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A Medicinal Chemistry Perspective on Protein Tyrosine Phosphatase Nonreceptor Type 2 in Tumor Immunology

文献类型：期刊论文

作者Huang, Qi4,5; Hu, Linghao5,6; Chen, Haowen3,5; Yang, Bingjie2,5,6; Sun, Xun1,4; Wang, Mingliang2,3,5,6
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2025-02-12
卷号68期号:4页码:3995-4021
ISSN号0022-2623
DOI10.1021/acs.jmedchem.4c01802
通讯作者Sun, Xun(sunxunf@shmu.edu.cn) ; Wang, Mingliang(wangmingliang@simm.ac.cn)
英文摘要PTPN2 (protein tyrosine phosphatase nonreceptor type 2) is an important member of the protein tyrosine phosphatase (PTP) family. It plays a crucial role in dephosphorylating tyrosine-phosphorylated proteins and modulating critical signaling pathways associated with T-cell receptors, IL-2, IFN gamma, and various cytokines. In recent years, the PTPN2's biological role has been clarified, particularly since its association with tumor immunology was gradually revealed in 2017, making it a star target for cancer immunotherapy. The dual inhibitor AC484, which targets both PTPN2 and PTP1B, is currently undergoing phase I clinical trials. This advancement has attracted great interest from researchers to develop new drugs based on its unique structure. This review outlines the structural modification processes of PTPN2-targeted agents, focusing primarily on inhibitors and degraders. Finally, this review endeavors to provide a comprehensive perspective on the evolving field of PTPN2-targeted drug discovery for tumor immunotherapy, offering valuable insights for future drug development.
WOS关键词STRUCTURE-BASED DESIGN ; T-CELL ; PTP INHIBITOR ; NEGATIVE REGULATOR ; POTENT INHIBITION ; INSULIN-RECEPTOR ; STRUCTURAL BASIS ; IN-VIVO ; TCPTP ; ACTIVATION
资助项目Shanghai Science and Technology Development Foundation[22YF1457600] ; Shanghai Science and Technology Development Funds[2023M733629] ; China Postdoctoral Science Foundation
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001419528900001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/316236]  
专题中国科学院上海药物研究所
通讯作者Sun, Xun; Wang, Mingliang
作者单位1.Fudan Univ, Inst Integrat Med, 12 Wulumuqi Zhong Rd, Shanghai 200040, Peoples R China
2.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China
3.Southern Med Univ, Sch Pharmaceut Sci, Guangzhou 510515, Guangdong, Peoples R China
4.Fudan Univ, Sch Pharm, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Zhongshan Inst Drug Discovery, Zhongshan 528400, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Huang, Qi,Hu, Linghao,Chen, Haowen,et al. A Medicinal Chemistry Perspective on Protein Tyrosine Phosphatase Nonreceptor Type 2 in Tumor Immunology[J]. JOURNAL OF MEDICINAL CHEMISTRY,2025,68(4):3995-4021.
APA Huang, Qi,Hu, Linghao,Chen, Haowen,Yang, Bingjie,Sun, Xun,&Wang, Mingliang.(2025).A Medicinal Chemistry Perspective on Protein Tyrosine Phosphatase Nonreceptor Type 2 in Tumor Immunology.JOURNAL OF MEDICINAL CHEMISTRY,68(4),3995-4021.
MLA Huang, Qi,et al."A Medicinal Chemistry Perspective on Protein Tyrosine Phosphatase Nonreceptor Type 2 in Tumor Immunology".JOURNAL OF MEDICINAL CHEMISTRY 68.4(2025):3995-4021.

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来源：上海药物研究所

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