靶向调控肿瘤相关巨噬细胞的小分子药物研究进展  

Advances in Small Molecule Drugs Targeting Tumor-Associated Macrophages

作　　者：金佳明 张庆云 王均伟 胡立宏 JIN Jiaming;ZHANG Qingyun;WANG Junwei;HU Lihong(School of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210023,China)

机构地区：[1]南京中医药大学药学院,江苏南京210023

出　　处：《药学进展》2023年第9期644-664,共21页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金(No.82173664);江苏省优秀青年基金(No.BK20220109)。

摘　　要：肿瘤相关巨噬细胞(TAMs)是肿瘤微环境中最丰富的先天免疫群体,也是形成免疫抑制微环境的主要推手,在肿瘤免疫逃避过程中起着至关重要的作用。因此,靶向调控TAMs已成为癌症免疫治疗的一种新策略。目前研究发现多种信号通路在调控TAMs功能中发挥重要作用,针对这些信号通路的小分子药物可通过调控TAMs功能发挥抗肿瘤作用,其中多个药物处于不同临床研究阶段。通过对调控TAMs功能的信号通路及相关小分子抑制剂的研发历程、结合模式等方面进行系统综述,以期为调控TAMs的小分子药物的研发提供思路。Tumor-associated macrophages(TAMs),the most abundant innate immune population in the tumor microenvironment and the main driving force in the formation of immunosuppressive microenvironment,play a crucial role in tumor immune escape.Therefore,targeted regulation of TAMs has become a new strategy for cancer immunotherapy.Recent studies have found that a variety of signaling pathways play an important role in regulating the function of TAMs.Small molecule drugs targeting these signaling pathways can exert anti-tumor effects by regulating TAMs,and many of them are in different clinical trial phases.This paper systematically reviews the signaling pathways regulating the function of TAMs as well as the development process and binding mode of related small molecule inhibitors in order to provide some insight for the development of small molecule drugs regulating TAMs.

关 键 词：肿瘤微环境 免疫治疗 肿瘤相关巨噬细胞 小分子抑制剂 

分 类 号：R914[医药卫生—药物化学] R979.1[医药卫生—药学]