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Research progress of LAG-3 in tumor immunity and targeted drug development
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Hang GONG, Xin ZHAO, Wen-xia CHEN, Ni-na XUE*
Acta Pharmaceutica Sinica | 2025, 60(5) : 1315 - 1324
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Acta Pharmaceutica Sinica | 2025, 60(5): 1315-1324
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Research progress of LAG-3 in tumor immunity and targeted drug development
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Hang GONG, Xin ZHAO, Wen-xia CHEN, Ni-na XUE*
Affiliations
  • State Key Laboratory of Bioactive Substances and Functions of Natural Medicines/Beijing Key Laboratory of Non-clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2025-05-12 doi: 10.16438/j.0513-4870.2024-1290
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Lymphocyte activation gene 3 (LAG-3) is an important inhibitory receptor on T cells, which plays a crucial role in tumor immune evasion. LAG-3 is primarily expressed on activated T cells, natural killer (NK) cells and B cells, et al. By binding to its ligands, LAG-3 inhibits T cell proliferation, activation, and effector functions. LAG-3 has emerged as the third immune checkpoint protein (ICP) used in clinical practice, following programmed death 1 (PD-1)/programmed death ligand 1 (PD-L1) and cytotoxic T lymphocyte-associated antigen 4 (CTLA-4). Currently, there has been at least 20 LAG-3-targeted drugs undergoing clinical trials. This article mainly reviews the structure, expression regulation, ligands, co-expressed ICP of LAG-3, as well as its application in tumor immunotherapy, and discusses the current challenges of targeting LAG-3 research.

lymphocyte activation gene 3  /  tumor microenvironment  /  tumor immunity  /  immune checkpoint inhibitor  /  monoclonal antibody
Hang GONG, Xin ZHAO, Wen-xia CHEN, Ni-na XUE. Research progress of LAG-3 in tumor immunity and targeted drug development[J]. Acta Pharmaceutica Sinica, 2025 , 60 (5) : 1315 -1324 . DOI: 10.16438/j.0513-4870.2024-1290
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Year 2025 volume 60 Issue 5
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doi: 10.16438/j.0513-4870.2024-1290
  • Receive Date：2024-12-25
  • Online Date：2025-10-29
  • Published：2025-05-12
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  • Received：2024-12-25
  • Revised：2025-02-09
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    State Key Laboratory of Bioactive Substances and Functions of Natural Medicines/Beijing Key Laboratory of Non-clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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