in gastric cancer and serves as an independent poor prognostic biomarker. Clin Transl Oncol 2016; 18(8):776-81; PMID:26527032; https://doi.org/10.1007/s12094-015-1430-8
- Shang P, Meng F, Liu Y, Chen X. Overexpression of ANCCA/ATAD2 in endometrial carcinoma and its correlation with tumor progression and poor prognosis. Tumour Biol 2015; 36(6):4479-85; PMID:25934333; https://doi.org/10.1007/s13277-015-3089-8
- Zheng L, Li T, Zhang Y, Guo Y, Yao J, Dou L, Guo K. Oncogene ATAD2 promotes cell proliferation, invasion and migration in cervical cancer. Oncol Rep 2015; 33(5):2337-44; PMID:25813398; https://doi.org/10.3892/or.2015.3867
- Wan WN, Zhang YX, Wang XM, Liu YJ, Zhang YQ, Que YH, Zhao WJ. ATAD2 is highly expressed in ovarian carcinomas and indicates poor prognosis. Asian Pacific J Cancer Prev 2014; 15(6):2777-83; PMID:24761900; https://doi.org/10.7314/APJCP.2014.15.6.2777
- Ciro M, Prosperini E, Quarto M, Grazini U, Walfridsson J, McBlane F, Nucifero P, Pacchiana G, Capra M, Christensen J, et al. ATAD2 is a novel cofactor for MYC, overexpressed and amplified in aggressive tumors. Cancer Res 2009; 69(21):8491-8; PMID:19843847; https://doi.org/10.1158/0008-5472.CAN-09-2131
- Zou JX, Guo L, Revenko AS, Tepper CG, Gemo AT, Kung HJ, Chen HW. Androgen-induced coactivator ANCCA mediates specific androgen receptor signaling in prostate cancer. Cancer Res 2009; 69(8):3339-46; PMID:19318566; https://doi.org/10.1158/0008-5472.CAN-08-3440
- Zou JX, Revenko AS, Li LB, Gemo AT, Chen HW. ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ERalpha, is required for coregulator occupancy and chromatin modification. Proc Natl Acad Sci U S A 2007; 104(46):18067-72; PMID:17998543; https://doi.org/10.1073/pnas.0705814104
- Jones MH, Hamana N, Nezu J, Shimane M. A novel family of bromodomain genes. Genomics 2000; 63(1):40-5; PMID:10662543; https://doi.org/10.1006/geno.1999.6071
- Guetg C, Lienemann P, Sirri V, Grummt I, Hernandez-Verdun D, Hottiger MO, Fussenegger M, Santoro R. The NoRC complex mediates the heterochromatin formation and stability of silent rRNA genes and centromeric repeats. EMBO J 2010; 29(13):2135-46; PMID:20168299; https://doi.org/10.1038/emboj.2010.17
- Gu L, Frommel SC, Oakes CC, Simon R, Grupp K, Gerig CY, Bar D, Robinson MD, Baer C, Weiss M, et al. BAZ2A (TIP5) is involved in epigenetic alterations in prostate cancer and its overexpression predicts disease recurrence. Nat Genet 2015; 47(1):22-30; PMID:25485837; https://doi.org/10.1038/ng.3165
- Philpott M, Yang J, Tumber T, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Keates T, Felletar I, Ciulli A, et al. Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery. Mol Biosyst 2011; 7(10):2899-908; PMID:21804994; https://doi.org/10.1039/c1mb05099k
- Schiltz RL, Mizzen CA, Vassilev A, Cook RG, Allis CD, Nakatani Y. Overlapping but distinct patterns of histone acetylation by the human coactivators p300 and PCAF within nucleosomal substrates. J Biol Chem 1999; 274(3):1189-92; PMID:9880483; https://doi.org/10.1074/jbc.274.3.1189
- Kim JY, Lee KS, Seol JE, Yu K, Chakravarti D, Seo SB. Inhibition of p53 acetylation by INHAT subunit SET/TAF-Ibeta represses p53 activity. Nucleic Acids Res 2012; 40(1):75-87; PMID:21911363; https://doi.org/10.1093/nar/gkr614
- Ge X, Jin Q, Zhang F, Yan T, Zhai Q. PCAF acetylates {beta}-catenin and improves its stability. Mol Biol Cell 2009; 20(1):419-27; PMID:18987336; https://doi.org/10.1091/mbc.E08-08-0792
- Perez-Luna M, Aguasca M, Perearnau A, Serratosa J, Martinez-Balbas M, Jesus Pujol M, Bachs O. PCAF regulates the stability of the transcriptional regulator and cyclin-dependent kinase inhibitor p27 Kip1. Nucleic Acids Res 2012; 40(14):6520-33; PMID:22547391; https://doi.org/10.1093/nar/gks343
- Malatesta M, Steinhauer C, Mohammad F, Pandey DP, Squatrito M, Helin K. Histone acetyltransferase PCAF is required for Hedgehog-Gli-dependent transcription and cancer cell proliferation. Cancer Res 2013; 73(20):6323-33; PMID:23943798; https://doi.org/10.1158/0008-5472.CAN-12-4660
- Mujtaba S, He Y, Zeng L, Farooq A, Carlson JE, Ott M, Verdin E, Zhou MM. Structural basis of lysine-acetylated HIV-1 Tat recognition by PCAF bromodomain. Mol Cell 2002; 9(3):575-86; PMID:11931765; https://doi.org/10.1016/S1097-2765(02)00483-5
- Wang Q, Wang R, Zhang B, Zhang S, Zheng Y, Wang Z. Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication. Med Chem Comm 2013; 4(4):737-40; https://doi.org/10.1039/C3MD20376J
- Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Muller S, Siegal G, et al. Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain. J Med Chem 2016; 59(4):1648-53; PMID:26731131; https://doi.org/10.1021/acs.jmedchem.5b01719
- Mujtaba S, He Y, Zeng L, Yan S, Plotnikova O, Sachchidanand Sanchez R, Zeleznik-Le NJ, Ronai Z, Zhou MM. Structural mechanism of the bromodomain of the coactivator CBP in p53 transcriptional activation. Mol Cell 2004; 13(2):251-63; PMID:14759370; https://doi.org/10.1016/S1097-2765(03)00528-8
- Dancy BM, Cole PA. Protein lysine acetylation by p300/CBP. Chem Rev 2015; 115(6):2419-52; PMID:25594381; https://doi.org/10.1021/cr500452k
- Ogryzko VV, Schiltz RL, Russanova V, Howard BH, Nakatani Y. The transcriptional coactivators p300 and CBP are histone acetyltransferases. Cell 1996; 87(5):953-9; PMID:8945521; https://doi.org/10.1016/S0092-8674(00)82001-2
- Iyer NG, Ozdag H, Caldas C. p300/CBP and cancer. Oncogene 2004; 23(24):4225-31; PMID:15156177; https://doi.org/10.1038/sj.onc.1207118
- Arif M, Pradhan SK, Thanuja GR, Vedamurthy BM, Agrawal S, Dasgupta D, Kundu TK. Mechanism of p300 specific histone acetyltransferase inhibition by small molecules. J Med Chem 2009; 52(2):267-77; PMID:19086895; https://doi.org/10.1021/jm800657z
- Hohmann AF, Martin LJ, Minder JL, Roe JS, Shi J, Steurer S, Bader G, McConnell D, Pearson M, Gerstberger T, et al. Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition. Nat Chem Biol 2016; 12(9):672-9; PMID:27376689; https://doi.org/10.1038/nchembio.2115
- Yu X, Li Z, Shen J. BRD7: a novel tumor suppressor gene in different cancers. Am J Transl Res 2016; 8(2):742-8; PMID:27158366
- Wu WJ, Hu KS, Chen DL, Zeng ZL, Luo HY, Wang F, Wang DS, Wang ZQ, He F, Xu RH. Prognostic relevance of BRD7 expression in colorectal carcinoma. Eur J Clin Invest 2013; 43(2):131-40; PMID:23215825; https://doi.org/10.1111/eci.12024
- Park YA, Lee JW, Kim HS, Lee YY, Kim TJ, Choi CH, Choi JJ, Jeon HK, Cho YJ, Ryu JY, et al. Tumor suppressive effects of bromodomain-containing protein 7 (BRD7) in epithelial ovarian carcinoma. Clin Cancer Res 2014; 20(3):565-75; PMID:24198243; https://doi.org/10.1158/1078-0432.CCR-13-1271
- Chen CL, Wang Y, Pan QZ, Tang Y, Wang QJ, Pan K, Huang LX, He J, Zhao JJ, Jiang SS, et al. Bromodomain-containing protein 7 (BRD7) as a potential tumor suppressor in hepatocellular carcinoma. Oncotarget 2016; 7(13):16248-61; PMID:26919247; https://doi.org/10.18632/oncotarget.7637
- Li D, Yang Y, Zhu G, Liu X, Zhao M, Li X, Yang Q. MicroRNA-410 promotes cell proliferation by targeting BRD7 in non-small cell lung cancer. FEBS Lett 2015; 589(17):2218-23; PMID:26149213; https://doi.org/10.1016/j.febslet.2015.06.031
- Park YA, Lee JW, Choi JJ, Jeon HK, Cho Y, Choi C, Kim TJ, Lee NW, Kim BG, Bae DS. The interactions between MicroRNA-200c and BRD7 in endometrial carcinoma. Gynecol Oncol 2012; 124(1):125-33; PMID:22015043; https://doi.org/10.1016/j.ygyno.2011.09.026
- Harte MT, O'Brien GJ, Ryan NM, Gorski JJ, Savage KI, Crawford NT, Mullan PB, Harkin DP. BRD7, a subunit of SWI/SNF complexes, binds directly to BRCA1 and regulates BRCA1-dependent transcription. Cancer Res 2010; 70(6):2538-47; PMID:20215511; https://doi.org/10.1158/0008-5472.CAN-09-2089
- Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, et al. Selective inhibition of BET bromodomains. Nature 2010; 468(7327):1067-73; PMID:20871596; https://doi.org/10.1038/nature09504
- Nicodeme E, Jeffrey KL, Schaefer U, Beinke S, Dewell S, Chung CW, Chandwani R, Marazzi I, Wilson P, Coste H, et al. Suppression of inflammation by a synthetic histone mimic. Nature 2010; 468(7327):1119-23; PMID:21068722; https://doi.org/10.1038/nature09589
- Mirguet O, Gosmini R, Toum J, Clement CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes RM, Crowe M, Pineau O, et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem 2013; 56(19):7501-15; PMID:24015967; https://doi.org/10.1021/jm401088k
- French CA, Ramirez CL, Kolmakova J, Hickman TT, Cameron MJ, Thyne ME, Kutok JL, Toretsky JA, Tadavarthy AK, Kees UR, et al. BRD-NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells. Oncogene 2008; 27(15):2237-42; PMID:17934517; https://doi.org/10.1038/sj.onc.1210852
- Zuber J, Shi J, Wang E, Rappaport AR, Herrmann H, Sison EA, Magoon D, Qi J, Blatt K, Wunderlich M, et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature 2011; 478(7370):524-8; PMID:21814200; https://doi.org/10.1038/nature10334
- Mertz JA, Conery AR, Bryant BM, Sandy P, Balasubramanian S, Mele DA, Bergeron L, Sims RJ, 3rd. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci U S A 2011; 108(40):16669-74; PMID:21949397; https://doi.org/10.1073/pnas.1108190108
- Soodgupta D, Pan D, Cui G, Senpan A, Yang X, Lu L, Weilbaecher KN, Prochownik EV, Lanza GM, Tomasson MH. Small molecule MYC inhibitor conjugated to integrin-targeted nanoparticles extends survival in a mouse model of disseminated multiple myeloma. Mol Cancer Ther 2015; 14(6):1286-94; PMID:25824336; https://doi.org/10.1158/1535-7163.MCT-14-0774-T
- Ott CJ, Kopp N, Bird L, Paranal RM, Qi J, Bowman T, Rodig SJ, Kung AL, Bradner JE, Weinstock DM. BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. Blood 2012; 120(14):2843-52; PMID:22904298; https://doi.org/10.1182/blood-2012-02-413021
- Chapuy B, McKeown MR, Lin CY, Monti S, Roemer MG, Qi J, Rahl PB, Sun HH, Yeda KT, Doench JG, et al. Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma. Cancer Cell 2013; 24(6):777-90; PMID:24332044; https://doi.org/10.1016/j.ccr.2013.11.003
- Cheng Z, Gong Y, Ma Y, Lu K, Lu X, Pierce LA, Thompson RC, Muller S, Knapp S, Wang J. Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clin Cancer Res 2013; 19(7):1748-59; PMID:23403638; https://doi.org/10.1158/1078-0432.CCR-12-3066
- Liu F, Hon GC, Villa GR, Turner KM, Ikegami S, Yang H, Ye Z, Li B, Kuan S, Lee AY, et al. EGFR Mutation promotes glioblastoma through epigenome and transcription factor network remodeling. Mol Cell 2015; 60(2):307-18; PMID:26455392; https://doi.org/10.1016/j.molcel.2015.09.002
- Bandopadhayay P, Bergthold G, Nguyen B, Schubert S, Gholamin S, Tang Y, Bolin S, Schumacher SE, Zeid R, Masoud S, et al. BET bromodomain inhibition of MYC-amplified medulloblastoma. Clin Cancer Res 2014; 20(4):912-25; PMID:24297863; https://doi.org/10.1158/1078-0432.CCR-13-2281
- Henssen A, Thor T, Odersky A, Heukamp L, El-Hindy N, Beckers A, Speleman F, Althoff K, Schafers S, Schramm A, et al. BET bromodomain protein inhibition is a therapeutic option for medulloblastoma. Oncotarget 2013; 4(11):2080-95; PMID:24231268; https://doi.org/10.18632/oncotarget.1534
- Venkataraman S, Alimova I, Balakrishnan I, Harris P, Birks DK, Griesinger A, Amani V, Cristiano B, Remke M, Taylor MD, et al. Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma. Oncotarget 2014; 5(9):2355-71; PMID:24796395; https://doi.org/10.18632/oncotarget.1659
- Li GQ, Guo WZ, Zhang Y, Seng JJ, Zhang HP, Ma XX, Zhang G, Li J, Yan B, Tang HW, et al. Suppression of BRD4 inhibits human hepatocellular carcinoma by repressing MYC and enhancing BIM expression. Oncotarget 2016; 7(3):2462-74; PMID:26575167; https://doi.org/10.18632/oncotarget.6275
- Hong SH, Eun JW, Choi SK, Shen Q, Choi WS, Han JW, Nam SW, You JS. Epigenetic reader BRD4 inhibition as a therapeutic strategy to suppress E2F2-cell cycle regulation circuit in liver cancer. Oncotarget 2016; 7(22):32628-40; PMID:27081696; https://doi.org/10.18632/oncotarget.8701
- McCleland ML, Mesh K, Lorenzana E, Chopra VS, Segal E, Watanabe C, Haley B, Mayba O, Yaylaoglu M, Gnad F, et al. CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest 2016; 126(2):639-52; PMID:26752646; https://doi.org/10.1172/JCI83265
- Zhang L, Tong Y, Zhang X, Pan M, Chen S. Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth. Drug Des Devel Ther 2015; 9:5851-62; https://doi.org/10.2147/DDDT.S92943
- Garcia PL, Miller AL, Kreitzburg KM, Council LN, Gamblin TL, Christein JD, Heslin MJ, Arnoletti JP, Richardson JH, Chen D, et al. The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models. Oncogene 2016; 35(7):833-45; PMID:25961927; https://doi.org/10.1038/onc.2015.126
- Mazur PK, Herner A, Mello SS, Wirth M, Hausmann S, Sanchez-Rivera FJ, Lofgren SM, Kuschma T, Hahn SA, Vangala D, et al. Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma. Nat Med 2015; 21(10):1163-71; PMID:26390243; https://doi.org/10.1038/nm.3952
- Kumar K, Raza SS, Knab LM, Chow CR, Kwok B, Bentrem DJ, Popovic R, Ebine K, Licht JD, Munshi HG. GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1. Sci Rep 2015; 5:9489; PMID:25807524; https://doi.org/10.1038/srep09489
- Klocker H, Culig Z, Kaspar F, Hobisch A, Eberle J, Reissigl A Bartsch G. Androgen signal transduction and prostatic carcinoma. World J Urol 1994; 12(2):99-103; PMID:8087144; https://doi.org/10.1007/BF00184245
- Asangani IA, Dommeti VL, Wang X, Malik R, Cieslik M, Yang R, Escara-Wilke J, Wilder-Romans K, Dhanireddy S, Engelke C, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature 2014; 510(7504):278-82; PMID:24759320; https://doi.org/10.1038/nature13229
- Chan SC, Selth LA, Li Y, Nyquist MD, Miao L, Bradner JE, Raj GV, Tilley WD, Dehm SM. Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies. Nucleic Acids Res 2015; 43(12):5880-97; PMID:25908785; https://doi.org/10.1093/nar/gkv262
- Blee AM, Liu S, Wang L, Huang H. BET bromodomain-mediated interaction between ERG and BRD4 promotes prostate cancer cell invasion. Oncotarget 2016; 7(25):38319-32; PMID:27223260; https://doi.org/10.18632/oncotarget.9513
- Lockwood WW, Zejnullahu K, Bradner JE, Varmus H. Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins. Proc Natl Acad Sci U S A 2012; 109(47):19408-13; PMID:23129625; https://doi.org/10.1073/pnas.1216363109
- Shimamura T, Chen Z, Soucheray M, Carretero J, Kikuchi E, Tchaicha JH, Gao Y, Cheng KA, Cohoon TJ, Qi J, et al. Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer. Clin Cancer Res 2013; 19(22):6183-92; PMID:24045185; https://doi.org/10.1158/1078-0432.CCR-12-3904
- Tsai LH, Wu JY, Cheng YW, Chen CY, Sheu GT, Wu TC, Lee H. The MZF1/c-MYC axis mediates lung adenocarcinoma progression caused by wild-type lkb1 loss. Oncogene 2015; 34(13):1641-9; PMID:24793789; https://doi.org/10.1038/onc.2014.118
- Peifer M, Fernandez-Cuesta L, Sos ML, George J, Seidel D, Kasper LH, Plenker D, Leenders F, Sun R, Zander T, et al. Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer. Nat Genet 2012; 44(10):1104-10; PMID:22941188; https://doi.org/10.1038/ng.2396
- Lenhart R, Kirov S, Desilva H, Cao J, Lei M, Johnston K, Peterson R, Schweizer L, Purandare A, Ross-Macdonald P, et al. Sensitivity of small cell lung cancer to BET inhibition Is mediated by regulation of ASCL1 gene expression. Mol Cancer Ther 2015; 14(10):2167-74; PMID:26253517; https://doi.org/10.1158/1535-7163.MCT-15-0037
- Clarke R, Liu MC, Bouker KB, Gu Z, Lee RY, Zhu Y, Skaar TC, Gomez B, O'Brien K, Wang Y, et al. Antiestrogen resistance in breast cancer and the role of estrogen receptor signaling. Oncogene 2003; 22(47):7316-39; PMID:14576841; https://doi.org/10.1038/sj.onc.1206937
- Sengupta S, Biarnes MC, Clarke R, Jordan VC. Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement. Breast Cancer Res Treat 2015; 150(2):265-78; PMID:25721606; https://doi.org/10.1007/s10549-015-3319-1
- Bihani T, Ezell SA, Ladd B, Grosskurth SE, Mazzola AM, Pietras M, Reimer C, Zinda M, Fawell S, D'Cruz CM. Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers. Oncotarget 2015; 6(4):2407-20; PMID:25537515; https://doi.org/10.18632/oncotarget.2964
- Borbely G, Haldosen LA, Dahlman-Wright K, Zhao C. Induction of USP17 by combining BET and HDAC inhibitors in breast cancer cells. Oncotarget 2015; 6(32):33623-35; PMID:26378038; https://doi.org/10.18632/oncotarget.5601
- Shu S, Lin CY, He HH, Witwicki RM, Tabassum DP, Roberts JM, Janiszewska M, Huh SJ, Liang Y, Ryan J, et al. Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer. Nature 2016; 529(7586):413-7; PMID:26735014; https://doi.org/10.1038/nature16508
- Perez-Pena J, Serrano-Heras G, Montero JC, Corrales-Sanchez V, Pandiella A, Ocana A. In silico analysis guides selection of BET inhibitors for triple-negative breast cancer treatment. Mol Cancer Ther 2016; 15(8):1823-33; PMID:27256375; https://doi.org/10.1158/1535-7163.MCT-16-0004
- da Motta LL, Ledaki I, Purshouse K, Haider S, De Bastiani MA, Baban D, Morotti M, Steers G, Wigfield S, Bridges E, et al. The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer. Oncogene 2016; PMID:27292261; https://doi.org/10.1038/onc.2016.184 Oncogene 2016:1-11
- Bernardi R, Gianni L. Hallmarks of triple negative breast cancer emerging at last? Cell Res 2014; 24(8):904-5; PMID:24810303; https://doi.org/10.1038/cr.2014.61
- Chaidos A, Caputo V, Gouvedenou K, Liu B, Marigo I, Chaudhry MS, Rotolo A, Tough DF, Smithers NN, Bassil AK, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood 2014; 123(5):697-705; PMID:24335499; https://doi.org/10.1182/blood-2013-01-478420
- Wyce A, Degenhardt Y, Bai Y, Le B, Korenchuk S, Crouthame MC, McHugh CF, Vessella R, Creasy CL, Tummino PJ, et al. Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer. Oncotarget 2013; 4(12):2419-29; PMID:24293458; https://doi.org/10.18632/oncotarget.1572
- Berenguer-Daize C, Astorgues-Xerri L, Odore E, Cayol M, Cvitkovic E, Noel K, Bekradda M, MacKenzie S, Rezai K, Lokiec F, et al. OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models. Int J Cancer 2016; 139(9):2047-55; PMID:27388964; https://doi.org/10.1002/ijc.30256
- Coude MM, Braun T, Berrou J, Dupont M, Bertrand S, Masse A, Raffoux E, Itzykson R, Delord M, Riveiro ME, et al. BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget 2015; 6(19):17698-712; PMID:25989842; https://doi.org/10.18632/oncotarget.4131
- Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 2011; 478(7370):529-33; PMID:21964340; https://doi.org/10.1038/nature10509
- Wyspianska BS, Bannister AJ, Barbieri I, Nangalia J, Godfrey A, Calero-Nieto FJ, Robson S, Rioja I, Li J, Wiese M, et al. BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms. Leukemia 2014; 28(1):88-97; PMID:23929215; https://doi.org/10.1038/leu.2013.234
- Pastori C, Daniel M, Penas C, Volmar CH, Johnstone AL, Brothers SP, Graham RM, Allen B, Sarkaria JN, Komotar RJ, et al. BET bromodomain proteins are required for glioblastoma cell proliferation. Epigenetics 2014; 9(4):611-20; PMID:24496381; https://doi.org/10.4161/epi.27906
- Dawson MA, Gudgin EJ, Horton SJ, Giotopoulos G, Meduri E, Robson S, Cannizzaro E, Osaki H, Wiese M, Putwain S, et al. Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia. Leukemia 2014; 28(2):311-20; PMID:24220271; https://doi.org/10.1038/leu.2013.338
- Gallagher SJ, Mijatov B, Gunatilake D, Tiffen JC, Gowrishankar K, Jin L, Pupo GM, Cullinane C, Prinjha RK, Smithers N, et al. The epigenetic regulator I-BET151 induces BIM-dependent apoptosis and cell cycle arrest of human melanoma cells. J Invest Dermatol 2014; 134(11):2795-805; PMID:24906137; https://doi.org/10.1038/jid.2014.243
- Gallagher SJ, Mijatov B, Gunatilake D, Gowrishankar K, Tiffen J, James W, Jin L, Pupo G, Cullinane C, McArthur GA, et al. Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151. Pigment Cell Melanoma Res 2014; 27(6):1126-37; PMID:24924589; https://doi.org/10.1111/pcmr.12282
- Siegel MB, Liu SQ, Davare MA, Spurgeon SE, Loriaux MM, Druker BJ, Scott EC, Tyner JW. Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma. Oncotarget 2015; 6(22):18921-32; PMID:26254279; https://doi.org/10.18632/oncotarget.4214
- Wong C, Laddha SV, Tang L, Vosburgh E, Levine AJ, Normant E, Sandy P, Harris CR, Chan CS, Xu EY. The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. Cell Death Dis 2014; 5:e1450; PMID:25299775; https://doi.org/10.1038/cddis.2014.396
- Moros A, Rodriguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martinez A, Wiestner A, Normant E, Campo E, et al. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia 2014; 28(10):2049-59; PMID:24721791; https://doi.org/10.1038/leu.2014.106
- Bhadury J, Nilsson LM, Muralidharan SV, Green LC, Li Z, Gesner EM, Hansen HC, Keller UB, McLure KG, Nilsson JA. BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma. Proc Natl Acad Sci U S A 2014; 111(26):E2721-30; PMID:24979794; https://doi.org/10.1073/pnas.1406722111
- Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, et al. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res 2013; 73(11):3336-46; PMID:23576556; https://doi.org/10.1158/0008-5472.CAN-12-3292
- Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem 2013; 56(22):9251-64; PMID:24144283; https://doi.org/10.1021/jm401334s
- Millan DS, Alvarez Morales MA, Barr KJ, Cardillo D, Collis A, Dinsmore CJ, Escobedo JA, Foley KP, Herbertz T, Hubbs S, et al. FT-1101: A structurally distinct pan-BET bromodomain inhibitor with activity in preclinical models of hematologic malignancies. Poster presented at: 57th Annual Meeting & Exposition of American Society of Hematology (ASH); 2015 Dec 5–8; Orlando, USA
- Albrecht BK, Gehling VS, Hewitt MC, Vaswani RG, Cote A, Leblanc Y, Nasveschuk CG, Bellon S, Bergeron L, Campbell R, et al. Identification of a benzoisoxazoloazepine inhibitor (CPI-0610) of the bromodomain and extra-terminal (BET) family as a candidate for human clinical trials. J Med Chem 2016; 59(4):1330-9; PMID:26815195; https://doi.org/10.1021/acs.jmedchem.5b01882
- Lejeune P, Sugawara T, Gelato KA, Ellinger-Ziegelbauer H, Fernandez-Montalvan AE, Schmees N, Siegel S, Weinmann H, Gekeler V, Walter AO, et al. BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models. Poster presented at: 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18–22; Philadelphia, USA. https://doi.org/10.1158/1538-7445.AM2015-3524
- Liu PCC, Liu XM, Stubbs MC, Maduskuie T, Sparks R, Zolotarjova N, Li J, Wen X, Favata M, Feldman P, et al. Discovery of a novel BET inhibitor INCB054329. Poster presented at: 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18–22; Philadelphia, USA. https://doi.org/10.1158/1538-7445.AM2015-3523
- Shapiro GI, Dowlati A, LoRusso P, Eder JP, Anderson A, Do KT, Kagey MH, Sirard C, Bradner JE, Landau SB. Clinically efficacy of the BET bromodomain inhibitor TEN-010 in an open-label substudy with patients with documented NUT-midline carcinoma (NMC). Poster presented at: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2015 Nov 5–9; Boston, USA. https://doi.org/10.1158/1535-7163.TARG-15-A49
- Structural Genomics Consortium (SGC). BAY-299 A probe for BRD1 and TAF1 [Accessed 2016, Sept 7]. http://www.thesgc.org/chemical-probes/BAY-299
- Structural Genomics Consortium (SGC). Bromosporine [Accessed 2016, Sept 6]. http://www.thesgc.org/chemical-probes/Bromosporine
- Vidler LR, Brown N, Knapp S, Hoelder S. Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. J Med Chem 2012; 55(17):7346-59; PMID:22788793; https://doi.org/10.1021/jm300346w
- Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H, et al. Fragment-based discovery of low-micromolar ATAD2 bromodomain inhibitors. J Med Chem 2015; 58(14):5649-73; PMID:26155854; https://doi.org/10.1021/acs.jmedchem.5b00772
- Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, et al. Structure-based optimization of naphthyridones into potent ATAD2 bromodomain inhibitors. J Med Chem 2015; 58(15):6151-78; PMID:26230603; https://doi.org/10.1021/acs.jmedchem.5b00773
- Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, et al. Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B. J Med Chem 2015; 58(5):2553-9; PMID:25719566; https://doi.org/10.1021/jm501963e
- Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, et al. Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B. J Med Chem 2016; 59(4):1410-24; PMID:25799074; https://doi.org/10.1021/acs.jmedchem.5b00209
- Middeljans E, Wan X, Jansen PW, Sharma V, Stunnenberg HG, Logie C. SS18 together with animal-specific factors defines human BAF-type SWI/SNF complexes. PLoS One 2012; 7(3):e33834; PMID:22442726; https://doi.org/10.1371/journal.pone.0033834
- Picaud S, Strocchia M, Terracciano S, Lauro G, Mendez J, Daniels DL, Riccio R, Bifulco G, Bruno I, Filippakopoulos P. 9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain. J Med Chem 2015; 58(6):2718-36; PMID:25703523; https://doi.org/10.1021/jm501893k
- Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, et al. Discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition. J Med Chem 2016; 59(4):1425-39; PMID:25856009; https://doi.org/10.1021/acs.jmedchem.5b00256
- Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Muller S, et al. LP99: Discovery and synthesis of the first selective BRD7/9 bromodomain inhibitor. Angew Chem Weinheim Bergstr Ger 2015; 127(21):6315-9; PMID:27346896; https://doi.org/10.1002/ange.201501394
- Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, et al. Structure-based design of an in vivo active selective BRD9 inhibitor. J Med Chem 2016; 59(10):4462-75; PMID:26914985; https://doi.org/10.1021/acs.jmedchem.5b01865
- Structural Genomics Consortium (SGC). TP-472 A BRD9/7 Probe [Accessed 2016, Sept 6]. http://www.thesgc.org/chemical-probes/TP-472
- Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, et al. 1,3-dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med Chem Lett 2014; 5(11):1190-5; PMID:25408830; https://doi.org/10.1021/ml5002932
- Structural Genomics Consortium (SGC). OF-1 A chemical probe for BRPF bromodomains [Accessed 2016, Sept 6]. http://www.thesgc.org/chemical-probes/OF-1
- Structural Genomics Consortium (SGC). PFI-4 A chemical probe for BRPF1B [Accessed 2016, Sept 7]. http://www.thesgc.org/chemical-probes/PFI-4
- Structural Genomics Consortium (SGC). NI-57 A chemical probe for BRPF bromodomains [Accessed 2016, Sept 7]. http://www.thesgc.org/chemical-probes/NI-57
- Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, et al. Discovery of a chemical tool inhibitor targeting the bromodomains of TRIM24 and BRPF. J Med Chem 2016; 59(4):1642-7; PMID:25974391; https://doi.org/10.1021/acs.jmedchem.5b00458
- Medina PP, Romero OA, Kohno T, Montuenga LM, Pio R, Yokota J, Sanchez-Cespedes M. Frequent BRG1/SMARCA4-inactivating mutations in human lung cancer cell lines. Hum Mutat 2008; 29(5):617-22; PMID:18386774; https://doi.org/10.1002/humu.20730
- Brownlee PM, Chambers AL, Oliver AW, Downs JA. Cancer and the bromodomains of BAF180. Biochem Soc Trans 2012; 40(2):364-9; PMID:22435813; https://doi.org/10.1042/BST20110754
- Kwon SJ, Lee SK, Na J, Lee SA, Lee HS, Park JH, Chung JK, Youn H, Kwon J. Targeting BRG1 chromatin remodeler via its bromodomain for enhanced tumor cell radiosensitivity in vitro and in vivo. Mol Cancer Ther 2015; 14(2):597-607; PMID:25504753; https://doi.org/10.1158/1535-7163.MCT-14-0372
- Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, et al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance. Sci Adv 2015;1(10):e1500723; PMID:26702435; https://doi.org/10.1126/sciadv.1500723
- Structural Genomics Consortium (SGC). PFI-3 A selective chemical probe for SMARCA bromodomains [Accessed 2016, Sept 6]: http://www.thesgc.org/chemical-probes/PFI-3
- Vangamudi B, Paul TA, Shah PK, Kost-Alimova M, Nottebaum L, Shi X, Zhan Y, Leo E, Mahadeshwar HS, Protopopov A, et al. The SMARCA2/4 ATPase domain surpasses the bromodomain as a drug target in SWI/SNF-mutant cancers: insights from cDNA rescue and PFI-3 inhibitor studies. Cancer Res 2015; 75(18):3865-78; PMID:26139243; https://doi.org/10.1158/0008-5472.CAN-14-3798
- Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Muller S, Knapp S, Brenton JD, et al. Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the switch/sucrose nonfermenting complex. J Med Chem 2016; 59(10):5095-101; PMID:27119626; https://doi.org/10.1021/acs.jmedchem.5b01997
- Sachchidanand , Resnick-Silverman L, Yan S, Mutjaba S, Liu WJ, Zeng L, Manfredi JJ, Zhou MM. Target structure-based discovery of small molecules that block human p53 and CREB binding protein association. Chem Biol 2006; 13(1):81-90; PMID:16426974; https://doi.org/10.1016/j.chembiol.2005.10.014
- Borah JC, Mujtaba S, Karakikes I, Zeng L, Muller M, Patel J, Moshkina N, Morohashi K, Zhang W, Gerona-Navarro G, et al. A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. Chem Biol 2011; 18(4):531-41; PMID:21513889; https://doi.org/10.1016/j.chembiol.2010.12.021
- Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, et al. Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy. Cancer Res 2015; 75(23):5106-19; PMID:26552700; https://doi.org/10.1158/0008-5472.CAN-15-0236
- Zucconi BE, Luef B, Xu W, Henry RA, Nodelman IM, Bowman GD, Andrews AJ, Cole PA. Modulation of p300/CBP acetylation of nucleosomes by bromodomain ligand I-CBP112. Biochemistry 2016; 55(27):3727-34; PMID:27332697; https://doi.org/10.1021/acs.biochem.6b00480
- Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J Am Chem Soc 2014; 136(26):9308-19; PMID:24946055; https://doi.org/10.1021/ja412434f
- Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, et al. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc Natl Acad Sci U S A 2015; 112(34):10768-73; PMID:26261308; https://doi.org/10.1073/pnas.1501956112
- Conery AR, Centore RC, Neiss A, Keller PJ, Joshi S, Spillane KL, Sandy P, Hatton C, Pardo E, Zawadzke L, et al. Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma. Elife 2016; 5:pii:e10483; PMID:26731516; https://doi.org/10.7554/eLife.10483
- Chekler EL, Pellegrino JA, Lanz TA, Denny RA, Flick AC, Coe J, Langille J, Basak A, Liu S, Stock IA, et al. Transcriptional profiling of a selective CREB binding protein bromodomain inhibitor highlights therapeutic opportunities. Chem Biol 2015; 22(12):1588-96; PMID:26670081; https://doi.org/10.1016/j.chembiol.2015.10.013
- Taylor AM, Cote A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, et al. Fragment-based discovery of a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor (CPI-637). ACS Med Chem Lett 2016; 7(5):531-6; PMID:27190605; https://doi.org/10.1021/acsmedchemlett.6b00075
- Denis GV. Bromodomain coactivators in cancer, obesity, type 2 diabetes, and inflammation. Discov Med 2010; 10(55):489-99; PMID:21189220
- Nicholas DA, Andrieu G, Strissel KJ, Nikolajczyk BS Denis GV. BET bromodomain proteins and epigenetic regulation of inflammation: implications for type 2 diabetes and breast cancer. Cell Mol Life Sci 2016; PMID:27491296; https://doi.org/10.1007/s00018-016-2320-0
- Rvx 208. Drugs R D 2011; 11(2):207-13; PMID:21679009; https://doi.org/10.2165/11595140-000000000-00000
- Nicholls SJ, Puri R, Wolski K, Ballantyne CM, Barter PJ, Brewer HB, Kastelein JJ, Hu B, Uno K, Kataoka Y, et al. Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial. Am J Cardiovasc Drugs 2016; 16(1):55-65; PMID:26385396; https://doi.org/10.1007/s40256-015-0146-z
- ClinicaTrials. gov. [Accessed 2016, Nov 9]. https://clinicaltrials.gov/">https://clinicaltrials.gov/">https://clinicaltrials.gov/
- Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A 2013; 110(49):19754-9; PMID:24248379; https://doi.org/10.1073/pnas.1310658110
- Bailey D, Jahagirdar R, Gordon A, Hafiane A, Campbell S, Chatur S, Wagner GS, Hansen HC, Chiacchia FS, Johansson J, et al. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol 2010; 55(23):2580-9; PMID:20513599; https://doi.org/10.1016/j.jacc.2010.02.035
- Gilham D, Wasiak S, Tsujikawa LM, Halliday C, Norek K, Patel RG, Kulikowski E, Johansson J, Sweeney M, Wong NC. RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease. Atherosclerosis 2016; 247:48-57; PMID:26868508; https://doi.org/10.1016/j.atherosclerosis.2016.01.036
- Siebel AL, Trinh SK, Formosa MF, Mundra PA, Natoli AK, Reddy-Luthmoodoo M, Huynh K, Khan AA, Carey AL, van Hall G, et al. Effects of the BET-inhibitor, RVX-208 on the HDL lipidome and glucose metabolism in individuals with prediabetes: A randomized controlled trial. Metabolism 2016; 65(6):904-14; PMID:27173469; https://doi.org/10.1016/j.metabol.2016.03.002
- Fu W, Farache J, Clardy SM, Hattori K, Mander P, Lee K, Rioja I, Weissleder R, Prinjha RK, Benoist C, et al. Epigenetic modulation of type-1 diabetes via a dual effect on pancreatic macrophages and beta cells. Elife 2014; 3:e04631; PMID:25407682; https://doi.org/10.7554/eLife.04631
- Deeney JT, Belkina AC, Shirihai OS, Corkey BE Denis GV. BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic beta-Cell. PLoS One 2016; 11(3):e0151329; PMID:27008626; https://doi.org/10.1371/journal.pone.0151329
- Nadeem A, Al-Harbi NO, Al-Harbi MM, El-Sherbeeny AM, Ahmad SF, Siddiqui N, Ansari MA, Zoheir KM, Attia SM, Al-Hosaini KA, et al. Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation. Pharmacol Res 2015; 99:248-57; PMID:26149470; https://doi.org/10.1016/j.phrs.2015.06.001
- Xiao Y, Liang L, Huang M, Qiu Q, Zeng S, Shi M, Zou Y, Ye Y, Yang X, Xu H. Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IkappaB kinase-dependent NF-kappaB activation in rheumatoid fibroblast-like synoviocytes. Rheumatology (Oxford) 2016; 55(1):173-84; PMID:26324948; https://doi.org/10.1093/rheumatology/kev312
- Klein K, Kabala PA, Grabiec AM, Gay RE, Kolling C, Lin LL, Gay S, Tak PP, Prinjha RK, Ospelt C, et al. The bromodomain protein inhibitor I-BET151 suppresses expression of inflammatory genes and matrix degrading enzymes in rheumatoid arthritis synovial fibroblasts. Ann Rheum Dis 2016; 75(2):422-9; PMID:25467295; https://doi.org/10.1136/annrheumdis-2014-205809
- Barrett E, Brothers S, Wahlestedt C Beurel E. I-BET151 selectively regulates IL-6 production. Biochim Biophys Acta 2014; 1842(9):1549-55; PMID:24859008; https://doi.org/10.1016/j.bbadis.2014.05.013
- Huang M, Zeng S, Zou Y, Shi M, Qiu Q, Xiao Y, Chen G, Yang X, Liang L, Xu H. BET bromodomain suppression inhibits vascular inflammation by blocking NF-kappaB and MAPK activation. Br J Pharmacol 2016; 174(1):101-115; PMID:27774624; https://doi.org/10.1111/bph.13657
- Balasubramanyam K, Swaminathan V, Ranganathan A, Kundu TK. Small molecule modulators of histone acetyltransferase p300. The Journal of biological chemistry 2003; 278(21):19134-40; PMID:12624111; https://doi.org/10.1074/jbc.M301580200
- Milite C, Castellano S, Benedetti R, Tosco A, Ciliberti C, Vicidomini C, Boully L, Franci G, Altucci L, Mai A, et al. Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs). Bioorg Med Chem 2011; 19(12):3690-701; PMID:21292492; https://doi.org/10.1016/j.bmc.2011.01.013
- Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A. Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases. Bioorg Med Chem Lett 2008; 18(9):2788-92; PMID:18434144; https://doi.org/10.1016/j.bmcl.2008.04.017
- Castellano S, Milite C, Feoli A, Viviano M, Mai A, Novellino E, Tosco A, Sbardella G. 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 2015; 10(1):144-57; PMID:25333655; https://doi.org/10.1002/cmdc.201402371
- Wei W, Coelho CM, Li X, Marek R, Yan S, Anderson S, Meyers D, Mukherjee C, Sbardella G, Castellano S, et al. p300/CBP-associated factor selectively regulates the extinction of conditioned fear. J Neurosci 2012; 32(35):11930-41; PMID:22933779; https://doi.org/10.1523/JNEUROSCI.0178-12.2012
- Colussi C, Scopece A, Vitale S, Spallotta F, Mattiussi S, Rosati J, Illi B, Mai A, Castellano S, Sbardella G, et al. P300/CBP associated factor regulates nitroglycerin-dependent arterial relaxation by N(epsilon)-lysine acetylation of contractile proteins. Arterioscler Thromb Vasc Biol 2012; 32(10):2435-43; PMID:22859492; https://doi.org/10.1161/ATVBAHA.112.254011
- Colussi C, Rosati J, Straino S, Spallotta F, Berni R, Stilli D, Rossi S, Musso E, Macchi E, Mai A, et al. Nepsilon-lysine acetylation determines dissociation from GAP junctions and lateralization of connexin 43 in normal and dystrophic heart. Proc Natl Acad Sci U S A 2011; 108(7):2795-800; PMID:21282606; https://doi.org/10.1073/pnas.1013124108
- Vecellio M, Spallotta F, Nanni S, Colussi C, Cencioni C, Derlet A, Bassetti B, Tilenni M, Carena MC, Farsetti A, et al. The histone acetylase activator pentadecylidenemalonate 1b rescues proliferation and differentiation in the human cardiac mesenchymal cells of type 2 diabetic patients. Diabetes 2014; 63(6):2132-47; PMID:24458358; https://doi.org/10.2337/db13-0731
- Chatterjee S, Mizar P, Cassel R, Neidl R, Selvi BR, Mohankrishna DV, Vedamurthy BM, Schneider A, Bousiges O, Mathis C, et al. A novel activator of CBP/p300 acetyltransferases promotes neurogenesis and extends memory duration in adult mice. J Neurosci 2013; 33(26):10698-712; PMID:23804093; https://doi.org/10.1523/JNEUROSCI.5772-12.2013