A review of the known MTA-cooperative PRMT5 inhibitors

Mei Hu and Xiang Chen

RSC Adv., 2024, 14, 39653
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Design, synthesis, and biological evaluation of novel BTK-targeting proteolysis targeting chimeras (PROTACs) with enhanced pharmacokinetic properties

Ying Lin, Jing Liu, Xinjian Tian, Jin Wang, Huahua Su, Jianpin Xiang, Tao Cao, Yonghui Wang, Qiong Xie and Xufen Yu

European Journal of Medicinal Chemistry, 2025, 289, 117420
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Generating Surprisingly Powerful Pharmacology from Chemically Induced Protein Interactions

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Fluorinated Proteolysis Targeting Chimeras-Sorafenib Nanoassembly for Epigenetic Remodeling to Combat Multi-Pathway Drug Resistance in Hepatocellular Carcinoma

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Bifaceted functions of histone methyltransferases

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PRMT7 in cancer: Structure, effects, and therapeutic potentials

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Self‐Oxygenating PROTAC Microneedle for Spatiotemporally‐Confined Protein Degradation and Enhanced Glioblastoma Therapy

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Epigenetic dysregulation in pancreatic cancer: emerging biomarkers and clinical applications

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Integrating PROTAC-based targeted protein degradation with nanodelivery systems to overcome cancer therapeutic resistance

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Chemical Epigenetics: Small Molecules Targeting Chromatin Modifiers in Disease Modulation

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Cell Biochem Biophys, 2026
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Epigenetic modifications in cancer drug resistance: molecular mechanisms and therapeutic interventions

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Mol Biomed, 2026, 7
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Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer

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J. Med. Chem., 2023, 66, 16168
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Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation

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Bridged PROTAC, DNA-based PROTAC and hydrophobic tag technologies for targeted protein degradation

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Modular Assembly of Heterotrifunctional Molecules Enabled by Iodosulfonylation of Allenes and Subsequent Amination

Xiaofeng Lin, Chuxiong Peng, Shijie Liu, Jianpin Xiang, Binyan Lin, Qichen Zhan, Peng Cao and Tao Cao

J. Med. Chem., 2024, 67, 21251
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Recent advance in the targeted protein degradation technology for overcoming acute leukemia

Xin Jin, Zhonghua Shi, Zhuo Liang, Jia Chen, Chenxi Wang, Yongxin Lou, Xiaoran Cao, Lei Zhu, Yihuan Zhao, Changkuo Zhao, Xianheng Wang and Qiang Huang

European Journal of Medicinal Chemistry Reports, 2026, 17, 100331
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Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2

Julia Velez, Brandon Dale, Kwang-Su Park, H. Ümit Kaniskan, Xufen Yu and Jian Jin

European Journal of Medicinal Chemistry, 2024, 267, 116154
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Epigenetic Therapy in Hormone Positive Breast Cancer: The Role of PIK3CA

Ryan Blawski and Eneda Toska

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Discovery of the first-in-class DOT1L PROTAC degrader

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European Journal of Medicinal Chemistry, 2025, 291, 117595
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Recent update on the development of EZH2 inhibitors and degraders for cancer therapy

Meiyue Tang, Ming Gong, Xiaoliang Liu, Tiantian Zhang, Zhenghua Liu and Dandan Song

European Journal of Medicinal Chemistry, 2025, 299, 118106
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(+)-Miliusol suppresses the Warburg effect and induces regulated cell death in triple-negative breast cancer through targeting EIF3D and remodeling cancer metabolism

Jin Zhang, Lin Jia, Xiya Chen, Yan Wu, Xiaohan Sun, Ling Zou, Xiaoling Cheng, Jingnan Huang, Hongchao Zhou, Lingyun Dai, Le Zhou, Zhendan He, Bo Liu, Yue Hao and Dahong Yao

Acta Pharmaceutica Sinica B, 2026
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A Second-Generation Route to the Cereblon Fragment of ARV-471, Vepdegestrant

David J. Bernhardson, Jonathan Fifer, Zebediah C. Girvin, Ian Hotham, Johnny W. Lee, Melissa Lee, Valerie May, Blake Rauschenberger, Chase A. Salazar, Liam S. Sharninghausen, Robert A. Singer, Ryan Sullivan, Zheng Wang, Ethan Weinstein, Gerald A. Weisenburger and Joseph M. Zanghi

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Histone Modifications in Cardiovascular Disease: Mechanisms and Therapeutic Opportunities

Yu Zheng, Yu‐Xuan Gao, Mei‐Xing Guo, Li‐Ting Wang, Xiao‐Wen Zheng, Yi‐Hao Liao, Ya Li, Jun‐Ping Zhu and Jia‐Ming Wei

MedComm, 2026, 7
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Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader

Md Kabir, Lihuai Qin, Kaixiu Luo, Yan Xiong, Rebecca A. Sidi, Kwang-Su Park and Jian Jin

J. Med. Chem., 2024, 67, 6880
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Liver-targeting chimeras as a potential modality for the treatment of liver diseases

Chuanjie Chen, Yongzhang Pan, Xiaoyu Yang, Huiqin Li, Xinhui Cai, Shengyuan He, Qiong Wang, Yiwen Yang, Runzi Zheng, Huiwen Li, Shengjie Yuan, Xin Dong, Priyadarshani Nadeeshika Samarawickrama, Meiting Zi, Yonghan He and Xuan Zhang

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Targeted degradation of CDK4/6 by LA-CB1 inhibits EMT and suppresses tumor growth in orthotopic breast cancer

Jingliang He, Shunfang Liu, Siyi Zhang, Qi Gao, Lan Zhu, Ningyang Xu, Zhongke Hu, Xingyu Zhang, Shaojie Ma, Xiujun Wang, Bin Liu and Wei Liu

Sci Rep, 2025, 15
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