用于肿瘤免疫治疗的CD73小分子抑制剂研究进展  

Research Progress in CD73 Small Molecule Inhibitors for Tumor Immunotherapy

作　　者：杨羚羚 陈曦 姜莹莹 宁香丽 李国菠 YANG Lingling;CHEN Xi;JIANG Yingying;NING Xiangli;LI Guobo(School of Food and Bioengineering,Xihua University,Chengdu 610039 China;West China School of Pharmacy,Sichuan University,Chengdu 610041 China)

机构地区：[1]西华大学食品与生物工程学院,四川成都610039 [2]四川大学华西药学院,四川成都610041

出　　处：《西华大学学报（自然科学版）》2024年第4期100-109,148,共11页Journal of Xihua University:Natural Science Edition

基　　金：四川省科技厅自然科学面上项目(2023NSFSC0606);四川省科技厅青年科技创新团队项目(2023NSFSC0606)。

摘　　要：高浓度的腺苷可通过抑制肿瘤免疫反应和刺激肿瘤血管生成来促进肿瘤生长,在免疫逃逸和肿瘤进展中发挥重要作用。大量的腺苷由外切核苷酸酶CD73产生,因此通过抑制CD73的活性来调控腺苷水平可能是未来肿瘤免疫治疗的一种很有前途的治疗策略。截至目前,对CD73抑制剂的研究仍处于早期阶段,尚无CD73小分子抑制剂被批准上市。本文简要综述目前报道的CD73小分子抑制剂在其抑制作用和结构设计等方面的研究现状,并对CD73小分子抑制剂未来的研究方向进行展望,以期为靶向CD73的创新小分子药物研发提供参考。High levels of adenosine promote tumor growth by inhibiting the tumor immune response and stimulating tumor angiogenesis,plays an important role in immune escape and tumor progression.The large amount of adenosine is produced by the ecto-5'-nucleotidase CD73.Therefore,regulating adenosine levels by inhibiting the activity of CD73 may be a promising therapeutic strategy for future tumor immunotherapy.Currently,research on CD73 inhibitors is still in the early stage,and no small molecule CD73 inhibitors have been approved for marketing.This article provides a brief review of the current research status of the currently reported CD73 small molecule inhibitors in terms of their inhibitory effects and structural design,and look forward to the future research direction of CD73 small molecule inhibitors,with a view to provide more information for the development of innovative small molecule drugs targeting CD73.

关 键 词：肿瘤免疫治疗 CD73 小分子抑制剂 核苷酸类 构效关系 

分 类 号：R979.5[医药卫生—药品]