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免疫检查点PD-1/PD-L1小分子抑制剂的研究进展
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引用本文:田季平,张剑,周金培,张惠斌.免疫检查点PD-1/PD-L1小分子抑制剂的研究进展[J].中国药科大学学报,2019,50(1):1-10.
Cite:TIAN Jiping,ZHANG Jian,ZHOU Jinpei,ZHANG Huibin.Advances in small molecule inhibitors of PD-1/PD-L1 immune checkpoint pathway[J].J China Pharm Univ,2019,50(1):1-10.
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作者单位
田季平 中国药科大学新药研究中心 
张剑 中国药科大学新药研究中心 
周金培 中国药科大学新药研究中心 
张惠斌 中国药科大学新药研究中心 
中文摘要:研究发现多种肿瘤通过上调自身和肿瘤微环境的PD-L1表达,持续激活PD-1(programmed cell death protein 1,PD-1)/PD-L1(programmed cell death-ligand 1)信号通路,抑制T细胞的功能,导致肿瘤免疫逃逸的发生。目前已有多种PD-1/PD-L1单抗药物上市,并且获得了较为满意的临床效果。但因为单抗生产成本高昂,存储运输条件苛刻,有免疫原性等问题,寻找免疫检查点PD-1/PD-L1小分子抑制剂成为了当前新药开发的热点。本文详细介绍了PD-1/PD-L1的生物学机制,按结构分类综述了PD-1/PD-L1小分子抑制剂的研究进展,并对小分子抑制剂的研发进行了展望。
中文关键词:肿瘤免疫  PD-1/PD-L1  免疫检查点  小分子抑制剂  进展
 
Advances in small molecule inhibitors of PD-1/PD-L1 immune checkpoint pathway
Abstract:Studies have found that a variety of tumors continue to activate PD-1(programmed cell death protein 1, PD-1)/PD-L1(programmed cell death-ligand 1)signaling pathway by up-regulating PD-L1 expression in tumor cells and microenvironment. The dysfunction of T cells leads to the occurrence of tumor immune escape. Several PD-1/PD-L1 monoclonal antibodies have been marketed to achieve significant clinical efficacy. However, because of the high production cost, the harsh conditions for storage and transportation, and the potential immunogenicity of monoclonal antibody, the seeking for PD-1/PD-L1 small molecule inhibitors has become a hot spot in the development of new drugs. In this paper, the biological mechanisms of PD-1/PD-L1 was introduced in detail. Based on the structural classification, the research progress of PD-1/PD-L1 small molecule inhibitors was reviewed, with a prospect of the development of small molecule inhibitors.
keywords:tumor immunology  PD-1/PD-L1  immune checkpoint  small molecule inhibitor  advances
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