靶向PD-1/PD-L1的新策略:降解剂、双功能分子及共价抑制剂OA北大核心CSTPCD
New strategies for targeting PD-1/PD-L1:degraders,bifunctional molecules and covalent inhibitors
靶向细胞程序性死亡受体-1(programmed cell death protein-1,PD-1)/细胞程序性死亡配体-1(programmed cell death ligand-1,PD-L1)已成为最具前景的肿瘤免疫治疗靶点之一.目前,PD-1/PD-L1单克隆抗体药物及小分子抑制剂都面临着相应的发展瓶颈,许多研究者尝试探索不同的策略以阻断PD-L1/PD-L1通路,期望改善肿瘤治疗的效果.本文总结了靶向PD-L1的降解剂、双功能分子及共价抑制剂,旨在为PD-1/PD-L1药物的开发提供有益的思路.
Programmed cell death protein-1(PD-1)/programmed cell death ligand-1(PD-L1)has been considered to be one of the most promising targets for tumor immunotherapy.At present,both monoclonal antibody drugs and small molecule inhibitors targeting PD-1/PD-L1 are facing bottlenecks.Numerous researchers have tried to explore different strategies to block the PD-L1/PD-L1 pathway,hoping to improve the effects of tumor immunotherapy.This review focuses on the degraders,bifunctional molecules and covalent inhibitors that target PD-L1,aiming to provide inspiring insights for the development of anti-PD-1/PD-L1 drugs.
王志杰;廖晓彤;郭霞;陈建军
南方医科大学深圳医院, 深圳 518100||南方医科大学药学院, 广州 510515南方医科大学药学院, 广州 510515南方医科大学深圳医院, 深圳 518100
药学
PD-1/PD-L1肿瘤免疫降解剂双功能分子共价抑制剂
PD-1/PD-L1tumor immunotherapydegradersbifunctional moleculescovalent inhibitors
《中国药科大学学报》 2024 (001)
靶向PD-L1&CXCL12双功能小分子的设计、合成及作为癌症双免疫疗法的研究
5-14 / 10
This study was supported by the National Natural Science Foundation of China(No.82173668,No.82373706)国家自然科学基金项目(No.82173668,No.82373706)
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