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Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging

文献类型：期刊论文

作者Zhu, Shulei2; Li, Yalei1; Huang, Yushu2; Zhang, Minmin1; Gu, Xiaofan2; He, Yang2; Liu, Hongchun1; Ma, Mingliang2,3; Lu, Wei2
刊名JOURNAL OF MATERIALS CHEMISTRY B
出版日期2020-03-07
卷号8期号:9页码:1878-1896
ISSN号2050-750X
DOI10.1039/c9tb02505g
通讯作者Ma, Mingliang(mlma@brain.ecnu.edu.cn) ; Lu, Wei(wlu@chem.ecnu.edu.cn)
英文摘要Cancer-specific bioimaging has been correlated with fluorescence-guided tumor therapy, garnering extensive interest from researchers. Herein, a highly efficient tumor-targeting fluorescent probe (NP-001), which is integrated with 4-hydroxy-1,8-naphthalimide and NVP-AUY922, for tumor imaging has been established. 4-Hydroxy-1,8-naphthalimide is a fluorescent molecule with remarkable imaging compatibility. NVP-AUY922 is a heat shock protein 90 (HSP90) inhibitor with preferential tumor selectivity that is conjugated to 4-hydroxy-1,8-naphthalimide as a tumor-targeting ligand. NP-002, a resorcinol-blocked probe which prevented binding with an amino acid residue of the HSP90 ATP binding pocket, was also synthesized as a control. In vitro and ex vivo assays showed that NP-001 could arrest cell proliferation, induce apoptosis and accumulate to inhibit HSP90. Confocal laser scanning microscopy (CLSM) also confirmed that NP-001 could be selectively internalized by tumor cells for cancer-specific bioimaging. Moreover, pharmacokinetic studies and histological analysis also indicated that NP-001 had a relatively longer retention time and showed no major organ-related toxicities. Overall, these encouraging data suggest that NP-001 is a promising new candidate for the early diagnosis of metastatic disease as well as targeted tumor imaging.
WOS关键词SHOCK-PROTEIN 90 ; MOLECULAR CHAPERONE ; EXTRACELLULAR HSP90 ; BREAST-CANCER ; TUMOR-GROWTH ; IN-VITRO ; INHIBITORS ; DISCOVERY ; PATHWAYS ; BIOMOLECULES
资助项目China Postdoctoral Science Foundation[2019M651435]
WOS研究方向Materials Science
语种英语
WOS记录号WOS:000519095400005
出版者ROYAL SOC CHEMISTRY
源URL[http://119.78.100.183/handle/2S10ELR8/281138]  
专题新药研究国家重点实验室
通讯作者Ma, Mingliang; Lu, Wei
作者单位1.Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
2.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China
3.East China Normal Univ, Key Lab Brain Funct Genom, Minist Educ, Sch Life Sci, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China
推荐引用方式
GB/T 7714		 Zhu, Shulei,Li, Yalei,Huang, Yushu,et al. Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging[J]. JOURNAL OF MATERIALS CHEMISTRY B,2020,8(9):1878-1896.
APA Zhu, Shulei.,Li, Yalei.,Huang, Yushu.,Zhang, Minmin.,Gu, Xiaofan.,...&Lu, Wei.(2020).Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging.JOURNAL OF MATERIALS CHEMISTRY B,8(9),1878-1896.
MLA Zhu, Shulei,et al."Optimized HSP90 mediated fluorescent probes for cancer-specific bioimaging".JOURNAL OF MATERIALS CHEMISTRY B 8.9(2020):1878-1896.

入库方式： OAI收割

来源：上海药物研究所

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