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CSF1R inhibitor C19 for glioma immunotherapy enabled by brain-targeting liposomal delivery

文献类型：期刊论文

作者Song, Wen-qin1,2; Wu, Yue-qian2,3; Zhu, Quan-feng4; Xia, Xing-ping1,2; Wang, Rui2; Yang, Lu1,2; Hu, Li-hong1; Wang, Jun-wei1; Huang, Yong-zhuo1,2,5; Wang, Hui-yuan2
刊名ACTA PHARMACOLOGICA SINICA
出版日期2026-02-06
页码11
关键词glioma immunotherapy tumor-associated macrophages CSF1R inhibitor blood-brain barrier brain-targeted delivery
ISSN号1671-4083
DOI10.1038/s41401-025-01727-z
英文摘要Immunotherapy targeting tumor-associated macrophages (TAMs) has emerged as a promising approach for treating glioma, driven by advances in drug discovery and development, including colony-stimulating factor 1 receptor (CSF1R) inhibitors. We previously developed a CSF1R inhibitor, C19, for TAM-targeting immunotherapy, which can reprogram TAMs and remodel the tumor immunosuppressive microenvironment. However, the application of CSF1R inhibitors in brain cancer is limited due to inefficient delivery across the blood-brain barrier (BBB). To address this limitation, we designed a brain-targeted liposomal delivery system (T12-Lipo) modified with the transferrin receptor-binding peptide T12. T12-Lipo can specifically bind to transferrin receptors, which are overexpressed in both the BBB and TAMs, thus enhancing the delivery efficiency of C19 across the BBB and to TAMs. This system promoted TAM repolarization toward an anti-tumor M1-like phenotype and thereby facilitated T-cell-mediated tumor killing. T12-Lipo improved the BBB permeability of C19, exhibiting significant therapeutic efficacy against glioma growth. The brain-targeted liposomal formulation of the CSF1R inhibitor C19 represents a promising and effective approach for glioma immunotherapy.T12 peptide-modified liposomes loaded with CSF1R inhibitor C19 can penetrate the BBB, promote M1 phenotypic differentiation of macrophages, effectively activate T-cell immunity, alleviate the tumor immunosuppressive microenvironment, and improve the therapeutic efficacy against glioma.
WOS关键词TUMOR ; CODELIVERY
资助项目National Key Research and Development Program of China[2024YFA1210200] ; National Natural Science Foundation of China[82341232] ; Natural Science Foundation of Shanghai Municipal[24ZR1477500] ; Department of Science and Technology of Guangdong Province (High-level Innovative Research Institute)[2021B0909050003] ; Zhongshan Municipal Bureau of Science and Technology[CXTD2022011]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001681838900001
出版者NATURE PUBL GROUP
源URL[http://119.78.100.183/handle/2S10ELR8/322824]  
专题国家级研究中心_原创新药研究全国重点实验室
通讯作者Wang, Jun-wei; Huang, Yong-zhuo; Wang, Hui-yuan
作者单位1.Nanjing Univ Chinese Med, Sch Pharm, Jiangsu Key Lab Funct Subst Chinese Med, Nanjing 210023, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Shanghai Univ Tradit Chinese Med, Sch Pharm, Shanghai 201203, Peoples R China
4.Shanghai Starriver Bilingual Sch, Shanghai 201108, Peoples R China
5.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528437, Peoples R China
推荐引用方式
GB/T 7714		 Song, Wen-qin,Wu, Yue-qian,Zhu, Quan-feng,et al. CSF1R inhibitor C19 for glioma immunotherapy enabled by brain-targeting liposomal delivery[J]. ACTA PHARMACOLOGICA SINICA,2026:11.
APA Song, Wen-qin.,Wu, Yue-qian.,Zhu, Quan-feng.,Xia, Xing-ping.,Wang, Rui.,...&Wang, Hui-yuan.(2026).CSF1R inhibitor C19 for glioma immunotherapy enabled by brain-targeting liposomal delivery.ACTA PHARMACOLOGICA SINICA,11.
MLA Song, Wen-qin,et al."CSF1R inhibitor C19 for glioma immunotherapy enabled by brain-targeting liposomal delivery".ACTA PHARMACOLOGICA SINICA (2026):11.

入库方式： OAI收割

来源：上海药物研究所

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