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Chemical Inhibitors of a Selective SWI/SNF Function Synergize with ATR Inhibition in Cancer Cell Killing

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The Bromodomain Inhibitor PFI-3 Sensitizes Cancer Cells to DNA Damage by Targeting SWI/SNF

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Discovery of SMD-3236: A Potent, Highly Selective and Efficacious SMARCA2 Degrader for the Treatment of SMARC4-Deficient Human Cancers

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Introducing structure-based three-dimensional pharmacophore models for accelerating the discovery of selective BRD9 binders

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Mammalian SWI/SNF Enzymes and the Epigenetics of Tumor Cell Metabolic Reprogramming

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SWI/SNF Chromatin Remodeling Enzymes in Melanoma

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Enhancer reprogramming underlies therapeutic utility of a SMARCA2 degrader in SMARCA4 mutant cancer

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Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold

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Discovery of High-Affinity SMARCA2/4 Bromodomain Ligands and Development of Potent and Exceptionally Selective SMARCA2 PROTAC Degraders

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Thyroid Hormone Receptor β Suppression of RUNX2 Is Mediated by Brahma-Related Gene 1–Dependent Chromatin Remodeling

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Histone Modifying Enzymes and Chromatin Modifiers in Glioma Pathobiology and Therapy Responses

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Partial Inactivation of the Chromatin Remodelers SMARCA2 and SMARCA4 in Virus-Infected Cells by Caspase-Mediated Cleavage

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SMARCA4 biology in alveolar rhabdomyosarcoma

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Therapeutic targeting of chromatin alterations in leukemia and solid tumors

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The role of SWI/SNF chromatin remodelers in the repair of DNA double strand breaks and cancer therapy

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SMARCA2 deficiency in NSCLC: a clinicopathologic and immunohistochemical analysis of a large series from a single institution

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BRG1 regulation by miR-155 in human leukemia and lymphoma cell lines

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PROTACs: Promising Approaches for Epigenetic Strategies to Overcome Drug Resistance

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Comparative RNAi Screens in Isogenic Human Stem Cells Reveal SMARCA4 as a Differential Regulator

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Hartley, A., Leung, H. Y., & Ahmad, I. (2020) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2020.1821644 · Cited by 12

Altering mammalian transcription networking with ADAADi: An inhibitor of ATP-dependent chromatin remodeling

Radhakrishnan, R., Chanana, U. B., Hussain, S., Sharma, S., Goel, K., Bisht, D., Patne, K., Swer, P. B., Hockensmith, J. W., & Muthuswami, R. (2021) · PLoS ONE · doi:10.1371/journal.pone.0251354 · Cited by 12

Tumor suppression via inhibition of SWI/SNF complex-dependent NF-κB activation

Kobayashi, K., Hiramatsu, H., Nakamura, S., Kobayashi, K., Haraguchi, T., & Iba, H. (2017) · Scientific Reports · doi:10.1038/s41598-017-11806-9 · Cited by 12

Pharmacological Modulation of Transcriptional Coregulators in Cancer

Bishop, T. R., Zhang, Y., & Erb, M. A. (2019) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2019.04.004 · Cited by 11

HELLS serves as a poor prognostic biomarker and its downregulation reserves the malignant phenotype in pancreatic cancer

Wang, F., Jing, Y., Cheng, C., Cao, Z., Jiao, J., & Chen, Z. (2021) · BMC Medical Genomics · doi:10.1186/s12920-021-01043-5 · Cited by 12

SMARCA2 and SMARCA4 Participate in DNA Damage Repair

Yu, L. L., & Wu, D. (2024) · Frontiers in Bioscience-Landmark · doi:10.31083/j.fbl2907262 · Cited by 11

Glutathione-dependent degradation of SMARCA2/4 for targeted lung cancer therapy with improved selectivity

Ji, M. H., Yu, D., Liu, X., Wang, L., Zhang, D., Yang, Z., Huang, W., Fan, H., Wang, L., & Sun, H. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116751 · Cited by 11

SMARCA4/BRG1 deficiency induces a targetable dependence on oxidative phosphorylation in clear cell renal cell carcinoma

Fang, R., Wang, X., Wu, R., Pan, R., Tian, M., Zhang, R., Wei, X., Wang, X., Ye, S., Li, F., et al. (2025) · Carcinogenesis · doi:10.1093/carcin/bgaf002 · Cited by 11

SMARCA2 protein: Structure, function and perspectives of drug design

Guo, Z., Wang, P., Han, Y., Jiang, S., Yang, X., & Cao, S. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117319 · Cited by 12

Comprehensive Analysis of SWI/SNF Inactivation in Lung Adenocarcinoma Cell Models

Peinado, P., Andrades, Á., Cuadros, M., Rodríguez, M. I., Coira, I. F., García, D. J., Álvarez-Pérez, J. C., Baliñas-Gavira, C., Arenas, A. M., Patiño-Mercau, J. R., et al. (2020) · Cancers · doi:10.3390/cancers12123712 · Cited by 11

B Lymphocyte Specification Is Preceded by Extensive Epigenetic Priming in Multipotent Progenitors

Strid, T., Okuyama, K., Tingvall-Gustafsson, J., Kuruvilla, J., Jensen, C. T., Lang, S., Javarappa, M. P. A., Somasundaram, R., Åhsberg, J., Cristóbal, S., et al. (2021) · The Journal of Immunology · doi:10.4049/jimmunol.2100048 · Cited by 11

The SWI/SNF Complex: A Frequently Mutated Chromatin Remodeling Complex in Cancer

Nguyen, V. T., Tessema, M., & Weissman, B. E. (2023) · Cancer treatment and research · doi:10.1007/978-3-031-45654-1_7 · Cited by 11

Targeting epigenetics using synthetic lethality in precision medicine

Chen, E. S. (2018) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-018-2866-0 · Cited by 11

In-Depth Characterization and Validation in BRG1 -Mutant Lung Cancers Define Novel Catalytic Inhibitors of SWI/SNF Chromatin RemodelingPreprint

Jagani, Z., Chenail, G., Xiang, K. X., Bushold, G., Bhang, H. C., Li, A., Elliott, G., Zhu, J., Vattay, A., Gilbert, T. J., et al. (2019) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/812628 · Cited by 11

Regulation of the Wnt signaling pathway during myogenesis by the mammalian SWI/SNF ATPase BRG1

Sharma, T., Olea‐Flores, M., & Imbalzano, A. N. (2023) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2023.1160227 · Cited by 10

BRM / SMARCA 2‐negative clear cell renal cell carcinoma is associated with a high percentage of BRM somatic mutations, deletions and promoter methylation

Xia, Q., Zhan, X., Fan, X., Ye, S., Shi, S., Li, R., Xue, W., Wang, X., Ma, H., Zhen-feng, L., et al. (2016) · Histopathology · doi:10.1111/his.13120 · Cited by 10

Discovery of Novel, Potent, and Orally Bioavailable SMARCA2 Proteolysis-Targeting Chimeras with Synergistic Antitumor Activity in Combination with Kirsten Rat Sarcoma Viral Oncogene Homologue G12C Inhibitors

Kotagiri, S., Wang, Y., Han, Y., Liang, X., Blazanin, N., Mazhar, H., Sebastian, M. M., Nguyen, P. K., Jiang, Y., & Lissanu, Y. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c02577 · Cited by 9

Preclinical and Clinical Advances of Targeted Protein Degradation as a Novel Cancer Therapeutic Strategy: An Oncologist Perspective

Yang, X., He, Y., Kim, R. D., Fleming, J. B., & Xie, H. (2020) · Targeted Oncology · doi:10.1007/s11523-020-00782-2 · Cited by 10

SWI/SNF complex, promising target in melanoma therapy: Snapshot view

Sisakht, M. M., Amirkhani, M. A., & Nilforoushzadeh, M. A. (2023) · Frontiers in Medicine · doi:10.3389/fmed.2023.1096615 · Cited by 8

The chromatin remodeling protein BRG1 mediates Ang II induced pro-fibrogenic response in renal fibroblasts

Hong, W., Zhu, Y., Lin, Y., Tang, S., Chen, J., Xu, L., Jiang, J., Zong, Y., Zhang, Y., Sun, A., et al. (2024) · Life Sciences · doi:10.1016/j.lfs.2023.122320 · Cited by 9

Pharmacologic inhibition of BAF chromatin remodeling complexes as a therapeutic approach to transcription factor-dependent cancersPreprint

Centore, R. C., Soares, L. M. M., Topal, S., Vaswani, R. G., Ichikawa, K., Li, Z., Fan, H. B., Setser, J. W., Lahr, D. L., Zawadzke, L. E., et al. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.09.11.557162 · Cited by 8

Advances in the study of the role of high-frequency mutant subunits of the SWI/SNF complex in tumors

Zhao, J., Zhu, J., Tang, Y., Zheng, K., & Li, Z. (2024) · Frontiers in Oncology · doi:10.3389/fonc.2024.1463892 · Cited by 7

Getting a Handle on Chemical Probes of Chomatin Readers

Waybright, J. M., & James, L. I. (2020) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0274 · Cited by 7

Recent Developments in Targeting Bromodomain and Extra Terminal Domain Proteins for Cancer Therapeutics

Cai, M., Dong, J., Li, H., & Qin, J. (2022) · Current Medicinal Chemistry · doi:10.2174/0929867329666220211091806 · Cited by 7

Targeted Protein Degradation of NUDT5 Reveals an Unexpected Non-Enzymatic Role in 6-Thioguanine-Mediated ToxicityPreprint

Marques, A.-S. M. C., Bauer, L. G., Nguyen, T. A., Orta, A. G., Venne, J. L., Cheng, L., Balıkçı, E., Tivon, B., London, N., Kubicek, S., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.03.16.643557 · Cited by 7

Therapeutic Discovery for Chromatin Complexes: Where Do We Stand?

Owens, D. D. G., Maitland, M. E. R., Arrowsmith, C. H., & Baršytė-Lovejoy, D. (2024) · Annual Review of Cancer Biology · doi:10.1146/annurev-cancerbio-062822-110356 · Cited by 7

Discovery of Potent, Highly Selective, and Efficacious SMARCA2 Degraders

Li, Z., Harikrishnan, L. S., Xu, G., Samanta, D., Clemente, J. C., Leng, L., Tu, W., Yang, L., Huang, L., Wang, M., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01878 · Cited by 6

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 120

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