Cited by 2,961Protein Degradation and InhibitorsChromatin Remodeling and CancerGenomics and Chromatin Dynamics

The DOI matches its Crossref record; 86 of the 86 references it cites were found in a registry or an index.

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

Open access

Lovén, Jakob, Hoke, Heather A., Lin, Charles Y., Lau, Ashley, Orlando, David A., Vakoc, Christopher R., Bradner, James E., Lee, Tong Ihn, Young, Richard A.·2013·Cell

DOI 10.1016/j.cell.2013.03.036PMC PMC3760967

Open this paper in CoChat — free account Open PDF

Abstract

Chromatin regulators have become attractive targets for cancer therapy, but it is unclear why inhibition of these ubiquitous regulators should have gene-specific effects in tumor cells. Here, we investigate how inhibition of the widely expressed transcriptional coactivator BRD4 leads to selective inhibition of the MYC oncogene in multiple myeloma (MM). BRD4 and Mediator were found to co-occupy thousands of enhancers associated with active genes. They also co-occupied a small set of exceptionally large super-enhancers associated with genes that feature prominently in MM biology, including the MYC oncogene. Treatment of MM tumor cells with the BET-bromodomain inhibitor JQ1 led to preferential loss of BRD4 at super-enhancers and consequent transcription elongation defects that preferentially impacted genes with super-enhancers, including MYC. Super-enhancers were found at key oncogenic drivers in many other tumor cells. These observations have implications for the discovery of cancer therapeutics directed at components of super-enhancers in diverse tumor types.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1016/j.cell.2013.03.036

Cites

86 of 86 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Ultrafast and memory-efficient alignment of short DNA sequences to the human genome.
Langmead, B., Trapnell, C., Pop, M., & Salzberg, S. L. (2009) · Genome Biology · doi:10.1186/gb-2009-10-3-r25 · Cited by 21,849
Model-based Analysis of ChIP-Seq (MACS)
Zhang, Y., Liu, T., Meyer, C. A., Eeckhoute, J., Johnson, D. S., Bernstein, B. E., Nusbaum, C., Myers, R. M., Brown, M., Li, W., et al. (2008) · Genome Biology · doi:10.1186/gb-2008-9-9-r137 · Cited by 18,386
Topological domains in mammalian genomes identified by analysis of chromatin interactions
Dixon, J. R., Selvaraj, S., Yue, F., Kim, A., Li, Y., Shen, Y., Hu, M., Liu, J. S., & Ren, B. (2012) · Nature · doi:10.1038/nature11082 · Cited by 6,829
NCBI reference sequences (RefSeq): a curated non-redundant sequence database of genomes, transcripts and proteins
Pruitt, K. D., Tatusova, T. A., & Maglott, D. R. (2006) · Nucleic Acids Research · doi:10.1093/nar/gkl842 · Cited by 4,441
Histone H3K27ac separates active from poised enhancers and predicts developmental state
Creyghton, M. P., Cheng, A. W., Welstead, G. G., Kooistra, T., Carey, B. W., Steine, E. J., Hanna, J., Lodato, M. A., Frampton, G. M., Sharp, P. A., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1016071107 · Cited by 4,302
Self-citation
Selective inhibition of BET bromodomains
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) · Nature · doi:10.1038/nature09504 · Cited by 4,262
Self-citation
Master Transcription Factors and Mediator Establish Super-Enhancers at Key Cell Identity Genes
Whyte, W. A., Orlando, D. A., Hnisz, D., Abraham, B. J., Lin, C. Y., Kagey, M. H., Rahl, P. B., Lee, T. I., & Young, R. A. (2013) · Cell · doi:10.1016/j.cell.2013.03.035 · Cited by 4,143
Self-citation
The landscape of somatic copy-number alteration across human cancers
Beroukhim, R., Mermel, C. H., Porter, D., Wei, G., Raychaudhuri, S., Donovan, J., Barretina, J., Boehm, J. S., Dobson, J., Urashima, M., et al. (2010) · Nature · doi:10.1038/nature08822 · Cited by 4,017
Epigenetics in Cancer
Esteller, M. (2008) · New England Journal of Medicine · doi:10.1056/nejmra072067 · Cited by 3,767
Integrative annotation of human large intergenic noncoding RNAs reveals global properties and specific subclassesPreprint
Cabili, M. N., Trapnell, C., Goff, L. A., Koziol, M. J., Tazón‐Vega, B., Regev, A., & Rinn, J. L. (2011) · Genes & Development · doi:10.1101/gad.17446611 · Cited by 3,551

Flagged first, then by citations

Show all 86 references

Sorted by citations

Items 601–700 of 1,008

The nuclear oncoprotein Fra-1: a transcription factor knocking on therapeutic applications’ door
Talotta, F., Casalino, L., & Verde, P. (2020) · Oncogene · doi:10.1038/s41388-020-1306-4 · Cited by 84
Super-enhancers: a new frontier for epigenetic modifiers in cancer chemoresistance
Li, G., Qu, Q., Qi, T.-T., Teng, X.-Q., Zhu, H., Wang, J., Lu, Q., & Qu, J. (2021) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-021-01974-y · Cited by 89
Epigenetics in the hematologic malignancies
Fong, C. Y., Morison, J., & Dawson, M. A. (2014) · Haematologica · doi:10.3324/haematol.2013.092007 · Cited by 87
Signal-Dependent Recruitment of BRD4 to Cardiomyocyte Super-Enhancers Is Suppressed by a MicroRNA
Stratton, M. S., Lin, C. Y., Anand, P., Tatman, P. D., Ferguson, B. S., Wickers, S. T., Ambardekar, A. V., Sucharov, C. C., Bradner, J. E., Haldar, S. M., et al. (2016) · Cell Reports · doi:10.1016/j.celrep.2016.06.074 · Cited by 86
Self-citation
Identification and Targeting of Long-Term Tumor-Propagating Cells in Small Cell Lung Cancer
Jahchan, N. S., Lim, J. S., Bola, B. M., Morris, K. L., Seitz, G., Tran, K. Q. T., Xu, L., Trapani, F., Morrow, C. J., Cristea, S., et al. (2016) · Cell Reports · doi:10.1016/j.celrep.2016.06.021 · Cited by 83
Challenges and Recent Advances in Medulloblastoma Therapy
Kumar, V., Kumar, V., McGuire, T. R., Coulter, D. W., Sharp, J. G., & Mahato, R. I. (2017) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2017.09.002 · Cited by 85
Super-Enhancer-Associated LncRNA UCA1 Interacts Directly with AMOT to Activate YAP Target Genes in Epithelial Ovarian Cancer
Lin, X., Spindler, T. J., Fonseca, M. A. D. S., Corona, R. I., Seo, J.-H., Dezem, F. S., Li, L., Lee, J. M., Long, H. W., Sellers, T. A., et al. (2019) · iScience · doi:10.1016/j.isci.2019.06.025 · Cited by 84
A C19MC-LIN28A-MYCN Oncogenic Circuit Driven by Hijacked Super-enhancers Is a Distinct Therapeutic Vulnerability in ETMRs: A Lethal Brain Tumor
Sin‐Chan, P., Mumal, I., Suwal, T., Ho, B., Fan, X., Singh, I., Du, Y., Lu, M., Patel, N., Torchia, J., et al. (2019) · Cancer Cell · doi:10.1016/j.ccell.2019.06.002 · Cited by 84
Self-citation
Multifaceted Roles of DNA Methylation in Neoplastic Transformation, from Tumor Suppressors to EMT and Metastasis
Casalino, L., & Verde, P. (2020) · Genes · doi:10.3390/genes11080922 · Cited by 83
Epigenetic modifications in prostate cancer
Sugiura, M., Sato, H., Kanesaka, M., Imamura, Y., Sakamoto, S., Ichikawa, T., & Kaneda, A. (2020) · International Journal of Urology · doi:10.1111/iju.14406 · Cited by 83
Effective therapy for AML with RUNX1 mutation by cotreatment with inhibitors of protein translation and BCL2
Mill, C. P., Fiskus, W. C., Dinardo, C. D., Birdwell, C. E., Davis, J. A., Kadia, T. M., Takahashi, K., Short, N. J., Daver, N. G., Ohanian, M. N., et al. (2021) · Blood · doi:10.1182/blood.2021013156 · Cited by 83
Predicting master transcription factors from pan-cancer expression data
Reddy, J., Fonseca, M. A., Corona, R. I., Nameki, R. A., Dezem, F. S., Klein, I. A., Chang, H. S. Y., Chaves‐Moreira, D., Afeyan, L. K., Malta, T. M., et al. (2021) · Science Advances · doi:10.1126/sciadv.abf6123 · Cited by 82
Self-citation
Transcriptional elongation control in developmental gene expression, aging, and disease
Aoi, Y., & Shilatifard, A. (2023) · Molecular Cell · doi:10.1016/j.molcel.2023.10.004 · Cited by 89
Epigenetic modulation of type-1 diabetes via a dual effect on pancreatic macrophages and β cells
Fu, W., Farache, J., Clardy, S. M., Hattori, K., Mander, P. K., Lee, K. C., Rioja, I., Weissleder, R., Prinjha, R. K., Benoist, C. O., et al. (2014) · eLife · doi:10.7554/elife.04631 · Cited by 84
Acute TNF-induced repression of cell identity genes is mediated by NFκB-directed redistribution of cofactors from super-enhancersPreprint
Schmidt, S. F., Larsen, B. D., Loft, A., Nielsen, R., Madsen, J. G. S., & Mandrup, S. (2015) · Genome Research · doi:10.1101/gr.188300.114 · Cited by 83
Combining BET and HDAC inhibitors synergistically induces apoptosis of melanoma and suppresses AKT and YAP signaling
Heinemann, A., Cullinane, C. M., Paoli‐Iseppi, R. D., Wilmott, J. S., Gunatilake, D., Madore, J., Strbenac, D., Yang, J. Y. H., Gowrishankar, K., Tiffen, J. C., et al. (2015) · Oncotarget · doi:10.18632/oncotarget.4242 · Cited by 82
Concepts to Target MYC in Pancreatic Cancer
Wirth, M., Mahboobi, S., Krämer, O. H., & Schneider, G. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0050 · Cited by 81
Super Enhancer–Regulated LncRNA LINC01089 Induces Alternative Splicing of DIAPH3 to Drive Hepatocellular Carcinoma Metastasis
Su, T., Zhang, N., Wang, T., Zeng, J., Li, W., Han, L., & Yang, M. (2023) · Cancer Research · doi:10.1158/0008-5472.can-23-0544 · Cited by 82
BET Bromodomain Inhibition Triggers Apoptosis of NF1-Associated Malignant Peripheral Nerve Sheath Tumors through Bim Induction
Patel, A. J., Liao, C.-P., Chen, Z., Liu, C., Wang, Y., & Le, L. Q. (2014) · Cell Reports · doi:10.1016/j.celrep.2013.12.001 · Cited by 82
Interactions between Retroviruses and the Host Cell Genome
Poletti, V., & Mavilio, F. (2017) · Molecular Therapy — Methods & Clinical Development · doi:10.1016/j.omtm.2017.10.001 · Cited by 85
Rewiring the Epigenetic Networks in MLL-Rearranged Leukemias: Epigenetic Dysregulation and Pharmacological Interventions
Chan, A., & Chen, C.-W. D. (2019) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2019.00081 · Cited by 83
Stromal remodeling by the BET bromodomain inhibitor JQ1 suppresses the progression of human pancreatic cancer
Yamamoto, K., Tateishi, K., Kudo, Y., Hoshikawa, M., Tanaka, M. H., Nakatsuka, T., Fujiwara, H., Miyabayashi, K., Takahashi, R., Tanaka, Y., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.11129 · Cited by 83
Super-enhancer-associated MEIS1 promotes transcriptional dysregulation in Ewing sarcoma in co-operation with EWS-FLI1
Lin, L., Huang, M., Shi, X., Mayakonda, A., Hu, K., Jiang, Y., Guo, X., Chen, L., Pang, B., Doan, N., et al. (2018) · Nucleic Acids Research · doi:10.1093/nar/gky1207 · Cited by 84
Targeting chromatin complexes in fusion protein-driven malignancies
Brien, G. L., Stegmaier, K., & Armstrong, S. A. (2019) · Nature reviews. Cancer · doi:10.1038/s41568-019-0132-x · Cited by 84
RNA polymerase II clusters form in line with surface condensation on regulatory chromatin
Pancholi, A., Klingberg, T., Zhang, W., Prizak, R., Mamontova, I., Noa, A., Sobucki, M., Kobitski, A. Y., Nienhaus, G. U., Zaburdaev, V., et al. (2021) · Molecular Systems Biology · doi:10.15252/msb.202110272 · Cited by 85
BET bromodomain inhibition suppresses transcriptional responses to cytokine‐Jak‐STAT signaling in a gene‐specific manner in human monocytes
Chan, C., Fang, C., Qiao, Y., Yarilina, A., Prinjha, R. K., & Ivashkiv, L. B. (2014) · European Journal of Immunology · doi:10.1002/eji.201444862 · Cited by 81
Functional Enhancers As Master Regulators of Tissue-Specific Gene Regulation and Cancer Development
Ko, J. Y., Oh, S., & Yoo, K. H. (2017) · Molecules and Cells · doi:10.14348/molcells.2017.0033 · Cited by 83
The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML
Gerlach, D., Tontsch-Grunt, U., Baum, A., Popow, J., Scharn, D., Hofmann, M. H., Engelhardt, H., Kaya, O., Beck, J., Schweifer, N., et al. (2018) · Oncogene · doi:10.1038/s41388-018-0150-2 · Cited by 82
Rational optimization of a transcription factor activation domain inhibitor
Basu, S., Martínez-Cristóbal, P., Frigolé-Vivas, M., Pesarrodona, M., Lewis, M., Szulc, E., Bañuelos, C. A., Sánchez-Zarzalejo, C., Bielskutė, S., Zhu, J., et al. (2023) · Nature Structural & Molecular Biology · doi:10.1038/s41594-023-01159-5 · Cited by 83
Super-enhancers and broad H3K4me3 domains form complex gene regulatory circuits involving chromatin interactions
Cao, F., Fang, Y., Tan, H. K., Goh, Y., Choy, J. Y. H., Koh, B. T. H., Hao Tan, J., Bertin, N., Ramadass, A., Hunter, E., et al. (2017) · Scientific Reports · doi:10.1038/s41598-017-02257-3 · Cited by 80
Chromatin dependencies in cancer and inflammation
Marazzi, I., Greenbaum, B. D., Low, D. H. P., & Guccione, E. (2018) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm.2017.113 · Cited by 80
Atypical 3q26/MECOM rearrangements genocopy inv(3)/t(3;3) in acute myeloid leukemia
Ottema, S., Mulet‐Lazaro, R., Beverloo, H. B., Erpelinck-Verschueren, C. A. J., van Herk, S., van der Helm, R. M., Havermans, M., Grob, T., Valk, P. J. M., Bindels, E. M., et al. (2020) · Blood · doi:10.1182/blood.2019003701 · Cited by 81
Transcriptional control by enhancers and enhancer RNAs
Lewis, M. W., Shen, L., & Franco, H. L. (2019) · Transcription · doi:10.1080/21541264.2019.1695492 · Cited by 84
p113 isoform encoded by CUX1 circular RNA drives tumor progression via facilitating ZRF1/BRD4 transactivation
Yang, F., Hu, A., Guo, Y., Wang, J., Li, D., Wang, X., Jin, S., Yuan, B., Cai, S., Zhou, Y., et al. (2021) · Molecular Cancer · doi:10.1186/s12943-021-01421-8 · Cited by 79
LARP7 suppresses P-TEFb activity to inhibit breast cancer progression and metastasis
Ji, X., Lu, H., Zhou, Q., & Luo, K. (2014) · eLife · doi:10.7554/elife.02907 · Cited by 79
Understanding MYC-driven aggressive B-cell lymphomas: pathogenesis and classification
Ott, G., Rosenwald, A., & Campo, E. (2013) · Hematology · doi:10.1182/asheducation-2013.1.575 · Cited by 79
Pan-cancer analysis on microRNA-associated gene activation
Tan, H., HUANG, S. H., Zhang, Z., Qian, X., Sun, P., & Zhou, X. (2019) · EBioMedicine · doi:10.1016/j.ebiom.2019.03.082 · Cited by 79
Epigenetic Regulation of Inflammatory Signaling and Inflammation-Induced Cancer
Tan, S. Y. X., Zhang, J., & Tee, W. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.931493 · Cited by 86
An atlas of regulatory elements in chicken: A resource for chicken genetics and genomics
Pan, Z., Wang, Y., Wang, M., Wang, Y., Zhu, X., Gu, S. V., Zhong, C., An, L., Shan, M., Damas, J., et al. (2023) · Science Advances · doi:10.1126/sciadv.ade1204 · Cited by 85
In vivo reprogramming drives Kras-induced cancer development
Shibata, H., Komura, S., Yamada, Y., Sankoda, N., Tanaka, A., Ukai, T., Kabata, M., Sakurai, S., Kuze, B., Woltjen, K., et al. (2018) · Nature Communications · doi:10.1038/s41467-018-04449-5 · Cited by 76
ETS family transcriptional regulators drive chromatin dynamics and malignancy in squamous cell carcinomas
Yang, H., Schramek, D., Adam, R. C., Keyes, B. E., Wang, P., Zheng, D., & Fuchs, E. V. (2015) · eLife · doi:10.7554/elife.10870 · Cited by 77
Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma
Siu, K. T., Ramachandran, J., Yee, A. J., Eda, H., Santo, L., Panaroni, C., Mertz, J. A., Sims, R. J., Cooper, M. R., & Raje, N. S. (2016) · Leukemia · doi:10.1038/leu.2016.355 · Cited by 81
Enhancers and chromatin structures: regulatory hubs in gene expression and diseases
Hu, Z., & Tee, W. (2017) · Bioscience Reports · doi:10.1042/bsr20160183 · Cited by 80
BRD4 has dual effects on the HMGB1 and NF-κB signalling pathways and is a potential therapeutic target for osteoarthritis
Jiang, Y., Zhu, L., Zhang, T., Lu, H., Wang, C., Xue, B., Xu, X., Liu, Y., Cai, Z., Sang, W., et al. (2017) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2017.08.009 · Cited by 76
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor
Divakaran, A., Talluri, S., Ayoub, A. M., Mishra, N. K., Cui, H., Widen, J. C., Berndt, N., Zhu, J.-Y., Carlson, A. S., Topczewski, J. J., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01248 · Cited by 76
Emerging Roles of Liquid–Liquid Phase Separation in Cancer: From Protein Aggregation to Immune-Associated Signaling
Lu, J., Qian, J., Xu, Z., Yin, S., Zhou, L., Zheng, S., & Zhang, W. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.631486 · Cited by 77
BET Proteins as Attractive Targets for Cancer Therapeutics
Sarnik, J., Popławski, T., & Tokarz, P. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222011102 · Cited by 78
BRD4 and MYC : power couple in transcription and disease
Kotekar, A., Singh, A. K., & Devaiah, B. N. (2022) · FEBS Journal · doi:10.1111/febs.16580 · Cited by 77
LSD1 Inhibition Disrupts Super-Enhancer–Driven Oncogenic Transcriptional Programs in Castration-Resistant Prostate Cancer
Li, M., Liu, M., Han, W., Wang, Z., Han, D. G., Patalano, S. C., Macoska, J. A., Balk, S. P., He, H. H., Corey, E., et al. (2023) · Cancer Research · doi:10.1158/0008-5472.can-22-2433 · Cited by 80
Situational Awareness: Regulation of the Myb Transcription Factor in Differentiation, the Cell Cycle and Oncogenesis
George, O., & Ness, S. A. (2014) · Cancers · doi:10.3390/cancers6042049 · Cited by 76
The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes
Atkinson, S. J., Soden, P. E., Angell, D. C., Bantscheff, M., Chung, C., Giblin, K. A., Smithers, N. N., Furze, R. C., Gordon, L. J., Drewes, G., et al. (2014) · MedChemComm · doi:10.1039/c3md00285c · Cited by 77
Supercharging BRD4 with NUT in carcinoma
Eagen, K. P., & French, C. A. (2021) · Oncogene · doi:10.1038/s41388-020-01625-0 · Cited by 77
A BRD4-mediated elongation control point primes transcribing RNA polymerase II for 3′-processing and termination
Arnold, M., Bressin, A., Jasnovidova, O., Meierhofer, D., & Mayer, A. (2021) · Molecular Cell · doi:10.1016/j.molcel.2021.06.026 · Cited by 75
Predicting CTCF-mediated chromatin interactions by integrating genomic and epigenomic features
Yan, K., Andricovich, J., Zeng, Z., Zhu, J., Tzatsos, A., & Peng, W. (2018) · Nature Communications · doi:10.1038/s41467-018-06664-6 · Cited by 73
Aberrant Signaling Pathways in T-Cell Acute Lymphoblastic Leukemia
Bongiovanni, D., Saccomani, V., & Piovan, E. (2017) · International Journal of Molecular Sciences · doi:10.3390/ijms18091904 · Cited by 78
Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors
Kalan, S., Amat, R., Schachter, M. M., Kwiatkowski, N. P., Abraham, B. J., Liang, Y., Zhang, T., Olson, C. M., Larochelle, S., Young, R. A., et al. (2017) · Cell Reports · doi:10.1016/j.celrep.2017.09.056 · Cited by 74
Self-citation
Gene-specific mechanisms direct glucocorticoid-receptor-driven repression of inflammatory response genes in macrophages
Sacta, M. A., Tharmalingam, B., Coppo, M., Rollins, D. A., Deochand, D. K., Benjamin, B., Yu, L., Zhang, B., Hu, X., Li, R., et al. (2018) · eLife · doi:10.7554/elife.34864 · Cited by 77
Super-enhancer switching drives a burst in gene expression at the mitosis-to-meiosis transition
Maezawa, S., Sakashita, A., Yukawa, M., Chen, X., Takahashi, K., Alavattam, K. G., Nakata, I., Weirauch, M. T., Barski, A., & Namekawa, S. H. (2020) · Nature Structural & Molecular Biology · doi:10.1038/s41594-020-0488-3 · Cited by 77
MLL3 loss drives metastasis by promoting a hybrid epithelial–mesenchymal transition state
Cui, J., Zhang, C., Lee, J., Bartholdy, B., Yang, D., Liu, Y., Erler, P., Galbo, P. M., Hodge, D. Q., Huangfu, D., et al. (2023) · Nature Cell Biology · doi:10.1038/s41556-022-01045-0 · Cited by 75
Distinct layers of BRD4-PTEFb reveal bromodomain-independent function in transcriptional regulation
Zheng, B., Gold, S. R., Iwanaszko, M., Howard, B. C., Wang, L., & Shilatifard, A. (2023) · Molecular Cell · doi:10.1016/j.molcel.2023.06.032 · Cited by 78
Affinity and dose of TCR engagement yield proportional enhancer and gene activity in CD4+ T cells
Allison, K. A., Sajti, E., Collier, J. G., Gosselin, D., Troutman, T. D., Stone, E. L., Hedrick, S. Μ., & Glass, C. K. (2016) · eLife · doi:10.7554/elife.10134 · Cited by 74
A novel LSD1 inhibitor NCD38 ameliorates MDS-related leukemia with complex karyotype by attenuating leukemia programs via activating super-enhancers
Sugino, N., Kawahara, M., Tatsumi, G., Kanai, A., Matsui, H., Yamamoto, R., Nagai, Y., Fujii, S., Shimazu, Y., Hishizawa, M., et al. (2017) · Leukemia · doi:10.1038/leu.2017.59 · Cited by 76
Epigenetic Modification Mechanisms Involved in Inflammation and Fibrosis in Renal Pathology
Morgado‐Pascual, J. L., Marchant, V. A., Rodrigues-Díez, R. R., Doladé, N. G., Suárez-Álvarez, B., Kerr, B., Valdivielso, J. M., Ruiz‐Ortega, M., & Rayego‐Mateos, S. (2018) · Mediators of Inflammation · doi:10.1155/2018/2931049 · Cited by 73
The enhancer RNA ARIEL activates the oncogenic transcriptional program in T-cell acute lymphoblastic leukemia
Tan, S. H., Leong, W. Z., Ngoc, P. C. T., Tan, T. K., Bertulfo, F. C., Lim, M. C., An, Ö., Li, Z., Yeoh, A. E. J., Fullwood, M. J., et al. (2019) · Blood · doi:10.1182/blood.2018874503 · Cited by 73
Beyond the Exome: The Non-coding Genome and Enhancers in Neurodevelopmental Disorders and Malformations of Cortical Development
Perenthaler, E., Yousefi, S., Niggl, E., & Barakat, T. S. (2019) · Frontiers in Cellular Neuroscience · doi:10.3389/fncel.2019.00352 · Cited by 75
Cancer-epigenetic function of the histone methyltransferase KMT2D and therapeutic opportunities for the treatment of KMT2D-deficient tumors
Dhar, S. S., & Lee, M. G. (2021) · Oncotarget · doi:10.18632/oncotarget.27988 · Cited by 73
Simultaneous disruption of PRC2 and enhancer function underlies histone H3.3-K27M oncogenic activity in human hindbrain neural stem cells
Brien, G. L., Bressan, R. B., Monger, C., Gannon, D., Lagan, E., Doherty, A. M., Healy, E., Neikes, H. K., Fitzpatrick, D. J., Deevy, O., et al. (2021) · Nature Genetics · doi:10.1038/s41588-021-00897-w · Cited by 80
Super Enhancers in Cancers, Complex Disease, and Developmental Disorders
Niederriter, A. R., Varshney, A., Parker, S. C. J., & Martin, D. M. (2015) · Genes · doi:10.3390/genes6041183 · Cited by 75
APOBEC signature mutation generates an oncogenic enhancer that drives LMO1 expression in T-ALL
Li, Z., Abraham, B. J., Berezovskaya, A., Farah, N., Liu, Y., León, T. E., Fielding, A. K., Tan, S. H., Sanda, T., Weintraub, A. S., et al. (2017) · Leukemia · doi:10.1038/leu.2017.75 · Cited by 73
Self-citation
High-resolution structural genomics reveals new therapeutic vulnerabilities in glioblastomaPreprint
Johnston, M. J. G., Nikolić, A., Ninkovic, N., Guilhamon, P., Cavalli, F. M. G., Seaman, S., Zemp, F. J., Lee, J., Abdelkareem, A. O., Ellestad, K. I., et al. (2019) · Genome Research · doi:10.1101/gr.246520.118 · Cited by 68
BET Bromodomain Proteins as Cancer Therapeutic Targets
Shu, S., & Polyak, K. (2016) · Cold Spring Harbor Symposia on Quantitative Biology · doi:10.1101/sqb.2016.81.030908 · Cited by 72
Haploinsufficiency for NR3C1, the gene encoding the glucocorticoid receptor, in blastic plasmacytoid dendritic cell neoplasms
Emadali, A., Hoghoughi, N., Duley, S., Hajmirza, A., Verhoeyen, E., Cosset, F., Bertrand, P., Roumier, C., Roggy, A., Suchaud-Martin, C., et al. (2016) · Blood · doi:10.1182/blood-2015-09-671040 · Cited by 76
Epigenetics in T‐cell acute lymphoblastic leukemia
Peirs, S., der Meulen, J. V., de Walle, I. V., Taghon, T., Speleman, F., Poppe, B. G., & Vlierberghe, P. V. (2014) · Immunological Reviews · doi:10.1111/imr.12237 · Cited by 76
Maintenance of macrophage transcriptional programs and intestinal homeostasis by epigenetic reader SP140
Mehta, S., Cronkite, D. A., Basavappa, M. G., Saunders, T. L., Adiliaghdam, F., Amatullah, H., Morrison, S. A., Pagan, J. D., Anthony, R. M., Tonnerre, P., et al. (2017) · Science Immunology · doi:10.1126/sciimmunol.aag3160 · Cited by 69
Preclinical Efficacy and Molecular Mechanism of Targeting CDK7-Dependent Transcriptional Addiction in Ovarian Cancer
Zhang, Z., Peng, H., Wang, X., Yin, X., Ma, P., Jing, Y., Cai, M., Liu, J., Zhang, M., Zhang, S., et al. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-17-0078 · Cited by 74
The Hippo pathway modulates resistance to BET proteins inhibitors in lung cancer cells
Gobbi, G., Donati, B., Do Valle, I. F., Reggiani, F., Torricelli, F., Remondini, D., Castellani, G., Ambrosetti, D. C., Ciarrocchi, A., & Sancisi, V. (2019) · Oncogene · doi:10.1038/s41388-019-0924-1 · Cited by 69
BET inhibitors in the treatment of hematologic malignancies: current insights and future prospects
Munshi, H., Abedin, S., & Boddy, C. (2016) · OncoTargets and Therapy · doi:10.2147/ott.s100515 · Cited by 71
Genomic Effects of the Vitamin D Receptor: Potentially the Link between Vitamin D, Immune Cells, and Multiple Sclerosis
Lu, M. S., Taylor, B. V., & Körner, H. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2018.00477 · Cited by 73
Oncogenic HOXB8 is driven by MYC-regulated super-enhancer and potentiates colorectal cancer invasiveness via BACH1
Ying, Y., Wang, Y., Huang, X., Sun, Y., Zhang, J., Li, M., Zeng, J., Wang, M., Xiao, W., Zhong, L., et al. (2019) · Oncogene · doi:10.1038/s41388-019-1013-1 · Cited by 69
Targeting the undruggable: exploiting neomorphic features of fusion oncoproteins in childhood sarcomas for innovative therapies
Knott, M. M. L., Hölting, T. L. B., Ohmura, S., Kirchner, T., Cidre‐Aranaz, F., & Grünewald, T. G. P. (2019) · Cancer and Metastasis Reviews · doi:10.1007/s10555-019-09839-9 · Cited by 72
Chromatin state dynamics confers specific therapeutic strategies in enhancer subtypes of colorectal cancer
Orouji, E., Raman, A. T., Singh, A. K., Sorokin, A. V., Arslan, E., Ghosh, A. K., Schulz, J., Terranova, C. J., Jiang, S., Tang, M., et al. (2021) · Gut · doi:10.1136/gutjnl-2020-322835 · Cited by 71
BRD4 in physiology and pathology: ‘‘BET’’ on its partners
Liang, Y., Tian, J., & Wu, T. (2021) · BioEssays · doi:10.1002/bies.202100180 · Cited by 74
Recurrent integration of human papillomavirus genomes at transcriptional regulatory hubs
Warburton, A., Markowitz, T. E., Katz, J. P., Pipas, J. M., & McBride, A. A. (2021) · npj Genomic Medicine · doi:10.1038/s41525-021-00264-y · Cited by 72
Brd4 and HEXIM1: Multiple Roles in P-TEFb Regulation and Cancer
Chen, R., Yik, J. H. N., Lew, Q. J., & Chao, S. (2014) · BioMed Research International · doi:10.1155/2014/232870 · Cited by 72
The E3 ubiquitin ligase TRIM23 regulates adipocyte differentiation via stabilization of the adipogenic activator PPARγ
Watanabe, M., Takahashi, H., Saeki, Y., Ozaki, T. J., Itoh, S., Suzuki, M., Mizushima, W., Tanaka, K., & Hatakeyama, S. (2015) · eLife · doi:10.7554/elife.05615 · Cited by 71
BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members
Hogg, S. J., Newbold, A., Vervoort, S. J., Cluse, L. A., Martin, B. P., Gregory, G. P., Lefebure, M., Vidacs, E., Tothill, R. W., Bradner, J. E., et al. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-15-0924 · Cited by 76
Self-citation
Guidance of super-enhancers in regulation of IL-9 induction and airway inflammation
Xiao, X., Fan, Y., Li, J., Zhang, X., Lou, X., Dou, Y., Shi, X., Lan, P., Xiao, Y., Minze, L. J., et al. (2018) · The Journal of Experimental Medicine · doi:10.1084/jem.20170928 · Cited by 75
Enhancers: bridging the gap between gene control and human disease
Karnuta, J. M., & Scacheri, P. C. (2018) · Human Molecular Genetics · doi:10.1093/hmg/ddy167 · Cited by 77
GSK2801, a BAZ2/BRD9 Bromodomain Inhibitor, Synergizes with BET Inhibitors to Induce Apoptosis in Triple-Negative Breast Cancer
Bevill, S. M., Olivares-Quintero, J. F., Sciaky, N., Golitz, B. T., Singh, D., Beltrán, A. S., Rashid, N. U., Stuhlmiller, T. J., Hale, A., Moorman, N. J., et al. (2019) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-18-1121 · Cited by 70
The hyper-activation of transcriptional enhancers in breast cancer
Li, Q., Wang, D.-Y., Ju, L., Yao, J., Gao, C., Lei, P., Li, L., Zhao, X., & Wu, M. (2019) · Clinical Epigenetics · doi:10.1186/s13148-019-0645-x · Cited by 72
Targeting MYCN-expressing triple-negative breast cancer with BET and MEK inhibitors
Schafer, J. M., Lehmann, B. D., Ericsson, P. I. G., Marshall, C. B., Beeler, J. S., Redman, L. N., Jin, H., Sanchez, V. M., Stubbs, M. C., Scherle, P., et al. (2020) · Science Translational Medicine · doi:10.1126/scitranslmed.aaw8275 · Cited by 69
SEA version 3.0: a comprehensive extension and update of the Super-Enhancer archive
Chen, C., Zhou, D., Gu, Y., Wang, C., Zhang, M., Lin, X., Xing, J., Wang, H., & Zhang, Y. (2019) · Nucleic Acids Research · doi:10.1093/nar/gkz1028 · Cited by 67
The role of distinct BRD4 isoforms and their contribution to high-grade serous ovarian carcinoma pathogenesis
Drumond‐Bock, A. L., & Bieniasz, M. (2021) · Molecular Cancer · doi:10.1186/s12943-021-01424-5 · Cited by 71
BRD4 regulates Nanog expression in mouse embryonic stem cells and preimplantation embryos
Liu, W., Stein, P., Cheng, X., Yang, W., Shao, N.-Y., Morrisey, E. E., Schultz, R. M., & You, J. (2014) · Cell Death and Differentiation · doi:10.1038/cdd.2014.124 · Cited by 72
Inhibition of Bromodomain and Extraterminal Domain Family Proteins Ameliorates Experimental Renal Damage
Suárez-Álvarez, B., Morgado‐Pascual, J. L., Rayego‐Mateos, S., Rodríguez, R. M. A., Rodrigues-Díez, R. R., Cannata‐Ortiz, P., Sanz, A. B., Egido, J., Tharaux, P., Ortíz, A., et al. (2016) · Journal of the American Society of Nephrology · doi:10.1681/asn.2015080910 · Cited by 71
Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia
Peirs, S., Frismantas, V., Matthijssens, F., Loocke, W. V., Pieters, T., Vandamme, N., Lintermans, B., Dobay, M. P., Berx, G., Poppe, B. G., et al. (2017) · Leukemia · doi:10.1038/leu.2017.10 · Cited by 71
Nasopharyngeal carcinoma super-enhancer–driven ETV6 correlates with prognosis
Ke, L., Zhou, H., Wang, C., Xiong, G., Xiang, Y., Ling, Y., Khabir, A., Tsao, G. S., Zeng, Y., Zeng, M., et al. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1705236114 · Cited by 70
Genomic characterization of genes encoding histone acetylation modulator proteins identifies therapeutic targets for cancer treatment
Hu, Z., Zhou, J., Jiang, J., Yuan, J., Zhang, Y., Wei, X., Loo, N., Wang, Y., Pan, Y., Zhang, T., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-08554-x · Cited by 68
The anti-cancer drugs curaxins target spatial genome organization
Kantidze, O. L., Luzhin, A. V., Nizovtseva, E. V., Safina, A. F., Valieva, M. E., Golov, A. K., Velichko, A. K., Lyubitelev, A. V., Feofanov, A. V., Gurova, K. V., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-09500-7 · Cited by 73
Strategies to Overcome Resistance Mechanisms in T-Cell Acute Lymphoblastic Leukemia
Follini, E., Marchesini, M., & Roti, G. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20123021 · Cited by 73

Authors: Lovén, J., Hoke, H. A., Lin, C. Y., Lau, A., Orlando, D. A., Vakoc, C. R., Bradner, J. E., Lee, T. I., & Young, R. A.
Affiliations: Whitehead Institute for Biomedical Research (US)
Dana-Farber Cancer Institute (US)
Cold Spring Harbor Laboratory (US)
Harvard University (US)
Corresponding author: Young, Richard A.
ORCID: Lin, Charles Y.
Orlando, David A.
Vakoc, Christopher R.
Bradner, James E.
Lee, Tong Ihn
Young, Richard A.
Venue: Cell
Publisher: Elsevier BV
Published: 2013-04
Volume: 153
Issue: 2
Pages: 320-334
ISSN: 0092-8674 (ISSN-L)
DOI: 10.1016/j.cell.2013.03.036
PMC: PMC3760967
OpenAlex: W1523117612
Cited by: 2,961
References: 86
Citations by year: 2026: 140 · 2025: 214 · 2024: 261 · 2023: 254 · 2022: 271 · 2021: 327 · 2020: 263 · 2019: 248 · 2018: 218 · 2017: 205 · 2016: 184 · 2015: 175 · 2014: 143 · 2013: 53
FWCI: 83.08
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 375 d)
Locations: Cell (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Cold Spring Harbor Laboratory Institutional Repository (Cold Spring Harbor Laboratory) (submittedVersion)
DSpace@MIT (Massachusetts Institute of Technology) (submittedVersion, cc-by-nc)
Funders: National Institutes of Health (5p30ca045508-35)
National Human Genome Research Institute (HG002668, R01HG002668)
National Cancer Institute (CA146445, R01CA146445, P30-CA045508, CA45508, P30CA014051)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics and Chromatin Dynamics
Keywords: super-enhancers, BRD4, MYC oncogene, multiple myeloma, BET inhibitors, JQ1, Mediator complex, transcriptional coactivator, transcription elongation, chromatin regulators, cancer therapy, enhancer disruption
MeSH terms: Bromodomain Containing Proteins, Antineoplastic Agents, Azepines, Chromatin, Enhancer Elements, Genetic, Humans, Multiple Myeloma, Neoplasms, Nuclear Proteins, Transcription Factors, Transcription, Genetic, Triazoles, Gene Expression Regulation, Neoplastic, Cell Cycle Proteins, Cell Line, Tumor, Genome-Wide Association Study, Mediator Complex, Transcription Elongation, Genetic

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Self-check

Citations

Cites

Cited by

Related

Metadata

Record

About these checks