BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

Cell - Tập 146 - Trang 904-917 - 2011
Jake E. Delmore1, Ghayas C. Issa1, Madeleine E. Lemieux2, Peter B. Rahl3, Junwei Shi4, Hannah M. Jacobs1, Efstathios Kastritis1, Timothy Gilpatrick1, Ronald M. Paranal1, Jun Qi1, Marta Chesi5, Anna C. Schinzel1, Michael R. McKeown1, Timothy P. Heffernan1, Christopher R. Vakoc6, P. Leif Bergsagel5, Irene M. Ghobrial1,7, Paul G. Richardson1,7, Richard A. Young3,8, William C. Hahn1,9
1Department of Medical Oncology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA
2Department of Pediatric Oncology, Dana-Farber Cancer Institute and Children's Hospital Boston, 450 Brookline Avenue, Boston, MA 02215, USA
3Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142 USA
4Cold Spring Harbor Laboratory, 1 Bungtown Road, Cold Spring Harbor, NY 11724, USA
5Comprehensive Cancer Center, Mayo Clinic Arizona, Scottsdale, AZ 85259, USA
6Cold Spring Harbor Laboratory, 1 Bungtown Road, Cold Spring Harbor, NY 11724 USA
7Department of Medicine, Harvard Medical School 25 Shattuck Street, Boston, MA 02115, USA
8Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02142, USA
9Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA

Tài liệu tham khảo

Amati, 1993, Oncogenic activity of the c-Myc protein requires dimerization with Max, Cell, 72, 233, 10.1016/0092-8674(93)90663-B Beroukhim, 2010, The landscape of somatic copy-number alteration across human cancers, Nature, 463, 899, 10.1038/nature08822 Bidwell, 2009, Targeting a c-Myc inhibitory polypeptide to specific intracellular compartments using cell penetrating peptides, J. Control. Release, 135, 2, 10.1016/j.jconrel.2008.11.015 Bisgrove, 2007, Conserved P-TEFb-interacting domain of BRD4 inhibits HIV transcription, Proc. Natl. Acad. Sci. USA, 104, 13690, 10.1073/pnas.0705053104 Blackwood, 1991, Max: a helix-loop-helix zipper protein that forms a sequence-specific DNA-binding complex with Myc, Science, 251, 1211, 10.1126/science.2006410 Chapman, 2011, Initial genome sequencing and analysis of multiple myeloma, Nature, 471, 467, 10.1038/nature09837 Chesi, 2008, AID-dependent activation of a MYC transgene induces multiple myeloma in a conditional mouse model of post-germinal center malignancies, Cancer Cell, 13, 167, 10.1016/j.ccr.2008.01.007 Chng, 2011, Clinical and biological implications of MYC activation: a common difference between MGUS and newly diagnosed multiple myeloma, Leukemia, 25, 1026, 10.1038/leu.2011.53 Claudio, 2002, A molecular compendium of genes expressed in multiple myeloma, Blood, 100, 2175, 10.1182/blood-2002-01-0008 Dang, 2009, MYC, microRNAs and glutamine addiction in cancers, Cell Cycle, 8, 3243, 10.4161/cc.8.20.9522 Dang, 2009, MYC-induced cancer cell energy metabolism and therapeutic opportunities, Clin. Cancer Res., 15, 6479, 10.1158/1078-0432.CCR-09-0889 Darnell, 2002, Transcription factors as targets for cancer therapy, Nat. Rev. Cancer, 2, 740, 10.1038/nrc906 Dean, 1983, Transcriptional activation of immunoglobulin alpha heavy-chain genes by translocation of the c-myc oncogene, Nature, 305, 443, 10.1038/305443a0 Dey, 2009, Brd4 marks select genes on mitotic chromatin and directs postmitotic transcription, Mol. Biol. Cell, 20, 4899, 10.1091/mbc.E09-05-0380 Dhalluin, 1999, Structure and ligand of a histone acetyltransferase bromodomain, Nature, 399, 491, 10.1038/20974 Dib, 2008, Characterization of MYC translocations in multiple myeloma cell lines, J. Natl. Cancer Inst. Monogr., 25, 10.1093/jncimonographs/lgn011 Filippakopoulos, 2010, Selective inhibition of BET bromodomains, Nature, 468, 1067, 10.1038/nature09504 Frank, 2003, MYC recruits the TIP60 histone acetyltransferase complex to chromatin, EMBO Rep., 4, 575, 10.1038/sj.embor.embor861 Frye, 2010, The art of the chemical probe, Nat. Chem. Biol., 6, 159, 10.1038/nchembio.296 Fukazawa, 2010, Inhibition of Myc effectively targets KRAS mutation-positive lung cancer expressing high levels of Myc, Anticancer Res., 30, 4193 Gomi, 1990, Glucocorticoid effects on myeloma cells in culture: correlation of growth inhibition with induction of glucocorticoid receptor messenger RNA, Cancer Res., 50, 1873 Hammoudeh, 2009, Multiple independent binding sites for small-molecule inhibitors on the oncoprotein c-Myc, J. Am. Chem. Soc., 131, 7390, 10.1021/ja900616b Harada, 1998, Expression of Bcl-2 family of proteins in fresh myeloma cells, Leukemia, 12, 1817, 10.1038/sj.leu.2401168 Harris, 1988, The E mu-myc transgenic mouse. A model for high-incidence spontaneous lymphoma and leukemia of early B cells, J. Exp. Med., 167, 353, 10.1084/jem.167.2.353 Haynes, 1992, The bromodomain: a conserved sequence found in human, Drosophila and yeast proteins, Nucleic Acids Res., 20, 2603, 10.1093/nar/20.10.2603 Hideshima, 2007, Understanding multiple myeloma pathogenesis in the bone marrow to identify new therapeutic targets, Nat. Rev. Cancer, 7, 585, 10.1038/nrc2189 Hurt, 2004, Overexpression of c-maf is a frequent oncogenic event in multiple myeloma that promotes proliferation and pathological interactions with bone marrow stroma, Cancer Cell, 5, 191, 10.1016/S1535-6108(04)00019-4 Jain, 2002, Sustained loss of a neoplastic phenotype by brief inactivation of MYC, Science, 297, 102, 10.1126/science.1071489 Jeong, 2010, Small-molecule inhibitors of c-Myc transcriptional factor suppress proliferation and induce apoptosis of promyelocytic leukemia cell via cell cycle arrest, Mol. Biosyst., 6, 1503, 10.1039/c002534h Keats, 2007, Promiscuous mutations activate the noncanonical NF-kappaB pathway in multiple myeloma, Cancer Cell, 12, 131, 10.1016/j.ccr.2007.07.003 Kim, 2008, An extended transcriptional network for pluripotency of embryonic stem cells, Cell, 132, 1049, 10.1016/j.cell.2008.02.039 Kim, 2006, Combined microarray analysis of small cell lung cancer reveals altered apoptotic balance and distinct expression signatures of MYC family gene amplification, Oncogene, 25, 130, 10.1038/sj.onc.1208997 Leder, 1986, Consequences of widespread deregulation of the c-myc gene in transgenic mice: multiple neoplasms and normal development, Cell, 45, 485, 10.1016/0092-8674(86)90280-1 Legartova, 2009, Nuclear topography of the 1q21 genomic region and Mcl-1 protein levels associated with pathophysiology of multiple myeloma, Neoplasma, 56, 404, 10.4149/neo_2009_05_404 Malo, 2006, Statistical practice in high-throughput screening data analysis, Nat. Biotechnol., 24, 167, 10.1038/nbt1186 Matsumura, 2003, E2F1 and c-Myc in cell growth and death, Cell Cycle, 2, 333, 10.4161/cc.2.4.428 Mattioli, 2005, Gene expression profiling of plasma cell dyscrasias reveals molecular patterns associated with distinct IGH translocations in multiple myeloma, Oncogene, 24, 2461, 10.1038/sj.onc.1208447 McMillin, 2010, Tumor cell-specific bioluminescence platform to identify stroma-induced changes to anticancer drug activity, Nat. Med., 16, 483, 10.1038/nm.2112 Mitsiades, 2004, Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors, Cancer Cell, 5, 221, 10.1016/S1535-6108(04)00050-9 Mitsiades, 2002, Molecular sequelae of proteasome inhibition in human multiple myeloma cells, Proc. Natl. Acad. Sci. USA, 99, 14374, 10.1073/pnas.202445099 Nair, 2003, X-ray structures of Myc-Max and Mad-Max recognizing DNA. Molecular bases of regulation by proto-oncogenic transcription factors, Cell, 112, 193, 10.1016/S0092-8674(02)01284-9 Nicodeme, 2010, Suppression of inflammation by a synthetic histone mimic, Nature, 468, 1119, 10.1038/nature09589 Oltersdorf, 2005, An inhibitor of Bcl-2 family proteins induces regression of solid tumours, Nature, 435, 677, 10.1038/nature03579 Palumbo, 1989, Altered expression of growth-regulated protooncogenes in human malignant plasma cells, Cancer Res., 49, 4701 Pomerantz, 2009, The 8q24 cancer risk variant rs6983267 shows long-range interaction with MYC in colorectal cancer, Nat. Genet., 41, 882, 10.1038/ng.403 Pomerantz, 2009, Evaluation of the 8q24 prostate cancer risk locus and MYC expression, Cancer Res., 69, 5568, 10.1158/0008-5472.CAN-09-0387 Rahl, 2010, c-Myc regulates transcriptional pause release, Cell, 141, 432, 10.1016/j.cell.2010.03.030 Rahman, 2011, The Brd4 extraterminal domain confers transcription activation independent of pTEFb by recruiting multiple proteins, including NSD3, Mol. Cell. Biol., 31, 2641, 10.1128/MCB.01341-10 Schlosser, 2005, Dissection of transcriptional programmes in response to serum and c-Myc in a human B-cell line, Oncogene, 24, 520, 10.1038/sj.onc.1208198 Schreiber, 2002, Signaling network model of chromatin, Cell, 111, 771, 10.1016/S0092-8674(02)01196-0 Schuhmacher, 2001, The transcriptional program of a human B cell line in response to Myc, Nucleic Acids Res., 29, 397, 10.1093/nar/29.2.397 Shaffer, 2008, IRF4 addiction in multiple myeloma, Nature, 454, 226, 10.1038/nature07064 Shou, 2000, Diverse karyotypic abnormalities of the c-myc locus associated with c-myc dysregulation and tumor progression in multiple myeloma, Proc. Natl. Acad. Sci. USA, 97, 228, 10.1073/pnas.97.1.228 Soucek, 1998, Design and properties of a Myc derivative that efficiently homodimerizes, Oncogene, 17, 2463, 10.1038/sj.onc.1202199 Soucek, 2002, Omomyc, a potential Myc dominant negative, enhances Myc-induced apoptosis, Cancer Res., 62, 3507 Stewart, 1984, Spontaneous mammary adenocarcinomas in transgenic mice that carry and express MTV/myc fusion genes, Cell, 38, 627, 10.1016/0092-8674(84)90257-5 Trimarchi, 2002, Sibling rivalry in the E2F family, Nat. Rev. Mol. Cell Biol., 3, 11, 10.1038/nrm714 Trudel, 2007, The Bcl-2 family protein inhibitor, ABT-737, has substantial antimyeloma activity and shows synergistic effect with dexamethasone and melphalan, Clin. Cancer Res., 13, 621, 10.1158/1078-0432.CCR-06-1526 Vervoorts, 2003, Stimulation of c-MYC transcriptional activity and acetylation by recruitment of the cofactor CBP, EMBO Rep., 4, 484, 10.1038/sj.embor.embor821 Wu, 2007, Cellular senescence is an important mechanism of tumor regression upon c-Myc inactivation, Proc. Natl. Acad. Sci. USA, 104, 13028, 10.1073/pnas.0701953104 Zeller, 2003, An integrated database of genes responsive to the Myc oncogenic transcription factor: identification of direct genomic targets, Genome Biol., 4, R69, 10.1186/gb-2003-4-10-r69 Zhan, 2007, Gene-expression signature of benign monoclonal gammopathy evident in multiple myeloma is linked to good prognosis, Blood, 109, 1692, 10.1182/blood-2006-07-037077 Zuber, 2011, RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia, Nature, 10.1038/nature10334 Boehm, J.S., Zhao, J.J., Yao, J., Kim, S.Y., Firestein, R., Dunn, I.F., Sjostrom, S.K., Garraway, L.A., Weremowicz, S., Richardson, A.L., et al. (2007). Integrative genomic approaches identify IKBKE as a breast cancer oncogene. Cell 129, 1065–1079. Bolstad, B.M., Irizarry, R.A., Astrand, M., and Speed, T.P. (2003). A comparison of normalization methods for high density oligonucleotide array data based on variance and bias. Bioinformatics 19, 185–193. Chesi, M., Robbiani, D.F., Sebag, M., Chng, W.J., Affer, M., Tiedemann, R., Valdez, R., Palmer, S.E., Haas, S.S., Stewart, A.K., et al. (2008). AID-dependent activation of a MYC transgene induces multiple myeloma in a conditional mouse model of post-germinal center malignancies. Cancer Cell 13, 167–180. Filippakopoulos, P., Qi, J., Picaud, S., Shen, Y., Smith, W.B., Fedorov, O., Morse, E.M., Keates, T., Hickman, T.T., Felletar, I., et al. (2010). Selective inhibition of BET bromodomains. Nature 468, 1067–1073. Hemann, M.T., Fridman, J.S., Zilfou, J.T., Hernando, E., Paddison, P.J., Cordon-Cardo, C., Hannon, G.J., and Lowe, S.W. (2003). An epi-allelic series of p53 hypomorphs created by stable RNAi produces distinct tumor phenotypes in vivo. Nat. Genet. 33, 396–400. Irizarry, R.A., Bolstad, B.M., Collin, F., Cope, L.M., Hobbs, B., and Speed, T.P. (2003a). Summaries of Affymetrix GeneChip probe level data. Nucleic Acids Res. 31, e15. Irizarry, R.A., Hobbs, B., Collin, F., Beazer-Barclay, Y.D., Antonellis, K.J., Scherf, U., and Speed, T.P. (2003b). Exploration, normalization, and summaries of high density oligonucleotide array probe level data. Biostatistics 4, 249–264. Johnson, W.E., Li, C., and Rabinovic, A. (2007). Adjusting batch effects in microarray expression data using empirical Bayes methods. Biostatistics 8, 118–127. Malo, N., Hanley, J.A., Cerquozzi, S., Pelletier, J., and Nadon, R. (2006). Statistical practice in high-throughput screening data analysis. Nat. Biotechnol. 24, 167–175. McMillin, D.W., Delmore, J., Weisberg, E., Negri, J.M., Geer, D.C., Klippel, S., Mitsiades, N., Schlossman, R.L., Munshi, N.C., Kung, A.L., et al. (2010). Tumor cell-specific bioluminescence platform to identify stroma-induced changes to anticancer drug activity. Nat. Med. 16, 483–489. Moffat, J., Grueneberg, D.A., Yang, X., Kim, S.Y., Kloepfer, A.M., Hinkle, G., Piqani, B., Eisenhaure, T.M., Luo, B., Grenier, J.K., et al. (2006). A lentiviral RNAi library for human and mouse genes applied to an arrayed viral high-content screen. Cell 124, 1283–1298. Rahl, P.B., Lin, C.Y., Seila, A.C., Flynn, R.A., McCuine, S., Burge, C.B., Sharp, P.A., and Young, R.A. (2010). c-Myc regulates transcriptional pause release. Cell 141, 432–445. Smyth, G.K. (2005). Limma: linear models for microarray data. In Bioinformatics and Computational Biology Solutions using R and Bioconductor, R. Gentleman, V. Carey, S. Dudoit, R. Irizarry, and W. Huber, eds. (New York: Springer). Subramanian, A., Tamayo, P., Mootha, V.K., Mukherjee, S., Ebert, B.L., Gillette, M.A., Paulovich, A., Pomeroy, S.L., Golub, T.R., Lander, E.S., and Mesirov, J.P. (2005). Gene set enrichment analysis: a knowledge-based approach for interpreting genome-wide expression profiles. Proc. Natl. Acad. Sci. USA 102, 15545–15550. Zuber, J., Rappaport, A.R., Luo, W., Wang, E., Chen, C., Vaseva, A.V., Shi, J., Weissmueller, S., Fellman, C., Taylor, M.J., et al. (2011). An integrated approach to dissecting oncogene addiction implicates a Myb-coordinated self-renewal program as essential for leukemia maintenance. Genes Dev. 25, 1628–1640.