中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
A pentapeptide enabled AL3810 liposome-based glioma-targeted therapy with immune opsonic effect attenuated

文献类型:期刊论文

作者Li, Jinyang2,3; Lu, Jiasheng2,3; Guo, Haiyan2,3; Zhou, Jianfen2,3; Wang, Songli2,3; Jiang, Kuan2,3; Chai, Zhilan2,3; Yao, Shengyu2,3; Wang, Xiaoyi2,3; Lu, Linwei7
刊名ACTA PHARMACEUTICA SINICA B
出版日期2021
卷号11期号:1页码:283-299
关键词Liposome mn c(RGDyK) Immune opsonization Immunogenicity Anti-glioma efficacy
ISSN号2211-3835
DOI10.1016/j.apsb.2020.07.024
通讯作者Lu, Weiyue(wylu@shmu.edu.cn)
英文摘要AL3810, a molecular dual inhibitor of the vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR), has earned the permission of phase II clinical trial for tumor treatment by China FDA. As a reversible ATP-competitive inhibitor, AL3810 targets ATP-binding site on intracellular region of VEGFR and FGFR, whereas, AL3810 lacking interplay with extracellular region of receptors rendered deficient blood-brain tumor barrier (BBTB) recognition, poor brain penetration and unsatisfactory anti-glioma efficacy. Integrin crvd3 overexpressed on capillary endothelial cells of BBTB as well as glioma cells illuminated ligand-modified liposomes for pinpoint spatial delivery into glioma. The widely accepted peptide c(RGDyK)-modified liposome loading AL3810 of multiple dosing caused hypothermia, activated anti-c(RGDyK)-liposome IgG and IgM antibody and pertinent complements C3b and C5b-9, and experienced complement-dependent opsonization. We newly proposed a pentapeptide mn with superb crvd3-binding affinity and tailored AL3810-loaded mn-modified liposome that afforded impervious blood circulation, targeting ability, and glioma therapeutic expertise as vastly alleviated immune opsonization on the underpinning of the finite antibodies and complements assembly. Stemming from attenuated immunogenicity, peptide mn strengthened liposome functions as a promising nanocarrier platform for molecular targeting agents. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
WOS关键词BLOOD-BRAIN-BARRIER ; GROWTH-FACTOR RECEPTOR ; ATHYMIC NUDE-MICE ; CANCER ; COMPLEMENT ; MECHANISMS ; EXPRESSION ; NORMALIZATION ; ANAPHYLAXIS ; CLEARANCE
资助项目National Natural Science Foundation of China[81773657] ; National Natural Science Foundation of China[81690263] ; Innovation Program of Shanghai Municipal Education Commission (China)[2017-01-07-00-07E00052] ; National Basic Research Program of China (973 Program, China)[2013CB932500]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000610494400019
出版者INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
源URL[http://119.78.100.183/handle/2S10ELR8/295907]  
专题中国科学院上海药物研究所
通讯作者Lu, Weiyue
作者单位1.Fudan Univ, Minhang Branch, Minghang Hosp, Zhongshan Hosp, Shanghai 201199, Peoples R China
2.Fudan Univ, Sch Pharm, Dept Pharmaceut, Shanghai 201203, Peoples R China
3.Fudan Univ, Key Lab Smart Drug Delivery, Minist Educ & PLA, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
5.Fudan Univ, Inst Brain Sci, State Key Lab Med Neurobiol, Shanghai 200032, Peoples R China
6.Fudan Univ, Inst Brain Sci, MOE Frontiers Ctr Brain Sci, Shanghai 200032, Peoples R China
7.Fudan Univ, Inst Integrat Med, Shanghai 200041, Peoples R China
8.Fudan Univ, Minghang Hosp, Inst Fudan Minghang Acad Hlth Syst, Shanghai 201199, Peoples R China
推荐引用方式
GB/T 7714
Li, Jinyang,Lu, Jiasheng,Guo, Haiyan,et al. A pentapeptide enabled AL3810 liposome-based glioma-targeted therapy with immune opsonic effect attenuated[J]. ACTA PHARMACEUTICA SINICA B,2021,11(1):283-299.
APA Li, Jinyang.,Lu, Jiasheng.,Guo, Haiyan.,Zhou, Jianfen.,Wang, Songli.,...&Lu, Weiyue.(2021).A pentapeptide enabled AL3810 liposome-based glioma-targeted therapy with immune opsonic effect attenuated.ACTA PHARMACEUTICA SINICA B,11(1),283-299.
MLA Li, Jinyang,et al."A pentapeptide enabled AL3810 liposome-based glioma-targeted therapy with immune opsonic effect attenuated".ACTA PHARMACEUTICA SINICA B 11.1(2021):283-299.

入库方式: OAI收割

来源:上海药物研究所

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