Selective inhibition of BET bromodomains

Efficacy and Safety of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in Chronic Myeloid Leukemia

Druker, B. J., Talpaz, M., Resta, D. J., Peng, B., Buchdunger, E., Ford, J., Lydon, N., Kantarjian, H. M., Capdeville, R., Ohno-Jones, S., et al. (2001) · New England Journal of Medicine · doi:10.1056/nejm200104053441401 · Cited by 5,237

Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr–Abl positive cells

Druker, B. J., Tamura, S., Buchdunger, E., Ohno-Jones, S., Segal, G. M., Fanning, S., Zimmermann, J., & Lydon, N. (1996) · Nature Medicine · doi:10.1038/nm0596-561 · Cited by 3,652

Use of all-trans retinoic acid in the treatment of acute promyelocytic leukemia

Huang, M., Ye, Y., Chen, S. R., Chai, J., Lu, J., Zhoa, L., Gu, L.-J., & Wang, Z.-Y. (1988) · Blood · doi:10.1182/blood.v72.2.567.567 · Cited by 2,445

The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability

Niesen, F., Berglund, H., & Vedadi, M. (2007) · Nature Protocols · doi:10.1038/nprot.2007.321 · Cited by 2,420

Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine Kinase

Schindler, T. H., Bornmann, W. G., Pellicena, P., Miller, W. T., Clarkson, B., & Kuriyan, J. (2000) · Science · doi:10.1126/science.289.5486.1938 · Cited by 1,785

c-Myc Regulates Transcriptional Pause Release

Rahl, P. B., Lin, C. Y., Seila, A. C., Flynn, R. A., McCuine, S., Burge, C. B., Sharp, P. A., & Young, R. A. (2010) · Cell · doi:10.1016/j.cell.2010.03.030 · Cited by 1,279

Recruitment of P-TEFb for Stimulation of Transcriptional Elongation by the Bromodomain Protein Brd4

Yang, Z., Yik, J. H. N., Chen, R., He, N., Jang, M. K., Ozato, K., & Zhou, Q. (2005) · Molecular Cell · doi:10.1016/j.molcel.2005.06.029 · Cited by 1,141

Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative.

Buchdunger, E., Zimmermann, J., Mett, H., Meyer, T., Müller, M., Druker, B. J., & Lydon, N. (1996) · PubMed · Cited by 1,057

Bromodomain: an acetyl‐lysine binding domain

Zeng, L., & Zhou, M. (2002) · FEBS Letters · doi:10.1016/s0014-5793(01)03309-9 · Cited by 751

Super-enhancers in cancer

Thandapani, P. (2019) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2019.02.014 · Cited by 167

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies

Rhyasen, G. W., Hattersley, M. M., Yao, Y., Dulak, A. M., Wang, W., Petteruti, P., Dale, I. L., Boiko, S., Cheung, T., Zhang, J., et al. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0141 · Cited by 166

Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer

He, S., Dong, G., Li, Y., Wu, S., Wang, W., & Sheng, C. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.201915896 · Cited by 166

Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression

Gacias, M., Gerona‐Navarro, G., Plotnikov, A. N., Zhang, G., Zeng, L., Kaur, J., Moy, G. A., Rusinova, E. V., Rodrı́guez, Y., Matikainen, B., et al. (2014) · Chemistry & Biology · doi:10.1016/j.chembiol.2014.05.009 · Cited by 165

Harnessing the potential of epigenetic therapy to target solid tumors

Ahuja, N., Easwaran, H., & Baylin, S. B. (2014) · Journal of Clinical Investigation · doi:10.1172/jci69736 · Cited by 165

Genome-wide Profiling Reveals Remarkable Parallels Between Insertion Site Selection Properties of the MLV Retrovirus and the piggyBac Transposon in Primary Human CD4+ T Cells

Gogol‐Döring, A., Ammar, I., Gupta, S., Bunse, M., Miskey, C., Chen, W., Uckert, W., Schulz, T. F., Izsvák, Z., & Ivics, Z. (2016) · Molecular Therapy · doi:10.1038/mt.2016.11 · Cited by 165

Brd4 and P300 Confer Transcriptional Competency during Zygotic Genome Activation

Chan, S. H., Tang, Y., Miao, L., Darwich‐Codore, H., Vejnar, C. E., Beaudoin, J.-D., Musaev, D., Fernández, J. P., Benitez, M. D. J., Bazzini, A., et al. (2019) · Developmental Cell · doi:10.1016/j.devcel.2019.05.037 · Cited by 165

Epigenetic modifications by dietary phytochemicals: Implications for personalized nutrition

Shankar, S., Kumar, D., & Srivastava, R. K. (2012) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2012.11.002 · Cited by 164

Affinity Map of Bromodomain Protein 4 (BRD4) Interactions with the Histone H4 Tail and the Small Molecule Inhibitor JQ1

Jung, M., Philpott, M., Müller, S., Schulze, J., Badock, V., Eberspächer, U., Moosmayer, D., Bader, B., Schmees, N., Fernández‐Montalván, A. E., et al. (2014) · Journal of Biological Chemistry · doi:10.1074/jbc.m113.523019 · Cited by 164

A Druggable TCF4- and BRD4-Dependent Transcriptional Network Sustains Malignancy in Blastic Plasmacytoid Dendritic Cell Neoplasm

Ceribelli, M., Hou, E. Z., Kelly, P. N., Huang, D. W., Wright, G. W., Ganapathi, K. A., Evbuomwan, M. O., Pittaluga, S., Shaffer, A. L., Marcucci, G., et al. (2016) · Cancer Cell · doi:10.1016/j.ccell.2016.10.002 · Cited by 164

Epigenetic drug discovery: breaking through the immune barrier

Tough, D. F., Tak, P. P., Tarakhovsky, A., & Prinjha, R. K. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.185 · Cited by 163

Emerging degrader technologies engaging lysosomal pathways

Ding, Y., Xing, D., Fei, Y., & Lu, B. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00624c · Cited by 165

BET Bromodomain Inhibitors Enhance Efficacy and Disrupt Resistance to AR Antagonists in the Treatment of Prostate Cancer

Asangani, I. A., Wilder-Romans, K., Dommeti, V. L., Krishnamurthy, P. M., Apel, I. J., Escara-Wilke, J. F., Plymate, S. R., Navone, N. M., Wang, S., Feng, F. Y.-C., et al. (2016) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-15-0472 · Cited by 162

1,4,9-Triazaspiro[5.5]undecan-2-one Derivatives as Potent and Selective METTL3 Inhibitors

Dolbois, A., Bedi, R. K., Bochenkova, E., Müller, A., Moroz, E., Danzhi Huang, A., & Caflisch, A. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00773 · Cited by 162

Positively selected enhancer elements endow osteosarcoma cells with metastatic competence

Morrow, J. J., Bayles, I., Funnell, A. P. W., Miller, T. E., Saiakhova, A., Lizardo, M. M., Bartels, C. F., Kapteijn, M. Y., Hung, S., Mendoza, A., et al. (2018) · Nature Medicine · doi:10.1038/nm.4475 · Cited by 161

Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

Martin, M. P., Olesen, S. H., Georg, G. I., & Schönbrunn, E. (2013) · ACS Chemical Biology · doi:10.1021/cb4003283 · Cited by 161

First-in-Human Study of Mivebresib (ABBV-075), an Oral Pan-Inhibitor of Bromodomain and Extra Terminal Proteins, in Patients with Relapsed/Refractory Solid Tumors

Piha-Paul, S. A., Sachdev, J. C., Barve, M. A., LoRusso, P. M., Szmulewitz, R. Z., Patel, S. P., Lara, P. N., Chen, X., Hu, B., Freise, K. J., et al. (2019) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-19-0578 · Cited by 161

Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications

Goracci, L., Desantis, J., Valeri, A., Castellani, B., Eleuteri, M., & Cruciani, G. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00793 · Cited by 161

Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy

Wanior, M., Krämer, A., Knapp, S., & Joerger, A. C. (2021) · Oncogene · doi:10.1038/s41388-021-01781-x · Cited by 162

Small-molecule inhibitors of the Myc oncoprotein

Fletcher, S., & Prochownik, E. V. (2014) · Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms · doi:10.1016/j.bbagrm.2014.03.005 · Cited by 160

c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells

Roderick, J. E., Tesell, J., Shultz, L. D., Brehm, M. A., Greiner, D. L., Harris, M. H., Silverman, L. B., Sallan, S. E., Gutiérrez, A., Look, A. T., et al. (2014) · Blood · doi:10.1182/blood-2013-08-522698 · Cited by 160

The role of osteoclast differentiation and function in skeletal homeostasis

Ikeda, K., & Takeshita, S. (2015) · The Journal of Biochemistry · doi:10.1093/jb/mvv112 · Cited by 160

The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer

da Motta, L. L., Ledaki, I., Purshouse, K. R., Haider, S. A., Bastiani, M. A. D., Baban, D., Morotti, M., Steers, G., Wigfield, S., Bridges, E., et al. (2016) · Oncogene · doi:10.1038/onc.2016.184 · Cited by 160

Design and characterization of bivalent BET inhibitors

Tanaka, M., Roberts, J. M., Seo, H., Souza, A., Paulk, J., Scott, T. G., DeAngelo, S. L., Dhe‐Paganon, S., & Bradner, J. E. (2016) · Nature Chemical Biology · doi:10.1038/nchembio.2209 · Cited by 160

Longitudinal single-cell RNA sequencing of patient-derived primary cells reveals drug-induced infidelity in stem cell hierarchy

Sharma, A., Cao, E. Y., Kumar, V., Zhang, X., Leong, H. S., Wong, A. M. L., Ramakrishnan, N., Hakimullah, M., Teo, H. M. V., Chong, F. T., et al. (2018) · Nature Communications · doi:10.1038/s41467-018-07261-3 · Cited by 159

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

Lam, F. C., Kong, Y. W., Huang, Q., Vu‐Han, T., Maffa, A., Kasper, E. M., & Yaffe, M. B. (2020) · Nature Communications · doi:10.1038/s41467-020-17503-y · Cited by 159

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

Shen, C., Ipsaro, J. J., Shi, J., Milazzo, J. P., Wang, E., Roe, J., Suzuki, Y., Pappin, D., Joshua‐Tor, L., & Vakoc, C. R. (2015) · Molecular Cell · doi:10.1016/j.molcel.2015.10.033 · Cited by 158

Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta

Bai, N., Miller, S. A., Andrianov, G. V., Yates, M., Kirubakaran, P., & Karanicolas, J. (2021) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c01451 · Cited by 157

Exploring Cellular Interactions of Liposomes Using Protein Corona Fingerprints and Physicochemical Properties

Bigdeli, A., Palchetti, S., Pozzi, D., Hormozi-Nezhad, M. R., Baldelli Bombelli, F., Caracciolo, G., & Mahmoudi, M. (2016) · ACS Nano · doi:10.1021/acsnano.6b00261 · Cited by 157

Cancer epigenetics drug discovery and development: the challenge of hitting the mark

Campbell, R. M., & Tummino, P. J. (2014) · Journal of Clinical Investigation · doi:10.1172/jci71605 · Cited by 157

Beating the odds: BETs in disease

Wang, C., & Filippakopoulos, P. (2015) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2015.06.002 · Cited by 156

Targeted protein degradation: current and future challenges

Hanzl, A., & Winter, G. E. (2020) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2019.11.012 · Cited by 157

Brg1 promotes both tumor-suppressive and oncogenic activities at distinct stages of pancreatic cancer formation

Roy, N., Malik, S., Villanueva, K. E., Urano, A., Lu, X., Von Figura, G., Seeley, E. S., Dawson, D. W., Collisson, E. A., & Hebrok, M. (2015) · Genes & Development · doi:10.1101/gad.256628.114 · Cited by 155

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

Meeting the Challenge of Targeting Cancer Stem Cells

Turdo, A., Veschi, V., Gaggianesi, M., Chinnici, A., Bianca, P., Todaro, M., & Stassi, G. (2019) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2019.00016 · Cited by 155

Understanding histone H3 lysine 36 methylation and its deregulation in disease

Li, J., Ahn, J. H., & Wang, G. G. (2019) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-019-03144-y · Cited by 155

BET Epigenetic Reader Proteins in Cardiovascular Transcriptional Programs

Borck, P. C., Guo, L., & Plutzky, J. (2020) · Circulation Research · doi:10.1161/circresaha.120.315929 · Cited by 155

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

Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation

Wei, J., Meng, F., Park, K.-S., Yim, H., Velez, J., Kumar, P., Wang, L., Xie, L., Chen, H., Shen, Y., et al. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.1c04841 · Cited by 154

Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions

Laraia, L., McKenzie, G. J., Spring, D. R., Venkitaraman, A. R., & Huggins, D. J. (2015) · Chemistry & Biology · doi:10.1016/j.chembiol.2015.04.019 · Cited by 154

NUT Midline Carcinomas of the Sinonasal Tract

Bishop, J. A., & Westra, W. H. (2012) · The American Journal of Surgical Pathology · doi:10.1097/pas.0b013e318254ce54 · Cited by 154

Epigenetic polypharmacology: from combination therapy to multitargeted drugs

de Lera, Á. R., & Ganesan, A. (2016) · Clinical Epigenetics · doi:10.1186/s13148-016-0271-9 · Cited by 154

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

Godfrey, L., Crump, N. T., Thorne, R., Lau, I., Repapi, E., Dimou, D., Smith, A., Harman, J. R., Telenius, J. M., Oudelaar, A. M., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-10844-3 · Cited by 154

Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway

Ottis, P., Palladino, C., Thienger, P., Britschgi, A., Heichinger, C., Berrera, M., Julien-Laferrière, A., Roudnicky, F., Kam‐Thong, T., Bischoff, J. R., et al. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.9b00525 · Cited by 154

Epigenetic regulator BRD4 is involved in cadmium-induced acute kidney injury via contributing to lysosomal dysfunction, autophagy blockade and oxidative stress

Gong, Z., Zhao, Y., Wang, Z., Fan, R., Liu, Z., & Wang, L. (2021) · Journal of Hazardous Materials · doi:10.1016/j.jhazmat.2021.127110 · Cited by 154

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

Chan, S. C., Selth, L. A., Li, Y., Nyquist, M. D., Lu, M., Bradner, J. E., Raj, G. V., Tilley, W. D., & Dehm, S. M. (2015) · Nucleic Acids Research · doi:10.1093/nar/gkv262 · Cited by 153

Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity

Klein, V. G., Bond, A. G., Craigon, C., Lokey, R. S., & Ciulli, A. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01496 · Cited by 152

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Dragovich, P. S., Pillow, T. H., Blake, R. A., Sadowsky, J. D., Adaligil, E., Adhikari, P., Bhakta, S., Blaquiere, N., Chen, J., dela Cruz-Chuh, J., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01845 · Cited by 152

A Comprehensive Patient-Derived Xenograft Collection Representing the Heterogeneity of Melanoma

Krepler, C., Sproesser, K., Brafford, P. A., Beqiri, M., Garman, B., Xiao, M., Shannan, B., Watters, A. K., Perego, M., Zhang, G., et al. (2017) · Cell Reports · doi:10.1016/j.celrep.2017.10.021 · Cited by 152

Enhancer Architecture and Essential Core Regulatory Circuitry of Chronic Lymphocytic Leukemia

Ott, C. J., Alexander Joel Federation, Schwartz, L. S., Kasar, S. N., Klitgaard, J. L., Lenci, R., Li, Q., Lawlor, M. A., Fernandes, S. M., Souza, A., et al. (2018) · Cancer Cell · doi:10.1016/j.ccell.2018.11.001 · Cited by 152

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

Single-Molecule Nanoscopy Elucidates RNA Polymerase II Transcription at Single Genes in Live Cells

Li, J., Dong, A., Saydaminova, K., Chang, H., Wang, G., Ochiai, H., Yamamoto, T., & Pertsinidis, A. (2019) · Cell · doi:10.1016/j.cell.2019.05.029 · Cited by 152

Bardoxolone conjugation enables targeted protein degradation of BRD4

Tong, B., Luo, M., Xie, Y., Spradlin, J. N., Tallarico, J. A., McKenna, J. M., Schirle, M., Maimone, T. J., & Nomura, D. K. (2020) · Scientific Reports · doi:10.1038/s41598-020-72491-9 · Cited by 152

BET bromodomain protein inhibition is a therapeutic option for medulloblastoma

Henssen, A. G., Thor, T., Odersky, A., Heukamp, L. C., Hindy, N. E., Beckers, A., Speleman, F., Althoff, K., Schäfers, S., Schramm, A. R., et al. (2013) · Oncotarget · doi:10.18632/oncotarget.1534 · Cited by 150

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

Lamoureux, F., Baud’huin, M., Calleja, L. R., Jacques, C., Berreur, M., Rédiní, F., Lecanda, F., Bradner, J. E., Heymann, D., & Ory, B. (2014) · Nature Communications · doi:10.1038/ncomms4511 · Cited by 150

Mission Possible: Advances in MYC Therapeutic Targeting in Cancer

Allen-Petersen, B. L., & Sears, R. C. (2019) · BioDrugs · doi:10.1007/s40259-019-00370-5 · Cited by 150

A chromatin link to caste identity in the carpenter ant Camponotus floridanusPreprint

Simola, D. F., Ye, C., Mutti, N. S., Dolezal, K., Bonasio, R., Liebig, J., Reinberg, D., & Berger, S. L. (2012) · Genome Research · doi:10.1101/gr.148361.112 · Cited by 150

A quantitative atlas of histone modification signatures from human cancer cells

LeRoy, G., DiMaggio, P. A., Chan, E. Y., Zee, B. M., Blanco, M. A., Bryant, B. M., Flaniken, I. Z., Liu, S., Kang, Y., Trojer, P., et al. (2013) · Epigenetics & Chromatin · doi:10.1186/1756-8935-6-20 · Cited by 149

Epigenetic regulation of epithelial–mesenchymal transition

Sun, L., & Fang, J. (2016) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-016-2303-1 · Cited by 149

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

Berenguer‐Daizé, C., Astorgues‐Xerri, L., Odore, E., Cayol, M., Cvitkovic, E., Noel, K., Békradda, M., MacKenzie, S., Rezaï, K., Lokiec, F. M., et al. (2016) · International Journal of Cancer · doi:10.1002/ijc.30256 · Cited by 149

Template-assisted covalent modification underlies activity of covalent molecular glues

Li, Y.-D., Ma, M. W., Hassan, M. M., Hunkeler, M., Teng, M., Puvar, K., Rutter, J. C., Lumpkin, R. J., Sandoval, B., Jin, C. Y., et al. (2024) · Nature Chemical Biology · doi:10.1038/s41589-024-01668-4 · Cited by 153

BRD4 Promotes DNA Repair and Mediates the Formation of TMPRSS2-ERG Gene Rearrangements in Prostate Cancer

Li, X., Baek, G., Ramanand, S. G., Sharp, A., Gao, Y., Yuan, W., Welti, J., Rodrigues, D. N., Dolling, D., Figueiredo, I., et al. (2018) · Cell Reports · doi:10.1016/j.celrep.2017.12.078 · Cited by 148

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

Trabucco, S. E., Gerstein, R. M., Evens, A. M., Bradner, J. E., Shultz, L. D., Greiner, D. L., & Zhang, H. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-3346 · Cited by 148

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

McDaniel, K. F., Wang, L., Soltwedel, T., Fidanze, S. D., Hasvold, L. A., Liu, D., Mantei, R. A., Pratt, J. K., Sheppard, G. S., Bui, M. H., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00746 · Cited by 148

T-cell Acute Lymphoblastic Leukemia: A Roadmap to Targeted Therapies

Cordo’, V., van der Zwet, J. C. G., Canté-Barrett, K., Pieters, R., & Meijerink, J. P. P. (2020) · Blood Cancer Discovery · doi:10.1158/2643-3230.bcd-20-0093 · Cited by 148

BET bromodomain proteins are required for glioblastoma cell proliferation

Pastori, C., Daniel, M. L., Penas, C., Volmar, C., Johnstone, A. L., Brothers, S. P., Graham, R. M., Allen, B. K., Sarkaria, J. N., Komotar, R. J., et al. (2014) · Epigenetics · doi:10.4161/epi.27906 · Cited by 147

Multiple myeloma immunoglobulin lambda translocations portend poor prognosis

Barwick, B. G., Neri, P. E., Bahlis, N. J., Nooka, A. K., Dhodapkar, M. V., Jaye, D. L., Hofmeister, C. C., Kaufman, J. L., Gupta, V. A., Auclair, D., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-09555-6 · Cited by 147

Targeting regulated cell death (RCD) with small-molecule compounds in triple-negative breast cancer: a revisited perspective from molecular mechanisms to targeted therapies

Liao, M., Qin, R., Huang, W., Zhu, H.-P., Peng, F., Han, B., & Liu, B. (2022) · Journal of Hematology & Oncology · doi:10.1186/s13045-022-01260-0 · Cited by 149

Characteristic roadmap of linker governs the rational design of PROTACs

Dong, Y., Ma, T., Xu, T., Feng, Z., Li, Y., Song, L., Yao, X., Ashby, C. R., & Hao, G.-F. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.04.007 · Cited by 146

Chemical genomics reveals histone deacetylases are required for core regulatory transcription

Gryder, B. E., Wu, L., Woldemichael, G. M., Pomella, S., Quinn, T. R., Park, P. M. C., Cleveland, A. H., Stanton, B. Z., Song, Y., Rota, R., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-11046-7 · Cited by 146

A proteome-wide atlas of drug mechanism of action

Mitchell, D. C., Kuljanin, M., Li, J., Vranken, J. G. V., Bulloch, N. J., Schweppe, D. K., Huttlin, E. L., & Gygi, S. P. (2023) · Nature Biotechnology · doi:10.1038/s41587-022-01539-0 · Cited by 146

BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction

Meng, S., Zhang, L., Tang, Y., Tu, Q., Zheng, L., Yu, L., Murray, D., Cheng, J., Kim, S., Zhou, X., et al. (2014) · Journal of Dental Research · doi:10.1177/0022034514534261 · Cited by 145

Isothermal Analysis of ThermoFluor Data can readily provide Quantitative Binding Affinities

Bai, N., Röder, H., Dickson, A., & Karanicolas, J. (2019) · Scientific Reports · doi:10.1038/s41598-018-37072-x · Cited by 145

Super-enhancer function and its application in cancer targeted therapy

Tang, F., Yang, Z., Tan, Y., & Li, Y. (2020) · npj Precision Oncology · doi:10.1038/s41698-020-0108-z · Cited by 145

Targeting HIV latency: pharmacologic strategies toward eradication

Xing, S., & Siliciano, R. F. (2012) · Drug Discovery Today · doi:10.1016/j.drudis.2012.12.008 · Cited by 144

A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

Baud, M. G. J., Lin-Shiao, E., Cardote, T. A. F., Tallant, C., Pschibul, A., Chan, K.-H., Zengerle, M., Garcia, J. R., Kwan, T. T.-L., Ferguson, F. M., et al. (2014) · Science · doi:10.1126/science.1249830 · Cited by 144

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

Fedorov, O., Castex, J., Tallant, C., Owen, D. R., Martin, S., Aldeghi, M., Monteiro, O., Filippakopoulos, P., Picaud, S., Trzupek, J. D., et al. (2015) · Science Advances · doi:10.1126/sciadv.1500723 · Cited by 144

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

Yokoyama, Y., Zhu, H., Lee, J., Kossenkov, A. V., Wu, S. Y., Wickramasinghe, J. M., Yin, X., Palozola, K. C., Gardini, A., Showe, L. C., et al. (2016) · Cancer Research · doi:10.1158/0008-5472.can-16-0854 · Cited by 144

YAP/TAZ Initiates Gastric Tumorigenesis via Upregulation of MYC

Choi, W., Kim, J., Park, J., Lee, D.-H., Hwang, D., Kim, J., Ashktorab, H., Smoot, D. T., Kim, S., Choi, C., et al. (2018) · Cancer Research · doi:10.1158/0008-5472.can-17-3487 · Cited by 144

The Design and Application of Target-Focused Compound Libraries

Harris, C. J., Hill, R. D., Sheppard, D. W., Slater, M. J., & Stouten, P. F. W. (2011) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/138620711795767802 · Cited by 144

MYC Is a Major Determinant of Mitotic Cell Fate

Topham, C. H., Tighe, A., Ly, P., Bennett, A., Sloss, O., Nelson, L., Ridgway, R. A., Huels, D. J., Littler, S., Schandl, C., et al. (2015) · Cancer Cell · doi:10.1016/j.ccell.2015.06.001 · Cited by 144

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

Hsu, S. C., Gilgenast, T. G., Bartman, C., Edwards, C. R., Stonestrom, A. J., Huang, P., Emerson, D. J., Evans, P., Werner, M. T., Keller, C. A., et al. (2017) · Molecular Cell · doi:10.1016/j.molcel.2017.02.027 · Cited by 143

Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation

Cheung, K. L., Zhang, F., Jaganathan, A., Sharma, R., Zhang, Q., Konuma, T., Shen, T., Lee, J., Ren, C., Chen, C., et al. (2017) · Molecular Cell · doi:10.1016/j.molcel.2016.12.022 · Cited by 143

The impact of epigenetics on cardiovascular disease

Prasher, D., Greenway, S. C., & Singh, R. B. (2019) · Biochemistry and Cell Biology · doi:10.1139/bcb-2019-0045 · Cited by 143

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

Garcia, P. L., Miller, A. L., Kreitzburg, K. M., Gamblin, T. L., Christein, J. D., Heslin, M. J., Arnoletti, J. P., Richardson, J. H., Chen, D., Hanna, C. A., et al. (2015) · Oncogene · doi:10.1038/onc.2015.126 · Cited by 141

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

Hewings, D. S., Fedorov, O., Filippakopoulos, P., Martin, S., Picaud, S., Tumber, A., Wells, C. D., Olcina, M. M., Freeman, K. M., Gill, A., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm301588r · Cited by 141

Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulation

Park‐Min, K., Lim, E., Lee, M. J., Park, S. H., Γιαννοπούλου, Ε., Yarilina, A., van der Meulen, M. C. H., Zhao, B., Smithers, N. N., Witherington, J. J., et al. (2014) · Nature Communications · doi:10.1038/ncomms6418 · Cited by 141

Chromatin remodelling drives immune cell–fibroblast communication in heart failure

Alexanian, M., Padmanabhan, A., Nishino, T., Travers, J. G., Ye, L., Pelonero, A., Lee, C. Y., Sadagopan, N., Huang, Y., Auclair, K., et al. (2024) · Nature · doi:10.1038/s41586-024-08085-6 · Cited by 140

Histone Regulation in the CNS: Basic Principles of Epigenetic Plasticity

Maze, I. S., Noh, K., & Allis, C. D. (2012) · Neuropsychopharmacology · doi:10.1038/npp.2012.124 · Cited by 140

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

Philpott, M., Yang, J., Tumber, T., Fedorov, O., Uttarkar, S., Filippakopoulos, P., Picaud, S., Keates, T., Felletár, I., Ciulli, A., et al. (2011) · Molecular BioSystems · doi:10.1039/c1mb05099k · Cited by 140

NUT midline carcinoma

French, C. A. (2014) · Nature reviews. Cancer · doi:10.1038/nrc3659 · Cited by 140

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

Fiskus, W. C., Sharma, S., Qi, J., Shah, B., Devaraj, S. G. T., Leveque, C. M., Portier, B. P., Iyer, S. P., Bradner, J. E., & Bhalla, K. N. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-14-0258 · Cited by 140

Synthetic transcription elongation factors license transcription across repressive chromatin

Erwin, G. S., Grieshop, M. P., Ali, A., Qi, J., Lawlor, M. A., Kumar, D., Ahmad, I., McNally, A. G., Teider, N., Worringer, K. A., et al. (2017) · Science · doi:10.1126/science.aan6414 · Cited by 140

Transcriptional Burst Initiation and Polymerase Pause Release Are Key Control Points of Transcriptional Regulation

Bartman, C., Hamagami, N., Keller, C. A., Giardine, B. M., Hardison, R. C., Blobel, G. A., & Raj, A. (2018) · Molecular Cell · doi:10.1016/j.molcel.2018.11.004 · Cited by 140

Bromo- and Extraterminal Domain Chromatin Regulators Serve as Cofactors for Murine Leukemia Virus Integration

Gupta, S. S., Maetzig, T., Maertens, G. N., Sharif, A., Rothe, M., Weidner-Glunde, M., Galla, M., Schambach, A., Cherepanov, P., & Schulz, T. F. (2013) · Journal of Virology · doi:10.1128/jvi.01942-13 · Cited by 139

Epigenomics and Interindividual Differences in Drug Response

Ivanov, M., Kacevska, M., & Ingelman‐Sundberg, M. (2012) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.2012.152 · Cited by 139

Plane of Best Fit: A Novel Method to Characterize the Three-Dimensionality of Molecules

Firth, N. C., Brown, N., & Blagg, J. (2012) · Journal of Chemical Information and Modeling · doi:10.1021/ci300293f · Cited by 139

SS18 Together with Animal-Specific Factors Defines Human BAF-Type SWI/SNF Complexes

Middeljans, E., Wan, X., Jansen, P. W., Sharma, V., Stunnenberg, H. G., & Logie, C. (2012) · PLoS ONE · doi:10.1371/journal.pone.0033834 · Cited by 139

Epigenetic treatment of pancreatic cancer: is there a therapeutic perspective on the horizon?

Heßmann, E., Johnsen, S. A., Siveke, J. T., & Ellenrieder, V. (2016) · Gut · doi:10.1136/gutjnl-2016-312539 · Cited by 139

The Short Isoform of BRD4 Promotes HIV-1 Latency by Engaging Repressive SWI/SNF Chromatin-Remodeling Complexes

Conrad, R. J., Fozouni, P., Thomas, S., Sy, H., Zhang, Q., Zhou, M., & Ott, M. (2017) · Molecular Cell · doi:10.1016/j.molcel.2017.07.025 · Cited by 139

Abstract 2318: BET bromodomain inhibitors for cancer therapy

Qi, J., Filippakopoulos, P., McKeown, M. R., Shaw, K. L., Smith, W. B., French, C. A., Kung, A. L., Knapp, S., & Bradner, J. E. (2011) · Cancer Research · doi:10.1158/1538-7445.am2011-2318

Abstract IA16: Chemical inhibition of bromodomains

Bradner, J. E. (2012) · Cancer Research · doi:10.1158/1538-7445.csb12-ia16

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

Chung, C., Coste, H., White, J. H. M., Mirguet, O., Wilde, J. I., Gosmini, R. L., Delves, C. J., Magny, S. D., Woodward, R., Hughes, S. A., et al. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm200108t · Cited by 338

Bromodomains: Structure, function and pharmacology of inhibition

Ferri, E., Petosa, C., & McKenna, C. E. (2015) · Biochemical Pharmacology · doi:10.1016/j.bcp.2015.12.005 · Cited by 249

Bromodomain Inhibition and Its Application to Human Disease

Dupper, N. J., Zhou, Y., Govin, J., & McKenna, C. E. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-813939-4.00011-5 · Cited by 2