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

Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms

Kleppe, M., Koche, R., Zou, L., van Galen, P., Hill, C. E., Dong, L., De Groote, S., Papalexi, E., Hanasoge Somasundara, A. V., Cordner, K., et al. (2018) · Cancer Cell · doi:10.1016/j.ccell.2017.11.009 · Cited by 279

Targeting Transcription Factors in Cancer

Bhagwat, A. S., & Vakoc, C. R. (2015) · Trends in Cancer · doi:10.1016/j.trecan.2015.07.001 · Cited by 276

Pathogenesis of NUT Midline Carcinoma

French, C. A. (2011) · Annual Review of Pathology Mechanisms of Disease · doi:10.1146/annurev-pathol-011811-132438 · Cited by 273

Gene bookmarking accelerates the kinetics of post-mitotic transcriptional re-activation

Zhao, R., Nakamura, T., Fu, Y., Lazar, Z., & Spector, D. L. (2011) · Nature Cell Biology · doi:10.1038/ncb2341 · Cited by 269

Getting pharmaceutical R&D back on target

Bunnage, M. E. (2011) · Nature Chemical Biology · doi:10.1038/nchembio.581 · Cited by 269

Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA

Zou, Z., Huang, B., Wu, X., Zhang, H., Qi, J., Bradner, J. E., Nair, S. K., & Chen, L.-F. (2013) · Oncogene · doi:10.1038/onc.2013.179 · Cited by 269

Readers of poly(ADP-ribose): designed to be fit for purpose

Teloni, F., & Altmeyer, M. (2015) · Nucleic Acids Research · doi:10.1093/nar/gkv1383 · Cited by 269

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

Hammitzsch, A., Tallant, C., Fedorov, O., O’Mahony, A., Brennan, P. E., Hay, D. A., Martínez, F. O., Al‐Mossawi, H., de Wit, J., Vecellio, M. L., et al. (2015) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1501956112 · Cited by 265

Liquid–liquid phase separation in tumor biology

Tong, X., Tang, R., Xu, J., Wang, W., Zhao, Y., Yu, X., & Shi, S. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-01076-x · Cited by 265

Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure

Pagliarini, R. A., Shao, W., & Sellers, W. R. (2015) · EMBO Reports · doi:10.15252/embr.201439949 · Cited by 264

Quinazoline and quinazolinone as important medicinal scaffolds: a comparative patent review (2011–2016)

Hameed, A., al‐Rashida, M., Uroos, M., Ali, S. A., Arshia, A., Ishtiaq, M., & Khan, K. M. (2018) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2018.1432596 · Cited by 264

BET bromodomain inhibition as a novel strategy for reactivation of HIV-1

Banerjee, C., Archin, N. M., Michaels, D., Belkina, A. C., Denis, G. V., Bradner, J. E., Sebastiani, P., Margolis, D. M., & Montano, M. A. (2012) · Journal of Leukocyte Biology · doi:10.1189/jlb.0312165 · Cited by 263

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

Zeng, S., Huang, W., Zheng, X., Cheng, L., Zhang, Z., Wang, J., & Shen, Z. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112981 · Cited by 264

BET bromodomain inhibition suppresses innate inflammatory and profibrotic transcriptional networks in heart failure

Duan, Q., McMahon, S., Anand, P., Shah, H., Thomas, S., Salunga, H. T., Huang, Y., Zhang, R., Sahadevan, A., Lemieux, M. E., et al. (2017) · Science Translational Medicine · doi:10.1126/scitranslmed.aah5084 · Cited by 262

Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes

Lamonica, J. M., Deng, W., Kadauke, S., Campbell, A. E., Gamsjaeger, R., Wang, H., Cheng, Y., Billin, A. N., Hardison, R. C., Mackay, J. P., et al. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1102140108 · Cited by 262

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

Diehl, C. J., & Ciulli, A. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00387b · Cited by 269

Bromodomain biology and drug discovery

Zaware, N., & Zhou, M. (2019) · Nature Structural & Molecular Biology · doi:10.1038/s41594-019-0309-8 · Cited by 264

Bromodomain and Extra-Terminal Motif Inhibitors: a Review of Preclinical and Clinical Advances in Cancer Therapy

Alqahtani, A., Choucair, K., Ashraf, M., Hamouda, D., Alloghbi, A., Khan, T. A., Senzer, N. N., & Nemunaitis, J. J. (2019) · Future Science OA · doi:10.4155/fsoa-2018-0115 · Cited by 260

MYC promotes tryptophan uptake and metabolism by the kynurenine pathway in colon cancerPreprint

Venkateswaran, N., Lafita‐Navarro, M. C., Hao, Y.-H., Kilgore, J. A., Perez‐Castro, L., Braverman, J., Borenstein‐Auerbach, N., Kim, M. G., Lesner, N. P., Mishra, P., et al. (2019) · Genes & Development · doi:10.1101/gad.327056.119 · Cited by 260

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

Picaud, S., Costa, D. D., Thanasopoulou, A., Filippakopoulos, P., Fish, P. V., Philpott, M., Fedorov, O., Brennan, P. E., Bunnage, M. E., Owen, D. R., et al. (2013) · Cancer Research · doi:10.1158/0008-5472.can-12-3292 · Cited by 257

Cause and Consequence of Cancer/Testis Antigen Activation in Cancer

Whitehurst, A. W. (2013) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-011112-140326 · Cited by 255

Targeting Epigenetics in Cancer

Bennett, R. L., & Licht, J. D. (2017) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010716-105106 · Cited by 254

Protein acylation: mechanisms, biological functions and therapeutic targets

Shang, S., Liu, J., & Hua, F. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-01245-y · Cited by 261

Protein–protein interaction inhibitors get into the groove

Mullard, A. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3680 · Cited by 253

Oncogenic Mechanisms in Burkitt LymphomaPreprint

Schmitz, R., Ceribelli, M., Pittaluga, S., Wright, G. W., & Staudt, L. M. (2014) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a014282 · Cited by 252

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

Imaide, S., Riching, K. M., Makukhin, N., Vetma, V., Whitworth, C., Hughes, S. J., Trainor, N., Mahan, S. D., Murphy, N., Cowan, A. D., et al. (2021) · Nature Chemical Biology · doi:10.1038/s41589-021-00878-4 · Cited by 251

Inhibition of Brd4 alleviates renal ischemia/reperfusion injury-induced apoptosis and endoplasmic reticulum stress by blocking FoxO4-mediated oxidative stress

Liu, H., Wang, L., Weng, X., Chen, H., Du, Y., Diao, C., Chen, Z., & Liu, X. (2019) · Redox Biology · doi:10.1016/j.redox.2019.101195 · Cited by 251

Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function

Sakamaki, J.-I., Wilkinson, S., Hahn, M., Tasdemir, N., O’Prey, J., Clark, W., Hedley, A., Nixon, C., Long, J. S., New, M., et al. (2017) · Molecular Cell · doi:10.1016/j.molcel.2017.04.027 · Cited by 249

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

What makes a good drug target?

Gashaw, I., Ellinghaus, P., Sommer, A., & Asadullah, K. (2011) · Drug Discovery Today · doi:10.1016/j.drudis.2011.09.007 · Cited by 248

Modulation of Protein–Protein Interactions for the Development of Novel Therapeutics

Πέττα, Ι., Lievens, S., Libert, C., Tavernier, J. H., & Bosscher, K. D. (2015) · Molecular Therapy · doi:10.1038/mt.2015.214 · Cited by 248

Clinical trials for BET inhibitors run ahead of the science

Andrieu, G., Belkina, A. C., & Denis, G. V. (2016) · Drug Discovery Today: Technologies · doi:10.1016/j.ddtec.2016.06.004 · Cited by 247

NSD3–NUT Fusion Oncoprotein in NUT Midline Carcinoma: Implications for a Novel Oncogenic Mechanism

French, C. A., Rahman, S., Walsh, E. M., Kühnle, S., Grayson, A. R., Lemieux, M. E., Grunfeld, N., Rubin, B. P., Antonescu, C. R., Zhang, S., et al. (2014) · Cancer Discovery · doi:10.1158/2159-8290.cd-14-0014 · Cited by 247

BRD4 Sustains Melanoma Proliferation and Represents a New Target for Epigenetic Therapy

Segura, M. F., Fontanals-Cirera, B., Gaziel‐Sovran, A., Guijarro, M. V., Hanniford, D., Zhang, G., González‐Gómez, P., Morante, M., Jubierre, L., Zhang, W., et al. (2013) · Cancer Research · doi:10.1158/0008-5472.can-13-0122-t · Cited by 247

Reactivation of Latent HIV-1 by Inhibition of BRD4

Zhu, J. K., Gaiha, G. D., John, S. P., Pertel, T., Chin, C. R., Gao, G., Qu, H., Walker, B. D., Elledge, S. J., & Brass, A. L. (2012) · Cell Reports · doi:10.1016/j.celrep.2012.09.008 · Cited by 246

The Expanding World of N-MYC–Driven Tumors

Rickman, D. S., Schulte, J. H., & Eilers, M. (2018) · Cancer Discovery · doi:10.1158/2159-8290.cd-17-0273 · Cited by 246

Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation

Itzen, F., Greifenberg, A. K., Bösken, C. A., & Geyer, M. (2014) · Nucleic Acids Research · doi:10.1093/nar/gku449 · Cited by 245

Metabolic regulation of osteoclast differentiation and function

Indo, Y., Takeshita, S., Ishii, K., Hoshii, T., Aburatani, H., Hirao, A., & Ikeda, K. (2013) · Journal of Bone and Mineral Research · doi:10.1002/jbmr.1976 · Cited by 245

Targeted protein degradation for cancer therapy

Hinterndorfer, M., Spiteri, V. A., Ciulli, A., & Winter, G. E. (2025) · Nature reviews. Cancer · doi:10.1038/s41568-025-00817-8 · Cited by 263

BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice

Korb, E., Herre, M., Zucker-Scharff, I., Darnell, R. B., & Allis, C. D. (2015) · Nature Neuroscience · doi:10.1038/nn.4095 · Cited by 245

Residual Complexes Containing SMARCA2 (BRM) Underlie the Oncogenic Drive of SMARCA4 (BRG1) Mutation

Wilson, B. G., Helming, K., Wang, X., Kim, Y., Vázquez, F., Jagani, Z., Hahn, W. C., & Roberts, C. W. M. (2014) · Molecular and Cellular Biology · doi:10.1128/mcb.01372-13 · Cited by 243

Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy

Wang, Z., Zhang, Z.-C., Wu, Y., Pi, Y., Lou, S., Liu, T., Lou, G., & Yang, C. Q. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01647-6 · Cited by 251

BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism

Boehm, D., Calvanese, V., Dar, R. D., Xing, S., Schroeder, S., Martins, L. J., Aull, K. H., Li, P.-C., Planelles, V., Bradner, J. E., et al. (2013) · Cell Cycle · doi:10.4161/cc.23309 · Cited by 242

A CD47-associated super-enhancer links pro-inflammatory signalling to CD47 upregulation in breast cancer

Betancur, P. A., Abraham, B. J., Yiu, Y. Y., Willingham, S. B., Khameneh, F., Zarnegar, M. A., Kuo, A. H., McKenna, K. M., Kojima, Y., Leeper, N. J., et al. (2017) · Nature Communications · doi:10.1038/ncomms14802 · Cited by 243

Synthesis of Biologically Active Molecules through Multicomponent Reactions

Insuasty, D., Castillo, J., Becerra, D., Rojas, H. A., & Abonı́a, R. (2020) · Molecules · doi:10.3390/molecules25030505 · Cited by 242

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

Theodoulou, N. H., Bamborough, P., Bannister, A. J., Becher, I., Bit, R. A., Che, K. H., Chung, C., Dittmann, A., Drewes, G., Drewry, D. H., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00256 · Cited by 241

A transcriptional switch governs fibroblast activation in heart disease

Alexanian, M., Przytycki, P. F., Micheletti, R., Padmanabhan, A., Ye, L., Travers, J. G., Gonzalez-Teran, B., Silva, A. C., Duan, Q., Ranade, S. S., et al. (2021) · Nature · doi:10.1038/s41586-021-03674-1 · Cited by 238

Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy

Στρατικόπουλος, Η., Dendy, M., Szabolcs, M. J., Khaykin, A. J., Lefèbvre, C., Zhou, M., & Parsons, R. E. (2015) · Cancer Cell · doi:10.1016/j.ccell.2015.05.006 · Cited by 236

BET bromodomain inhibition suppresses TH17-mediated pathology

Mele, D. A., Salmerón, A., Ghosh, S., Huang, H.-R., Bryant, B. M., & Lora, J. M. (2013) · The Journal of Experimental Medicine · doi:10.1084/jem.20130376 · Cited by 234

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy

Picaud, S., Fedorov, O., Thanasopoulou, A., Leonards, K., Jones, K. L., Meier, J. C., Olzscha, H., Monteiro, O., Martin, S., Philpott, M., et al. (2015) · Cancer Research · doi:10.1158/0008-5472.can-15-0236 · Cited by 234

CURATE.AI: Optimizing Personalized Medicine with Artificial Intelligence

Blasiak, A., Khong, J., & Kee, T. W. (2019) · SLAS TECHNOLOGY · doi:10.1177/2472630319890316 · Cited by 234

Metabolic regulation of chromatin modifications and gene expression

Schvartzman, J. M., Thompson, C. B., & Finley, L. W. S. (2018) · Journal of Cell Biology · doi:10.1083/jcb.201803061 · Cited by 233

Targeting tumour-supportive cellular machineries in anticancer drug development

Dobbelstein, M., & Moll, U. M. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4201 · Cited by 233

Biochemical Aspects of PD-L1 Regulation in Cancer Immunotherapy

Zhang, J., Dang, F., Ren, J., & Wei, W. (2018) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2018.09.004 · Cited by 233

Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic

Hu, Z., & Crews, C. M. (2022) · ChemBioChem · doi:10.1002/cbic.202100270 · Cited by 231

Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery

Fu, L., Tian, M., Li, X., Li, J., Huang, J. M., Ouyang, L., Zhang, Y., & Liu, B. (2015) · Oncotarget · doi:10.18632/oncotarget.3551 · Cited by 231

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia

Xu, B., On, D. M., Ma, A., Parton, T., Konze, K. D., Pattenden, S. G., Allison, D. F., Cai, L., Rockowitz, S., Liu, S., et al. (2014) · Blood · doi:10.1182/blood-2014-06-581082 · Cited by 231

Therapeutic Strategies to Inhibit MYCPreprint

McKeown, M. R., & Bradner, J. E. (2014) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a014266 · Cited by 231

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

Ember, S. W., Zhu, J.-Y., Olesen, S. H., Martin, M. P., Becker, A., Berndt, N., Georg, G. I., & Schönbrunn, E. (2014) · ACS Chemical Biology · doi:10.1021/cb500072z · Cited by 229

Enhancers are activated by p300/CBP activity-dependent PIC assembly, RNAPII recruitment, and pause release

Narita, T., Ito, S., Higashijima, Y., Chu, W. K., Neumann, K., Walter, J., Satpathy, S., Liebner, T., Hamilton, W. B., Maskey, E., et al. (2021) · Molecular Cell · doi:10.1016/j.molcel.2021.03.008 · Cited by 228

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

Martin, L. J., Koegl, M., Bader, G., Cockcroft, X. F., Fedorov, O., Fiegen, D., Gerstberger, T., Hofmann, M. H., Hohmann, A. F., Kessler, D., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01865 · Cited by 228

Differentiation of NUT Midline Carcinoma by Epigenomic Reprogramming

Schwartz, B. E., Hofer, M. D., Lemieux, M. E., Bauer, D. E., Cameron, M. J., West, N. H., Agoston, E. S., Reynoird, N., Khochbin, S., Ince, T. A., et al. (2011) · Cancer Research · doi:10.1158/0008-5472.can-10-3513 · Cited by 227

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection

Mills, R. J., Humphrey, S. J., Fortuna, P. R. J., Lor, M., Foster, S. R., Quaife-Ryan, G. A., Johnston, R. L., Dumenil, T. D., Bishop, C., Rudraraju, R., et al. (2021) · Cell · doi:10.1016/j.cell.2021.03.026 · Cited by 229

Evaluating Enhancer Function and Transcription

Field, A. R., & Adelman, K. (2020) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-011420-095916 · Cited by 227

The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

He, Y., Selvaraju, S., Curtin, M. L., Jakob, C. G., Zhu, H., Comess, K. M., Shaw, B., The, J., Lima-Fernandes, E., Szewczyk, M. M., et al. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2306 · Cited by 224

Quantitative Imaging with Fluorescent Biosensors

Okumoto, S., Jones, A. M., & Frommer, W. B. (2012) · Annual Review of Plant Biology · doi:10.1146/annurev-arplant-042110-103745 · Cited by 224

CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer

McCleland, M. L., Mesh, K., Lorenzana, E. G., Chopra, V. S., Segal, E., Watanabe, C. K., Haley, B., Mayba, O., Yaylaoglu, M., Gnad, F., et al. (2016) · Journal of Clinical Investigation · doi:10.1172/jci83265 · Cited by 224

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Chan, K.-H., Zengerle, M., Testa, A., & Ciulli, A. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01912 · Cited by 223

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Gechijian, L. N., Buckley, D. L., Lawlor, M. A., Reyes, J. M., Paulk, J., Ott, C. J., Winter, G. E., Erb, M. A., Scott, T. G., Xu, M., et al. (2018) · Nature Chemical Biology · doi:10.1038/s41589-018-0010-y · Cited by 222

Targeted protein degradation via intramolecular bivalent glues

Hsia, O., Hinterndorfer, M., Cowan, A. D., Iso, K., Ishida, T., Sundaramoorthy, R., Nakasone, M. A., Imrichova, H., Schätz, C., Rukavina, A., et al. (2024) · Nature · doi:10.1038/s41586-024-07089-6 · Cited by 222

Advances in the translational genomics of neuroblastoma: From improving risk stratification and revealing novel biology to identifying actionable genomic alterations

Bosse, K. R., & Maris, J. M. (2015) · Cancer · doi:10.1002/cncr.29706 · Cited by 222

BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

Bhadury, J., Nilsson, L. M., Muralidharan, S. V., Green, L. C., Li, Z., Gesner, E. M., Hansen, H. C., Keller, U. B., McLure, K. G., & Nilsson, J. A. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1406722111 · Cited by 221

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

Hewings, D. S., Wang, M., Philpott, M., Fedorov, O., Uttarkar, S., Filippakopoulos, P., Picaud, S., Vuppusetty, C., Marsden, B. D., Knapp, S., et al. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm200640v · Cited by 220

Biological plasticity rescues target activity in CRISPR knock outs

Smits, A. H., Ziebell, F., Joberty, G., Zinn, N., Mueller, W. F., Clauder-Münster, S., Eberhard, D., Fälth Savitski, M., Grandi, P., Jakob, P., et al. (2019) · Nature Methods · doi:10.1038/s41592-019-0614-5 · Cited by 219

A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation

Wurz, R. P., Dellamaggiore, K., Dou, H., Javier, N., LO, M. M. ‐., McCarter, J. D., Mohl, D. A., Sastri, C. E., Lipford, J. R., & Cee, V. J. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01781 · Cited by 218

MYC: a multipurpose oncogene with prognostic and therapeutic implications in blood malignancies

Ahmadi, S. E., Rahimi, S., Zarandi, B., Chegeni, R., & Safa, M. (2021) · Journal of Hematology & Oncology · doi:10.1186/s13045-021-01111-4 · Cited by 223

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

Albrecht, B. K., Gehling, V. S., Hewitt, M. C., Vaswani, R. G., Côté, A., Leblanc, Y., Nasveschuk, C. G., Bellon, S. F., Bergeron, L., Campbell, R., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01882 · Cited by 219

Chromatin signatures of cancerPreprint

Morgan, M. A., & Shilatifard, A. (2015) · Genes & Development · doi:10.1101/gad.255182.114 · Cited by 218

Control of Embryonic Stem Cell Identity by BRD4-Dependent Transcriptional Elongation of Super-Enhancer-Associated Pluripotency Genes

Di Micco, R., Fontanals-Cirera, B., Low, V., Ntziachristos, P., Yuen, S. K., Lovell, C. D., Dolgalev, I., Yonekubo, Y., Zhang, G., Rusinova, E., et al. (2014) · Cell Reports · doi:10.1016/j.celrep.2014.08.055 · Cited by 217

Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis

Savitski, M. M., Zinn, N., Faelth-Savitski, M., Poeckel, D., Gade, S., Becher, I., Muelbaier, M., Wagner, A. J., Strohmer, K., Werner, T., et al. (2018) · Cell · doi:10.1016/j.cell.2018.02.030 · Cited by 217

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

Pillow, T. H., Adhikari, P., Blake, R. A., Chen, J., Del Rosario, G., Deshmukh, G., Figueroa, I., Gascoigne, K. E., Kamath, A. V., Kaufman, S., et al. (2020) · ChemMedChem · doi:10.1002/cmdc.201900497 · Cited by 216

Role of Transcription Factor Acetylation in Diabetic Kidney Disease

Liu, R., Zhong, Y., Li, X., Chen, H., Jim, B., Zhou, M., Chuang, P. Y., & He, C. (2014) · Diabetes · doi:10.2337/db13-1810 · Cited by 216

A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells

Gatchalian, J., Malik, S., Ho, J., Lee, D.-S., Kelso, T. W. R., Shokhirev, M. N., Dixon, J. R., & Hargreaves, D. C. (2018) · Nature Communications · doi:10.1038/s41467-018-07528-9 · Cited by 216

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

Chaidos, A., Caputo, V. S., Gouvedenou, K., Liu, B., Marigo, I., Chaudhry, M. S., Rotolo, A., Tough, D. F., Smithers, N. N., Bassil, A. K., et al. (2013) · Blood · doi:10.1182/blood-2013-01-478420 · Cited by 215

NUT Carcinoma: Clinicopathologic features, pathogenesis, and treatment

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Histone Variant H2A.Z.2 Mediates Proliferation and Drug Sensitivity of Malignant Melanoma

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Chromatin Contributions to the Regulation of Innate Immunity

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Bromodomain and Extra-terminal (BET) Bromodomain Inhibition Activate Transcription via Transient Release of Positive Transcription Elongation Factor b (P-TEFb) from 7SK Small Nuclear Ribonucleoprotein

Bartholomeeusen, K., Xiang, Y., Fujinaga, K., & Peterlin, B. M. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.410746 · Cited by 212

Intensive treatment and survival outcomes in NUT midline carcinoma of the head and neck

Chau, N. G., Hurwitz, S., Mitchell, C. M., Aserlind, A. B., Grunfeld, N., Kaplan, L., Hsi, P. T., Bauer, D. E., Lathan, C. S., Galindo, C. R., et al. (2016) · Cancer · doi:10.1002/cncr.30242 · Cited by 212

The Chemical Biology of Reversible Lysine Post-translational Modifications

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BRD4 is a novel therapeutic target for liver fibrosis

Ding, N., Hah, N., Yu, R. T., Sherman, M. H., Benner, C., Leblanc, M., He, M., Liddle, C., Downes, M., & Evans, R. M. (2015) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1522163112 · Cited by 211

Dissecting fibrosis: therapeutic insights from the small-molecule toolbox

Nanthakumar, C. B., Hatley, R. J. D., Lemma, S., Gauldie, J., Marshall, R. P., & Macdonald, S. J. F. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4592 · Cited by 213

Efficacy of BET Bromodomain Inhibition in Kras-Mutant Non–Small Cell Lung Cancer

Shimamura, T., Chen, Z., Soucheray, M., Carretero, J., Kikuchi, E., Tchaicha, J. H., Gao, Y., Cheng, K. A., Cohoon, T. J., Qi, J., et al. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-3904 · Cited by 210

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

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JARID1B Is a Luminal Lineage-Driving Oncogene in Breast Cancer

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Brd4 binds to active enhancers to control cell identity gene induction in adipogenesis and myogenesis

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Histone modifications in epigenetic regulation of cancer: Perspectives and achieved progress

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Targeted Protein Degradation by Small Molecules

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Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition

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Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology

Blagg, J., & Workman, P. (2017) · Cancer Cell · doi:10.1016/j.ccell.2017.06.005 · Cited by 207

Abstract 2318: BET bromodomain inhibitors for cancer therapy

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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

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Bromodomain Inhibition and Its Application to Human Disease

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