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Isothermal kinase-triggered supramolecular assemblies as drug sensitizers

文献类型：期刊论文

作者Liu, Dongdong2,3; Miao, Zhe2; Wu, Chengling2; He, Fangfei2; Ren, Peng1; Bai, Shuo1; Jiang, Xingyu2,3,4; Gao, Yuan2,3
刊名CHEMICAL SCIENCE
出版日期2020-01-28
卷号11期号:4页码:1132-1139
ISSN号2041-6520
DOI10.1039/c9sc04317a
英文摘要Protein kinases, the main regulators of a vast map of cellular processes, are the most attractive targets in drug discovery. Despite a few successful examples of protein kinase inhibitors, the drug discovery strategy of downregulating protein kinase activity has been quite limited and often fails even in animal models. Here, we utilize protein kinase A (PKA) activity to design PKA-triggered supramolecular assemblies with anticancer activities. Grafting a suitable peptide to PNIPAM raises the critical temperature of the LCST polymer above body temperature. Interestingly, the corresponding phosphorylated polymer has a critical temperature below body temperature, making this peptide-appended PNIPAM a suitable polymer for the PKA-triggered supramolecular assembly process. PKA-triggered assembly occurs selectively in PKA-upregulated MCF-7 cells, which disturbs the cytoskeleton and sensitizes cancer cells against doxorubicin. The chemosensitization is also observed in vivo to identify effective tumor inhibitors with satisfactory biocompatibility. Overall, this phosphorylation-induced (in principle, PKA-catalyzed) supramolecular assembly opens up a promising chemotherapy strategy for combating kinase-upregulated cancer.
WOS关键词CANCER-CELLS ; PROTEIN ; MEMBRANE ; INHIBITORS ; INDUCE
资助项目National Key R&D Program of China[2017YFA0205901] ; NSFC[21675036] ; NSFC[51873046] ; NSFC[21705029] ; NSKF[201818] ; Hundred Talents Project of the Chinese Academy of Sciences
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000510929600022
出版者ROYAL SOC CHEMISTRY
资助机构National Key R&D Program of China ; NSFC ; NSKF ; Hundred Talents Project of the Chinese Academy of Sciences
源URL[http://ir.ipe.ac.cn/handle/122111/39273]  
专题中国科学院过程工程研究所
通讯作者Gao, Yuan
作者单位1.Chinese Acad Sci, Inst Proc Engn, Beijing 100190, Peoples R China
2.Natl Ctr Nanosci & Technol, CAS Key Lab Biomed Effects Nanomat & Nanosafety, CAS Ctr Excellence Nanosci, Beijing 100190, Peoples R China
3.Univ Chinese Acad Sci, Sino Danish Coll, Beijing 100049, Peoples R China
4.Southern Univ Sci & Technol, Dept Biomed Engn, Shenzhen 518055, Guangdong, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Dongdong,Miao, Zhe,Wu, Chengling,et al. Isothermal kinase-triggered supramolecular assemblies as drug sensitizers[J]. CHEMICAL SCIENCE,2020,11(4):1132-1139.
APA Liu, Dongdong.,Miao, Zhe.,Wu, Chengling.,He, Fangfei.,Ren, Peng.,...&Gao, Yuan.(2020).Isothermal kinase-triggered supramolecular assemblies as drug sensitizers.CHEMICAL SCIENCE,11(4),1132-1139.
MLA Liu, Dongdong,et al."Isothermal kinase-triggered supramolecular assemblies as drug sensitizers".CHEMICAL SCIENCE 11.4(2020):1132-1139.

入库方式： OAI收割

来源：过程工程研究所

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