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SMARCA4: Current status and future perspectives in non-small-cell lung cancer

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Epigenomic regulation of oncogenesis by chromatin remodeling

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CDK4/6 inhibitors target SMARCA4-determined cyclin D1 deficiency in hypercalcemic small cell carcinoma of the ovary

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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

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Discovery of Chemical Inhibitors of Human Bromodomains

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A comprehensive study of epigenetic alterations in hepatocellular carcinoma identifies potential therapeutic targets

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Mechanistic and Structural Features of PROTAC Ternary Complexes

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Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia

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Chromatin remodellers as therapeutic targets

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ARID1A mutant ovarian clear cell carcinoma: A clear target for synthetic lethal strategies

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PROTAC degraders as chemical probes for studying target biology and target validation

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Bromodomain Drug Discovery – the Past, the Present, and the Future

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Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action

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Epigenetic regulators in cancer therapy and progression

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BRM/SMARCA2 promotes the proliferation and chemoresistance of pancreatic cancer cells by targeting JAK2/STAT3 signaling

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Global identification of SWI/SNF targets reveals compensation by EP400

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Context-specific functions of chromatin remodellers in development and disease

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BRCA1/FANCD2/BRG1-Driven DNA Repair Stabilizes the Differentiation State of Human Mammary Epithelial Cells

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Chromatin dependencies in cancer and inflammation

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Synthetic lethal interaction between the tumour suppressor STAG2 and its paralog STAG1

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SMARCA4/2 loss inhibits chemotherapy-induced apoptosis by restricting IP3R3-mediated Ca2+ flux to mitochondria

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New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives

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Clinical progress and pharmacology of small molecule bromodomain inhibitors

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A Chemical Probe for the ATAD2 Bromodomain

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Brahma-related gene-1 promotes tubular senescence and renal fibrosis through Wnt/β-catenin/autophagy axis

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An Update of Epigenetic Drugs for the Treatment of Cancers and Brain Diseases: A Comprehensive Review

Sahafnejad, Z., Ramazi, S., & Allahverdi, A. (2023) · Genes · doi:10.3390/genes14040873 · Cited by 71 · see citing works

Ponatinib Shows Potent Antitumor Activity in Small Cell Carcinoma of the Ovary Hypercalcemic Type (SCCOHT) through Multikinase Inhibition

Lang, J. D., Hendricks, W. P. D., Yin, H., Kiefer, J. M., Ramos, P. M., Sharma, R., Pirrotte, P., Raupach, E. A., Sereduk, C., Tang, N., et al. (2018) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-17-1928 · Cited by 72 · see citing works

Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong in vivo Antitumor Activity

Yang, L., Tu, W., Huang, L., Miao, B., Kaneshige, A., Jiang, W., Leng, L., Wang, M., Wen, B., Sun, D., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00953 · Cited by 69 · see citing works

Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

Farnaby, W., Koegl, M., McConnell, D. B., & Ciulli, A. (2021) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2021.02.009 · Cited by 65 · see citing works

BAF Complex Maintains Glioma Stem Cells in Pediatric H3K27M Glioma

Panditharatna, E., Marques, J. G., Wang, T., Trissal, M. C., Liu, I., Jiang, L., Beck, A., Groves, A. P., Dharia, N. V., Li, D., et al. (2022) · Cancer Discovery · doi:10.1158/2159-8290.cd-21-1491 · Cited by 63 · see citing works

Targeting the chromatin remodeling enzyme BRG1 increases the efficacy of chemotherapy drugs in breast cancer cells

Wu, Q., Sharma, S., Cui, H., LeBlanc, S. E., Zhang, H., Muthuswami, R., Nickerson, J. A., & Imbalzano, A. N. (2016) · Oncotarget · doi:10.18632/oncotarget.8384 · Cited by 62 · see citing works

Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development

Jeffers, V., Yang, C., Huang, S., & Sullivan, W. J. (2017) · Microbiology and Molecular Biology Reviews · doi:10.1128/mmbr.00047-16 · Cited by 62 · see citing works

CRISPR/Cas9 knockouts reveal genetic interaction between strain-transcendent erythrocyte determinants of Plasmodium falciparum invasion

Kanjee, U., Grüring, C., Chaand, M., Lin, K., Egan, E. S., Manzo, J., Jones, P. L., Yu, T. M., Barker, R. H., Weekes, M. P., et al. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1711310114 · Cited by 62 · see citing works

Targeting Chromatin-Remodeling Factors in Cancer Cells: Promising Molecules in Cancer Therapy

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BRD9 binds cell type-specific chromatin regions regulating leukemic cell survival via STAT5 inhibition

Gaudio, N. D., Costanzo, A. D., Liu, N. Q., Conte, L., Migliaccio, A., Vermeulen, M., Martens, J. H. A., Stunnenberg, H. G., Nebbioso, A., & Altucci, L. (2019) · Cell Death and Disease · doi:10.1038/s41419-019-1570-9 · Cited by 61 · see citing works

Fast-acting chemical tools to delineate causality in transcriptional control

Jaeger, M. G., & Winter, G. E. (2021) · Molecular Cell · doi:10.1016/j.molcel.2021.02.015 · Cited by 60 · see citing works

Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective

Webb, T., Craigon, C., & Ciulli, A. (2022) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2022.128653 · Cited by 58 · see citing works

Targeting synthetic lethal paralogs in cancer

Ryan, C. J., Mehta, I., Kebabci, N., & Adams, D. J. (2023) · Trends in cancer · doi:10.1016/j.trecan.2023.02.002 · Cited by 58 · see citing works

Selectivity On-Target of Bromodomain Chemical Probes by Structure-Guided Medicinal Chemistry and Chemical Biology

Galdeano, C., & Ciulli, A. (2016) · Future Medicinal Chemistry · doi:10.4155/fmc-2016-0059 · Cited by 59 · see citing works

Chromatin Remodeling Factor BRG1 Regulates Stemness and Chemosensitivity of Glioma Initiating Cells

Ganguly, D., Sims, M. M., Cai, C., Fan, M., & Pfeffer, L. M. (2018) · Stem Cells · doi:10.1002/stem.2909 · Cited by 59 · see citing works

Using Chemical Epigenetics to Target Cancer

Wimalasena, V. K., Wang, T., Sigua, L. H., Durbin, A. D., & Qi, J. (2020) · Molecular Cell · doi:10.1016/j.molcel.2020.04.023 · Cited by 55 · see citing works

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

Myrianthopoulos, V., Gaboriaud‐Kolar, N., Tallant, C., Hall, M. L., Grigoriou, S., Brownlee, P. M., Fedorov, O., Rogers, C. M., Heidenreich, D. J., Wanior, M., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00355 · Cited by 54 · see citing works

BAF complexes drive proliferation and block myogenic differentiation in fusion-positive rhabdomyosarcoma

Laubscher, D., Gryder, B. E., Sunkel, B. D., Andrésson, Þ., Wachtel, M., Das, S., Roschitzki, B., Wolski, W., Wu, X., Chou, H.-C., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-27176-w · Cited by 54 · see citing works

Targeting epigenetic regulators for cancer therapy: modulation of bromodomain proteins, methyltransferases, demethylases, and microRNAs

Gelato, K. A., Adler, D., Ocker, M., & Haendler, B. (2015) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728222.2016.1134490 · Cited by 52 · see citing works

SMARCA4 deficiency-associated heterochromatin induces intrinsic DNA replication stress and susceptibility to ATR inhibition in lung adenocarcinoma

Kurashima, K., Kashiwagi, H., Shimomura, I., Suzuki, A., Takeshita, F., Mazevet, M., Harata, M., Yamashita, T., Yamamoto, Y., Kohno, T., et al. (2020) · NAR Cancer · doi:10.1093/narcan/zcaa005 · Cited by 52 · see citing works

Development of PROTAC Degrader Drugs for Cancer

Vetma, V., O’Connor, S., & Ciulli, A. (2024) · Annual Review of Cancer Biology · doi:10.1146/annurev-cancerbio-061824-105806 · Cited by 53 · see citing works

BRG1 is a prognostic indicator and a potential therapeutic target for prostate cancer

Muthuswami, R., Bailey, L. O., Radhakrishnan, R., Imbalzano, A. N., Nickerson, J. A., & Hockensmith, J. W. (2019) · Journal of Cellular Physiology · doi:10.1002/jcp.28161 · Cited by 51 · see citing works

SMARCA2-deficiency confers sensitivity to targeted inhibition of SMARCA4 in esophageal squamous cell carcinoma cell lines

Ehrenhöfer-Wölfer, K., Puchner, T., Schwarz, C., Rippka, J., Blaha-Ostermann, S., Strobl, U., Hörmann, A., Bader, G., Kornigg, S., Zahn, S. K., et al. (2019) · Scientific Reports · doi:10.1038/s41598-019-48152-x · Cited by 51 · see citing works

Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence

Duran-Frigola, M., Cigler, M., & Winter, G. E. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c11098 · Cited by 50 · see citing works

Drug Discovery and Chemical Biology of Cancer Epigenetics

Ribich, S. A., Harvey, D. M., & Copeland, R. A. (2017) · Cell chemical biology · doi:10.1016/j.chembiol.2017.08.020 · Cited by 49 · see citing works

The mechanisms of action of chromatin remodelers and implications in development and disease

Sahu, R. K., Singh, S., & Tomar, R. S. (2020) · Biochemical Pharmacology · doi:10.1016/j.bcp.2020.114200 · Cited by 50 · see citing works

Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation

Čermáková, K., & Hodges, H. C. (2018) · Molecules · doi:10.3390/molecules23081958 · Cited by 49 · see citing works

Sophisticated Conversations between Chromatin and Chromatin Remodelers, and Dissonances in Cancer

Clapier, C. R. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22115578 · Cited by 46 · see citing works

The role of chromatin remodeler SMARCA4/BRG1 in brain cancers: a potential therapeutic target

Navickas, S. M., Giles, K. A., Brettingham‐Moore, K. H., & Taberlay, P. C. (2023) · Oncogene · doi:10.1038/s41388-023-02773-9 · Cited by 45 · see citing works

Progress in the Development of non‐BET Bromodomain Chemical Probes

Theodoulou, N. H., Tomkinson, N. C. O., Prinjha, R. K., & Humphreys, P. G. (2016) · ChemMedChem · doi:10.1002/cmdc.201500540 · Cited by 45 · see citing works

Control of Stimulus-Dependent Responses in Macrophages by SWI/SNF Chromatin Remodeling Complexes

Gatchalian, J., Liao, J., Maxwell, M. B., & Hargreaves, D. C. (2020) · Trends in Immunology · doi:10.1016/j.it.2019.12.002 · Cited by 45 · see citing works

PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

Berlin, M. Y., Cantley, J. L., Bookbinder, M., Bortolon, E., Broccatelli, F., Cadelina, G. W., Chan, E. W., Chen, H., Chen, X., Cheng, Y., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01781 · Cited by 44 · see citing works

The Emerging Roles of ATP-Dependent Chromatin Remodeling Complexes in Pancreatic Cancer

Hasan, N. M., & Ahuja, N. (2019) · Cancers · doi:10.3390/cancers11121859 · Cited by 46 · see citing works

Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis

Wanior, M., Preuß, F., Ni, X., Krämer, A., Mathea, S., Göbel, T., Heidenreich, D. J., Simonyi, S., Kahnt, A. S., Joerger, A. C., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01242 · Cited by 43 · see citing works

Dysregulation of chromatin remodelling complexes in amyotrophic lateral sclerosis

Tibshirani, M., Zhao, B., Gentil, B. J., Minotti, S., Marques, C., Keith, J., Rogaeva, E., Zinman, L., Rouaux, C., Robertson, J., et al. (2017) · Human Molecular Genetics · doi:10.1093/hmg/ddx301 · Cited by 42 · see citing works

Degraders in epigenetic therapy: PROTACs and beyond

Dai, X., Ji, S., Fu, M., Liu, G.-Z., Liu, H., Wang, S., Shen, L., Wang, N., Herdewijn, P. A., Zheng, Y., et al. (2024) · Theranostics · doi:10.7150/thno.92526 · Cited by 44 · see citing works

Multidimensional pooled shRNA screens in human THP-1 cells identify candidate modulators of macrophage polarization

Surdziel, E., Clay, I., Nigsch, F., Thiemeyer, A., Allard, C., Hoffman, G. R., Reece-Hoyes, J. S., Phadke, T., Gambert, R., Keller, C. G., et al. (2017) · PLoS ONE · doi:10.1371/journal.pone.0183679 · Cited by 42 · see citing works

BRG1 in the Nucleus Accumbens Regulates Cocaine-Seeking Behavior

Wang, Z.-J., Martin, J. A., Mueller, L. E., Caccamise, A. J., Werner, C. T., Neve, R. L., Gancarz, A. M., Li, J., & Dietz, D. (2016) · Biological Psychiatry · doi:10.1016/j.biopsych.2016.04.020 · Cited by 41 · see citing works

Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery

Zhan, Y., Kost‐Alimova, M., Shi, X., Leo, E., Bardenhagen, J., Shepard, H. E., Appikonda, S., Vangamudi, B., Zhao, S., Tieu, T. N., et al. (2015) · Epigenetics & Chromatin · doi:10.1186/s13072-015-0026-4 · Cited by 41 · see citing works

The SMARCA4R1157W mutation facilitates chromatin remodeling and confers PRMT1/SMARCA4 inhibitors sensitivity in colorectal cancer

Zeng, X., Yao, B., Liu, J., Gong, G., Liu, M., Li, J., Pan, H., Li, Q., Yang, D., Lu, P., et al. (2023) · npj Precision Oncology · doi:10.1038/s41698-023-00367-y · Cited by 41 · see citing works

The Discovery of SWI/SNF Chromatin Remodeling Activity as a Novel and Targetable Dependency in Uveal Melanoma

Rago, F., Elliott, G., Li, A., Sprouffske, K., Kerr, G., Desplat, A., Abramowski, D., Chen, J. T., Farsidjani, A., Xiang, K. X., et al. (2020) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-19-1013 · Cited by 40 · see citing works

Polycomb and trithorax opposition in development and disease

Poynter, S. T., & Kadoch, C. (2016) · Wiley Interdisciplinary Reviews Developmental Biology · doi:10.1002/wdev.244 · Cited by 38 · see citing works

Abstract 3528: The SMARCA2/4 catalytic activity, but not the bromodomain, is a drug target in SWI/SNF mutant cancers

Vangamudi, B., Paul, T. A., Shah, P. K., Alimova, M., Nottebaum, L. M., Shi, X., Zhan, Y., Leo, E., Mahadeshwar, H. S., Protopopov, A. I., et al. (2015) · Cancer Research · doi:10.1158/1538-7445.am2015-3528

Abstract LB-258: Identification of SMARCA2/4 degraders for the treatment of SMARCA4-mutant and other cancers

Sasmal, S., Satyam, L. K., Pothuganti, M. K., Ettam, A., Nunna, S., Shareef, M. A., Gopinath, S., Mukherjee, S., Ramachandra, M., & Samajdar, S. (2018) · Cancer Research · doi:10.1158/1538-7445.am2018-lb-258

Abstract 5063: Epigenetic modulators show differential activity on lung adenocarcinoma cells with loss-of-function mutations of SWI/SNF protein SMARCA4

Rzymski, T., Wróbel, A., Mikuła, M., Pyziak, K., Bartosik, A. R., Sroka-Oleksiak, A., Paziewska, A., Grochowska, A., Statkiewicz, M., Paczkowska, K., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-5063

The ATPase module of mammalian SWI/SNF family complexes mediates subcomplex identity and catalytic activity–independent genomic targeting

Pan, J., McKenzie, Z. M., D’Avino, A. R., Mashtalir, N., Lareau, C. A., Pierre, R. S., Wang, L., Shilatifard, A., & Kadoch, C. (2019) · Nature Genetics · doi:10.1038/s41588-019-0363-5 · Cited by 121 · see citing works

Abstract 3592: Targeting SWI/SNF ATPases in enhancer-addicted human cancers

Parolia, A., Xiao, L., Qiao, Y., Bawa, P., Eyunni, S., Young, E., Mannan, R., Carson, S. E., Chang, Y., Zhang, Y., et al. (2022) · Cancer Research · doi:10.1158/1538-7445.am2022-3592