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Master Transcription Factors and Mediator Establish Super-Enhancers at Key Cell Identity Genes

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The landscape of somatic copy-number alteration across human cancers

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Epigenetics in Cancer

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Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13

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Phase separation of OCT4 controls TAD reorganization to promote cell fate transitions

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BET Epigenetic Reader Proteins in Cardiovascular Transcriptional Programs

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The Hierarchy of Transcriptional Activation: From Enhancer to Promoter

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BRD4 prevents the accumulation of R-loops and protects against transcription–replication collision events and DNA damage

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Browning of human adipocytes requires KLF11 and reprogramming of PPARγ superenhancersPreprint

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NSD3-Short Is an Adaptor Protein that Couples BRD4 to the CHD8 Chromatin Remodeler

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Enhancer Architecture and Essential Core Regulatory Circuitry of Chronic Lymphocytic Leukemia

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Aberrant Super‐Enhancer Landscape in Human Hepatocellular Carcinoma

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Transcriptional Programs Define Intratumoral Heterogeneity of Ewing Sarcoma at Single-Cell Resolution

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Downregulated METTL14 accumulates BPTF that reinforces super-enhancers and distal lung metastasis via glycolytic reprogramming in renal cell carcinoma

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Intratumoral Heterogeneity: From Diversity Comes Resistance

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The Role of Notch Receptors in Transcriptional Regulation

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Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

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Mammalian MYC Proteins and Cancer

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BACH2 immunodeficiency illustrates an association between super-enhancers and haploinsufficiency

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Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies

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Epstein-Barr Virus LMP1-Mediated Oncogenicity

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DOT1L inhibition reveals a distinct subset of enhancers dependent on H3K79 methylation

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Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models

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Dynamic control of chromatin-associated m6A methylation regulates nascent RNA synthesis

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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

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Beating the odds: BETs in disease

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Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle

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Kin28 regulates the transient association of Mediator with core promoters

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Epigenomic profiling of primary gastric adenocarcinoma reveals super-enhancer heterogeneity

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Multiple myeloma immunoglobulin lambda translocations portend poor prognosis

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KnockTF: a comprehensive human gene expression profile database with knockdown/knockout of transcription factors

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Safety and Efficacy of Bromodomain and Extra-Terminal Inhibitors for the Treatment of Hematological Malignancies and Solid Tumors: A Systematic Study of Clinical Trials

Sun, Y., Han, J., Wang, Z., Li, X., Sun, Y., & Hu, Z. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2020.621093 · Cited by 155

K27M in canonical and noncanonical H3 variants occurs in distinct oligodendroglial cell lineages in brain midline gliomas

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PRDM16 binds MED1 and controls chromatin architecture to determine a brown fat transcriptional programPreprint

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Histone demethylase KDM5D upregulation drives sex differences in colon cancer

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Noncanonical secondary structures arising from non-B DNA motifs are determinants of mutagenesis

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BET bromodomain proteins are required for glioblastoma cell proliferation

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Inhibition of Bromodomain Proteins for the Treatment of Human Diffuse Large B-cell Lymphoma

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Exploiting the Epigenome to Control Cancer-Promoting Gene-Expression Programs

Brien, G. L., Valerio, D. G., & Armstrong, S. A. (2016) · Cancer Cell · doi:10.1016/j.ccell.2016.03.007 · Cited by 155

Epigenetic regulation of epithelial–mesenchymal transition

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MLL4 Is Required to Maintain Broad H3K4me3 Peaks and Super-Enhancers at Tumor Suppressor Genes

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Cdk7: a kinase at the core of transcription and in the crosshairs of cancer drug discovery

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Chemical genomics reveals histone deacetylases are required for core regulatory transcription

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Transcriptional Control of Circadian Rhythms and Metabolism: A Matter of Time and Space

Kim, Y. H., & Lazar, M. A. (2020) · Endocrine Reviews · doi:10.1210/endrev/bnaa014 · Cited by 154

Editing the Epigenome: Reshaping the Genomic Landscape

Holtzman, L., & Gersbach, C. A. (2018) · Annual Review of Genomics and Human Genetics · doi:10.1146/annurev-genom-083117-021632 · Cited by 147

Reconstruction of the Global Neural Crest Gene Regulatory Network In Vivo

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The BET Protein BRD2 Cooperates with CTCF to Enforce Transcriptional and Architectural Boundaries

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Super-enhancer function and its application in cancer targeted therapy

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BET Inhibitors Suppress ALDH Activity by Targeting ALDH1A1 Super-Enhancer in Ovarian Cancer

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Super-Enhancer–Associated Long Noncoding RNA HCCL5 Is Activated by ZEB1 and Promotes the Malignancy of Hepatocellular Carcinoma

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BET Protein Antagonist JQ1 Is Synergistically Lethal with FLT3 Tyrosine Kinase Inhibitor (TKI) and Overcomes Resistance to FLT3-TKI in AML Cells Expressing FLT-ITD

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The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis

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The transcription factor NRSF contributes to epileptogenesis by selective repression of a subset of target genes

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Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Sheppard, G. S., Wang, L., Fidanze, S. D., Hasvold, L. A., Liu, D., Pratt, J. K., Park, C. H., Longenecker, K. L., Qiu, W., Torrent, M., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00628 · Cited by 140

Genome-wide analyses of chromatin interactions after the loss of Pol I, Pol II, and Pol III

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BiRen: predicting enhancers with a deep-learning-based model using the DNA sequence alone

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Defining super-enhancer landscape in triple-negative breast cancer by multiomic profiling

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Cancer and Aging - the Inflammatory Connection

Zinger, A., Cho, W. C. S., & Ben‐Yehuda, A. (2017) · Aging and Disease · doi:10.14336/ad.2016.1230 · Cited by 138

The essential and multifunctional TFIIH complex

Rimel, J. K., & Taatjes, D. J. (2018) · Protein Science · doi:10.1002/pro.3424 · Cited by 143

The role of epigenetics in the biology of multiple myeloma

Dimopoulos, K., Gimsing, P., & Grønbæk, K. (2014) · Blood Cancer Journal · doi:10.1038/bcj.2014.29 · Cited by 133

Molecular mechanisms of retroviral integration site selection

Kvaratskhelia, M., Sharma, A., Larue, R. C., Serrao, E., & Engelman, A. (2014) · Nucleic Acids Research · doi:10.1093/nar/gku769 · Cited by 150

The developmental origin of brain tumours: a cellular and molecular framework

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Transcriptional super-enhancers control cancer stemness and metastasis genes in squamous cell carcinoma

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Epigenetic remodelling shapes inflammatory renal cancer and neutrophil-dependent metastasis

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The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models

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BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor

Özer, H. G., El‐Gamal, D., Powell, B., Hing, Z. A., Blachly, J. S., Harrington, B. K., Mitchell, S. R., Grieselhuber, N. R., Williams, K., Lai, T.-H., et al. (2018) · Cancer Discovery · doi:10.1158/2159-8290.cd-17-0902 · Cited by 136

Super enhancer inhibitors suppress MYC driven transcriptional amplification and tumor progression in osteosarcoma

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Androgen Receptor Deregulation Drives Bromodomain-Mediated Chromatin Alterations in Prostate Cancer

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Selective Mediator dependence of cell-type-specifying transcription

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Superenhancer Analysis Defines Novel Epigenomic Subtypes of Non-APL AML, Including an RARα Dependency Targetable by SY-1425, a Potent and Selective RARα Agonist

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SCL/TAL1: a multifaceted regulator from blood development to disease

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KATs in cancer: functions and therapies

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KMT2D maintains neoplastic cell proliferation and global histone H3 lysine 4 monomethylation

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Super-Enhancers at the Nanog Locus Differentially Regulate Neighboring Pluripotency-Associated Genes

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Harnessing BET Inhibitor Sensitivity Reveals AMIGO2 as a Melanoma Survival Gene

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LncSEA: a platform for long non-coding RNA related sets and enrichment analysis

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Potent and selective bivalent inhibitors of BET bromodomains

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Advances in epigenetic therapeutics with focus on solid tumors

Jin, N. Y., George, T. L., Otterson, G. A., Verschraegen, C. F., Wen, H., Carbone, D. P., Herman, J. G., Bertino, E. M., & He, K. (2021) · Clinical Epigenetics · doi:10.1186/s13148-021-01069-7 · Cited by 135

The genetic regulatory signature of type 2 diabetes in human skeletal muscle

Scott, L. J., Erdos, M. R., Huyghe, J. R., Welch, R., Beck, A. T., Wolford, B. N., Chines, P. S., Didion, J. P., Narisu, N., Stringham, H. M., et al. (2016) · Nature Communications · doi:10.1038/ncomms11764 · Cited by 125

AMPK–ULK1-Mediated Autophagy Confers Resistance to BET Inhibitor JQ1 in Acute Myeloid Leukemia Stem Cells

Jang, J. E., Eom, J.-I., Jeung, H.-K., Cheong, J., Lee, J. Y., Kim, J. S., & Min, Y. H. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-1903 · Cited by 132

Chromatin landscapes reveal developmentally encoded transcriptional states that define human glioblastoma

Mack, S. C., Singh, I., Wang, X., Hirsch, R. A., Wu, Q., Villagomez, R., Bernatchez, J. A., Zhu, Z., Gimple, R. C., Kim, L. J. Y., et al. (2019) · The Journal of Experimental Medicine · doi:10.1084/jem.20190196 · Cited by 131

Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer

Zhang, H., Qi, J., Reyes, J. M., Li, L., Rao, P. K., Li, F., Lin, C. Y., Perry, J. A., Lawlor, M. A., Alexander Joel Federation, et al. (2016) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-0164 · Cited by 133

Targeting MYC in multiple myeloma

Jovanović, K., Roche‐Lestienne, C., Ghobrial, I. M., Facon, T. T. F., Quesnel, B., & Manier, S. (2018) · Leukemia · doi:10.1038/s41375-018-0036-x · Cited by 133

Bivalent Regions of Cytosine Methylation and H3K27 Acetylation Suggest an Active Role for DNA Methylation at Enhancers

Charlet, J., Duymich, C. E., Lay, F. D., Mundbjerg, K., Dalsgaard Sørensen, K., Liang, G., & Jones, P. A. (2016) · Molecular Cell · doi:10.1016/j.molcel.2016.03.033 · Cited by 128

Triplication of a 21q22 region contributes to B cell transformation through HMGN1 overexpression and loss of histone H3 Lys27 trimethylation

Lane, A. A., Chapuy, B., Lin, C. Y., Tivey, T. R., Li, H., Townsend, E. C., van Bodegom, D., Day, T. A., Wu, S.-C., Liu, H., et al. (2014) · Nature Genetics · doi:10.1038/ng.2949 · Cited by 134

Synergistic action of master transcription factors controls epithelial-to-mesenchymal transition

Chang, H., Liu, Y., Xue, M., Liu, H., Du, S., Zhang, L., & Wang, P. (2016) · Nucleic Acids Research · doi:10.1093/nar/gkw126 · Cited by 126

The transcriptional regulator Aire binds to and activates super-enhancers

Bansal, K., Yoshida, H., Benoist, C. O., & Mathis, D. J. (2017) · Nature Immunology · doi:10.1038/ni.3675 · Cited by 127

Common nonmutational NOTCH1 activation in chronic lymphocytic leukemia

Fabbri, G., Holmes, A. B., Viganotti, M., Scuoppo, C., Belver, L., Herranz, D., Yan, X., Kieso, Y., Rossi, D., Gaïdano, G., et al. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1702564114 · Cited by 128

Lkb1 inactivation drives lung cancer lineage switching governed by Polycomb Repressive Complex 2

Zhang, H., Fillmore Brainson, C., Koyama, S., Redig, A. J., Chen, T., Li, S., Gupta, M., Garcia-de-Alba, C., Paschini, M., Herter-Sprie, G. S., et al. (2017) · Nature Communications · doi:10.1038/ncomms14922 · Cited by 127

Somatic Superenhancer Duplications and Hotspot Mutations Lead to Oncogenic Activation of the KLF5 Transcription Factor

Zhang, X., Choi, P. S., Francis, J. M., Gao, G. F., Campbell, J. D., Ramachandran, A., Mitsuishi, Y., Ha, G., Shih, J., Vázquez, F., et al. (2017) · Cancer Discovery · doi:10.1158/2159-8290.cd-17-0532 · Cited by 126

STAT3 Interactors as Potential Therapeutic Targets for Cancer Treatment

Laudisi, F., Cherubini, F., Monteleone, G., & Stolfi, C. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19061787 · Cited by 133

Targeting the HTLV-I-Regulated BATF3/IRF4 Transcriptional Network in Adult T Cell Leukemia/Lymphoma

Nakagawa, M., Shaffer, A. L., Ceribelli, M., Zhang, M., Wright, G. W., Huang, D. W., Xiao, W., Powell, J. I., Petrus, M. N., Yang, Y., et al. (2018) · Cancer Cell · doi:10.1016/j.ccell.2018.06.014 · Cited by 129

Bromodomains and Their Pharmacological Inhibitors

Gallenkamp, D., Gelato, K. A., Haendler, B., & Weinmann, H. (2014) · ChemMedChem · doi:10.1002/cmdc.201300434 · Cited by 129

Role of Epigenetics in Cardiac Development and Congenital Diseases

Moore‐Morris, T., Vliet, P. P. V., Andelfinger, G., & Pucéat, M. (2018) · Physiological Reviews · doi:10.1152/physrev.00048.2017 · Cited by 133

BRD4 directs hematopoietic stem cell development and modulates macrophage inflammatory responses

Dey, A., Yang, W., Gégonne, A., Nishiyama, A., Pan, R., Yagi, R., Grinberg, A., Finkelman, F. D., Pfeifer, K. E., Zhu, J., et al. (2019) · The EMBO Journal · doi:10.15252/embj.2018100293 · Cited by 128

Lactate controls cancer stemness and plasticity through epigenetic regulation

Nguyen, N. B., Gevers, S., Kok, R. N. U., Burgering, L. M., Neikes, H. K., Akkerman, N., Betjes, M. A., Ludikhuize, M. C., Gulersonmez, C. M. C., Stigter, E. C. A., et al. (2025) · Cell Metabolism · doi:10.1016/j.cmet.2025.01.002 · Cited by 135

Detection of Enhancer-Associated Rearrangements Reveals Mechanisms of Oncogene Dysregulation in B-cell Lymphoma

Ryan, R. J. H., Drier, Y., Whitton, H. J., Cotton, M. J., Kaur, J., Issner, R., Gillespie, S. M., Epstein, C. B., Nardi, V., Sohani, A. R., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0370 · Cited by 127

Integrative analysis of public ChIP-seq experiments reveals a complex multi-cell regulatory landscape

Griffon, A., Barbier, Q., Dalino, J., van Helden, J., Spicuglia, S., & Ballester, B. (2014) · Nucleic Acids Research · doi:10.1093/nar/gku1280 · Cited by 126

A chemical toolbox for the study of bromodomains and epigenetic signaling

Wu, Q., Heidenreich, D. J., Zhou, S., Ackloo, S. Z., Krämer, A., Nakka, K. K., Lima‐Fernandes, E., Deblois, G., Duan, S., Vellanki, R. N., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-09672-2 · Cited by 124

Regulatory functions of the Mediator kinases CDK8 and CDK19

Fant, C. B., & Taatjes, D. J. (2018) · Transcription · doi:10.1080/21541264.2018.1556915 · Cited by 131

Epigenetic polypharmacology: A new frontier for epi‐drug discovery

Tomaselli, D., Lucidi, A., Rotili, D., & Mai, A. (2019) · Medicinal Research Reviews · doi:10.1002/med.21600 · Cited by 131

Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins

Shirasaki, R., Matthews, G. M., Gandolfi, S., de Matos Simoes, R., Buckley, D. L., Raja Vora, J., Sievers, Q. L., Brüggenthies, J. B., Dashevsky, O., Poarch, H., et al. (2021) · Cell Reports · doi:10.1016/j.celrep.2020.108532 · Cited by 123

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Bui, M. H., Li, X., Albert, D. H., Li, L., Lam, L. T., Faivre, E. J., Warder, S. E., Huang, X., Wilcox, D. M., Donawho, C. K., et al. (2017) · Cancer Research · doi:10.1158/0008-5472.can-16-1793 · Cited by 124

Super-enhancers and the super-enhancer reader BRD4: tumorigenic factors and therapeutic targets

Qian, H., Zhu, M., Tan, X., Zhang, Y., Liu, X., & Yang, L. (2023) · Cell Death Discovery · doi:10.1038/s41420-023-01775-6 · Cited by 106

Enhancer Deregulation in Myeloma

Neri, P. E. (2018) · Blood · doi:10.1182/blood-2018-99-109523 · Cited by 1

Disruption of BRD4 at H3K27Ac-enriched enhancer region correlates with decreased c-Myc expression in Merkel cell carcinoma

Sengupta, D., Kannan, A., Kern, M., Moreno, M. A., Vural, E. A., Stack, B. C., Suen, J. Y., Tackett, A. J., & Gao, L. (2015) · Epigenetics · doi:10.1080/15592294.2015.1034416 · Cited by 87

Oncogenic super-enhancers in cancer: mechanisms and therapeutic targets

Bacabac, M. S., & Xu, W. (2023) · Cancer and Metastasis Reviews · doi:10.1007/s10555-023-10103-4 · Cited by 41

Abstract 2498: Over-expression of dual-specificity phosphatase 4 (DUSP4) in multiple myeloma

Xia, T., Lau, K., Cheng, C. K., Chan, N. C. N., & Ng, M. H. L. (2018) · Cancer Research · doi:10.1158/1538-7445.am2018-2498 · Cited by 2