免疫检查点PD-1/PD-L1肽类抑制剂的研究进展  

Advances in Peptide-Based Inhibitors of PD-1/PD-L1 Immune Checkpoint Pathway

作　　者：陶慧敏 刘利华 程露[1] 王旻[1] 邱郑[1] TAO Hui-min;LIU Li-hua;CHENG Lu;WANG Min;QIU Zheng(Jiangsu Province State Key Laboratory,School of Life Science and Technology,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学江苏省重点实验室生命科学与技术学院,江苏南京211198

出　　处：《药物生物技术》2020年第6期574-579,共6页Pharmaceutical Biotechnology

基　　金：江苏省生物药物成药性研究重点实验室开放课题(No.JKLDBKF201708)。

摘　　要：肿瘤免疫治疗可通过抑制多种免疫检查点信号通路发挥作用,其中PD-1(Programmed cell death 1)/PD-L1(Programmed cell death ligand 1)通路抗体抑制剂获得极大成功。但随着PD-1/PD-L1单克隆抗体的临床应用,诸如生产成本高、实体肿瘤组织穿透力弱、免疫原性,免疫相关副反应严重等越来越多的限制与不足被逐渐发现。而小分子免疫检查点抑制剂的研究逐渐受到重视,其中肽类免疫检查点抑制剂具有高度的特异性和亲和力,被认为是一类具有潜力的抗体药物的补充和替代产品。文章对近年来PD-1/PD-L1肽类抑制剂的研究进行了综述。Tumor immunotherapy inhibits tumor growth by interfering various immune checkpoint pathways.Antibodies blocking(Programmed cell death 1)/PD-L1(Programmed cell death ligand 1) pathway has achieved tremendous clinic success.However,more and more limitations with these antibody drugs have been noticed such as production costs,poor tissue and tumor penetration,immunogenicity and immune-related adverse events(ir AEs).Thus,low-molecular weight inhibitors have become attractive,among which,peptide-based inhibitors are regarded as a potential supplementary and alternative of antibody because of their specificity and high affinity.In this review,the advance of PD-1/PD-L1 peptide-based inhibitors has been summarized.

关 键 词：肿瘤免疫 免疫检查点 PD-1/PD-L1相互作用 单克隆抗体 肽 抑制剂 

分 类 号：R730.51[医药卫生—肿瘤]