Chemistries of bifunctional PROTAC degraders

Cao, Chaoguo, He, Ming, Wang, Liguo, He, Yuna, Rao, Yu·2022·Chemical Society Reviews

DOI 10.1039/d2cs00220e

Cited by (315)

Items 101–200 of 315

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New PROTAC Designs for Targeted Protein Degradation in 2021–2025: Novel E3 Ligases and Pre-PROTACs
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Photocatalytic hydro-fluorosulfonylation of alkenes with N -fluorosulfonyl aldimines
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Yangguo Zhou, Qiong Zhang, Ziquan Zhao, Xiuqi Hu, Qidong You, Zhengyu Jiang · 2024 · European Journal of Medicinal Chemistry
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Yuxuan Wei, Zuxiao Chen, Chu‐Yu Huang, Hong Bo Cheng, Xiaofeng Jiang, Shiying Li · 2024 · Chemical Engineering Journal
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Hui Chen, Artem Gridnev, Netanya S. Schlamowitz, Wanyi Hu, Kuntala Dey, Guangrong Zheng, Jyoti R. Misra · 2024 · Heliyon
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Hua Yang, Jinling Qin, Yuanyuan Pei, Sumeng Guan, Mei Zhao, Yingge Wang, Yongfang Yao, Yongtao Duan, Moran Sun · 2023 · European Journal of Medicinal Chemistry
Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo
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Potential of the nanoplatform and PROTAC interface to achieve targeted protein degradation through the Ubiquitin–Proteasome system
Hanshu Xie, Chao Zhang · 2024 · European Journal of Medicinal Chemistry
Next-generation cancer therapeutics: PROTACs and the role of heterocyclic warheads in targeting resistance
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Qiuyue Zhang, Jia Yu, Qidong You, Lei Wang · 2024 · Journal of Medicinal Chemistry
A practical “preTACs-cytoblot” platform accelerates the streamlined development of PROTAC-based protein degraders
Zijian Rao, Kailin Li, Ju-Eun Hong, Danni Chen, Baoli Ding, Jiang Li, Xuxin Qi, Jiawen Hu, Bo Yang, Qiaojun He et al. · 2023 · European Journal of Medicinal Chemistry
Targeting Metabolism: Innovative Therapies for MASLD Unveiled
Weixin Wang, Xin Gao, Wentong Niu, Jinping Yin, Kan He · 2025 · International Journal of Molecular Sciences
Primary Amine-Based Photoclick Chemistry: From Concept to Diverse Applications in Chemical Biology and Medicinal Chemistry
Hao Hu, Hui‐Jun Nie, Xiaohua Chen · 2025 · Accounts of Chemical Research
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Xinyu Gou, Song He, Bilan Wang, Lingli Zhang, Yongzhong Cheng, Xiang Gao · 2025 · Advanced Drug Delivery Reviews
Nano Proteolysis Targeting Chimeras (PROTACs) with Anti‐Hook Effect for Tumor Therapy
Ni‐Yuan Zhang, Da‐Yong Hou, Xingjie Hu, Jian‐Xiao Liang, Man‐Di Wang, Zhang‐Zhi Song, Yi Li, Zhijia Wang, Hong‐Wei An, Wanhai Xu et al. · 2023 · Angewandte Chemie
Discovery of Potent and Selective c-Met Degraders for Hepatocellular Carcinoma Treatment
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Advancements in PROTAC-based therapies for neurodegenerative diseases
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Yangyang Chen, Yang Li, Jing Gao, Quanwei Yu, Yiwen Zhang, Jifa Zhang · 2024 · European Journal of Medicinal Chemistry
The application of PROTACs in immune-inflammation diseases
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Ligand-Directed Self-Assembling Chimeras for Targeted Protein O-GlcNAcylation
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Stimuli‐Responsive PROTACs for Controlled Protein Degradation
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A one-pot photocatalytic triazole-based linkerology for PROTACs
Jinhua Liu, Yaqi Deng, Jiabin Yin, Jian Ji, Cong Guan, Xuwen Chen, Xiang Wu, Tong Zhu, Shunying Liu · 2024 · Cell Reports Physical Science
Discovery of a Potent, selective and orally bioavailable CDK9 degrader for targeting transcription regulation in Triple-Negative breast cancer
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Jacopo Zattoni, Paola Vottero, Gea Carena, Chiara Uliveto, Giulia Pozzati, Benedetta Morabito, Ebenezea Gitari, Jack A. Tuszyński, Maral Aminpour · 2025 · Computer Methods and Programs in Biomedicine
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Rational modification of PROTACs for tumor-selective protein degradation
Zhongliang Fu, Meichen Pan, Chunrong Yang, Hongwei Hou, Jinghong Li · 2026 · Advanced Drug Delivery Reviews
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Liguo Wang, Zhouli Yang, Guangchen Li, Yongbo Liu, Chao Ai, Yu Rao · 2023 · Frontiers of Medicine
In Vivo Self‐Assembly of PROTACs by Bioorthogonal Chemistry for Precision Cancer Therapy
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In situ construction of intracellular supramolecular assemblies as an alternative strategy for protein degradation
Xiaoqian Hu, Qingxin Yao, Xiaobo Wu, Jiali Chen, Ruijia Zhang, Yan Zhao, Yuan Gao · 2025 · Nature Communications
Discovery of selective platelet-derived growth factor receptor-beta (PDGFR-β) bifunctional small-molecule degraders
Ru Si, Nanxin Liu, Jin Wang, Qingqing Zhang, Yanchen Li, Xiaoyan Pan, Jie Zhang · 2022 · Bioorganic & Medicinal Chemistry
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A Peptide-Based PROTAC Degrader of BRCA2 Sensitizes Metastatic Castration-Resistant Prostate Cancer to PARP Inhibition
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Split‐Deliver‐Click: Tumor‐Specific Protein Degradation via “AND” Logic‐Gated In‐Cell Bioorthogonal Clicking of PROTACs
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Tommaso Palomba, Giusy Tassone, Carmine Vacca, Matteo Bartalucci, Aurora Valeri, Cecilia Pozzi, Simon Cross, Lydia Siragusa, Jenny Desantis · 2022 · International Journal of Molecular Sciences
Selection of DNA-encoded Chemical Libraries for Compounds that can Induce Protein Ubiquitination
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Federica Carolina Balestrero, Laura Gioiello, Georgia Goutsiou, Sabina Sangaletti, Rita Maria Concetta Di Martino, Fabrizio Condorelli, Ambra A. Grolla, Tracey Pirali · 2025 · ACS Omega
Solid‐Phase Parallel Synthesis of Photocleavable Bifunctional Molecules Enables Efficient Phenotypic Protein Degrader Discovery
Baoli Ding, Jiawen Hu, Rongtian Zhang, Binyan Shou, Mengdie Chen, Jiang Li, Meng Yuan, Bo Yang, Qiaojun He, Ji Cao et al. · 2025 · Angewandte Chemie International Edition
Development and Mechanistic Evaluation of Cathepsin B‐Activatable Peptide‐Drug Conjugate PROTACs for Targeted Protein Degradation in Malignant Tumors: Advancing Precision Protein Degradation Therapeutics in Oncology
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PROTAC approaches against drug-resistant EGFR C797S/L858R/T790M mutants: biological evaluation and SAR studies (2020–2025)
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Discovery of an activatable near-infrared fluorescent and theranostic PROTAC for tumor-targeted detecting and degrading of BRD4
Keliang Li, Guoqiang Dong, Shanchao Wu, Chunquan Sheng · 2024 · Chinese Chemical Letters
Discovery of novel 20S proteasome subunit β5 PROTAC degraders as potential therapeutics for pharyngeal carcinoma and Bortezomib-resistant multiple myeloma
Shumei Wang, Zhenzhen Li, Siyue Ma, Shuxin Zhang, Shuxian Guo, Zhao Ma, Lüpei Du, Minyong Li · 2024 · Bioorganic Chemistry
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FAK inhibitors in cancer, a patent review – an update on progress
Ya‐Xi Ye, Yuyao Cao, Lisheng Xu, Hai-Chao Wang, Xinhua Liu, Hai‐Liang Zhu · 2024 · Expert Opinion on Therapeutic Patents
Synergistic DNA repair inhibition and genotoxic therapy in cisplatin-resistant tumors via microneedle-based co-delivery of PROTAC and Pt(IV)
Shenghui Wang, Runze Zhao, Mingge Hou, Xiyun Yan, Bing Ying Jiang · 2025 · Nano Research
Dynamic characteristics of proteolysis-targeting chimera systems revealed by in silico computations
Kexin Xu, Jingxuan Ge, Rongfan Tang, Tingjun Hou, Huiyong Sun · 2025 · Current Opinion in Structural Biology
Advances in light-controllable PROTACs: Design strategies, therapeutic applications and current challenges
Ji Wu, Ziyue Wang, Shi-Xuan Tan, Tingyu Li, Bingbing Chen, Qiqi Chen, Hao Li, Jin-Bo Niu, Xiang-Jing Fu, Jian Song et al. · 2025 · Bioorganic Chemistry
Opportunities and challenges of PROTAC in the treatment of protein-driven diseases
Zhe Zhou, Peng Liu, Yang Li, Xuelian Liu, Jinyao Li · 2026 · Results in Chemistry
Self-assembled Nano-PROTACs: bridging chemical design and biological barriers in targeted protein degradation
Ni‐Yuan Zhang, Jian-Xiao Liang, Bei-Ning Hu, Yi Wang, Hong‐Wei An, Hao Wang · 2026 · Advanced Drug Delivery Reviews
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Jingyu Jiang, Xinrui Yuan, Lei Hu · 2026 · Molecules
Design, synthesis and biological evaluation of novel TMPRSS2-PROTACs with florosubstituted 4-guanidino-N-phenylbenzamide derivative ligands
Hao Yang, Haoran Xu, Xinxin Lin, Zengxuan Cai, Yong Mei Xia, Yu Wang, Zejie Chen, Koutian Zhang, Yan‐Ling Wu, Jianwei Wang et al. · 2024 · Bioorganic & Medicinal Chemistry
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, Tao Cao · 2024 · Journal of Medicinal Chemistry
Rational Design, Synthesis, and Biological Evaluation of Novel c-Met Degraders for Lung Cancer Therapy
Xingyang Qiu, Qingquan Zheng, Dongdong Luo, Yue Ming, Tingting Zhang, Wenchen Pu, Min Ai, Jianhua He, Yong Peng · 2025 · Journal of Medicinal Chemistry
BRD4 as an emerging epigenetic therapeutic target for inflammatory bowel disease
Zonghui Ma, Andrew A. Bolinger, Irina V. Pinchuk, Bing Tian, Jia Zhou · 2024 · Advances in pharmacology
Discovery of the first selective and potent PROTAC degrader for the pseudokinase TRIB2
Chaowei Wen, Prathibha Reddy Gajjala, Yihan Liu, Bingzhong Chen, Mehtab S. Bal, Payal Sutaria, Qiao Yuanyuan, Yang Zheng, Yang Zhou, Jinwei Zhang et al. · 2024 · European Journal of Medicinal Chemistry
Proteolysis-Targeting Chimeras (PROTACs) targeting the BCR-ABL for the treatment of chronic myeloid leukemia – a patent review
André T. S. Vicente, Jorge A. R. Salvador · 2023 · Expert Opinion on Therapeutic Patents
A long march for targeted protein degradation in the new era: expanding E3 ligases
Dazhao Mi, A.D. Huang, Song Jingfeng, Yihua Chen · 2024 · Future Medicinal Chemistry
Expanding the druggable proteome strategies and innovations in targeted protein degradation
Ke Ma, Ting Liu, Wen-Bo Huan, Ke-Zheng Chen, Sheng‐Lin Qiao · 2025 · Nano Today
Mighty mini-PROTACs: an emerging class of degraders
Xiao Chen, Kefan Liao, Jiawei Yuan, Jianchao Zhang, Hai Rao · 2025 · European Journal of Medicinal Chemistry
Design, synthesis, and biological evaluation of novel PROTACs based on unnatural dipeptide CRBN ligands
Kun Huang, Peng Luo, Caihua Li, Nan Huang, Kun Yao, Xiong-Xiong Lan, Ling-Feng Du, Yan Miao, Qing Hua Tang, Ying Xu et al. · 2025 · European Journal of Medicinal Chemistry
Design of RGD-functionalized GSH-responsive pegylated polymeric protacs for selective BRD4 degradation and EndMT-driven cardiac fibrosis inhibition
Tao Bi, Lei Chen, Ting Wang, Wenjun Miao, Silong Zhai, Rui Huang, Qin Sun, Yuehua Chen, Hongna Su, Jie Zhou et al. · 2026 · Journal of Nanobiotechnology
An ultrasound-activated PROTAC prodrug with self-reporting fluorescence for targeted protein degradation
Tao Li, Yalan Tu, He Dong, Wenjiao Xie, Xiaoyu Pan, Youyong Yuan · 2026 · Biomaterials
PROTAC® technology and potential for its application in infection control
Maria Zakharova, М. В. Чудинов · 2024 · Fine Chemical Technologies
TRL-PROTAC: A pre-trained generator of PROTACs targeting specific proteins optimized by reinforcement learning
Yuhao Dai, Fei Zhu · 2024 · Computer Science and Information Systems
Solid‐Phase Parallel Synthesis of Photocleavable Bifunctional Molecules Enables Efficient Phenotypic Protein Degrader Discovery
Baoli Ding, Jiawen Hu, Rongtian Zhang, Binyan Shou, Mengdie Chen, Li Jiang, Meng Yuan, Bo Yang, Qiaojun He, Ji Cao et al. · 2025 · Angewandte Chemie