个人信息Personal Information
教授
博士生导师
硕士生导师
主要任职:Director, State Key laboratory of Fine Chemicals
其他任职:精细化工国家重点实验室主任、国务院学科评议组成员
性别:男
毕业院校:大连理工大学
学位:博士
所在单位:化工学院
学科:应用化学. 精细化工. 化学生物学
办公地点:大连理工大学精细化工国家重点实验室
西部校区化工实验楼F-202#
http://peng-group.dlut.edu.cn/
联系方式:大连理工大学精细化工国家重点实验室 西部校区化工实验楼F-202 辽宁省大连市高新区凌工路2号,大连116024 Tel: 0411-84986306; Fax: 0411-84986292;课题组网址:http://peng-group.dlut.edu.cn/
电子邮箱:pengxj@dlut.edu.cn
Aminopeptidase-N-activated Theranostic Prodrug for NIR Tracking of Local Tumor Chemotherapy
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论文类型:期刊论文
发表时间:2018-11-21
发表刊物:ADVANCED FUNCTIONAL MATERIALS
收录刊物:SCIE、Scopus
卷号:28
期号:47
ISSN号:1616-301X
关键字:cancer diagnosis; enzyme activation; NIR tracking; theranostic prodrugs; tumor chemotherapy
摘要:The development of molecular theranostic prodrugs for in vivo cancer diagnosis and targeted chemotherapy is urgently required. Enzyme-activated prodrugs display superior selectivity as a result of cancer-specific enzymes which serve as cancer biomarkers. Herein, an aminopeptidase N (APN)-activated theranostic prodrug Nile blue-C-6-amide-p-fluorophenylalanyl-l-melphalanyl (NBFMel) is reported for fluorescence cancer diagnosis and local tumor treatment. NBFMel demonstrates negligible cytotoxicity and very weak fluorescence due to the photoinduced electron transfer (PET) between melphalan and Nile blue fluorophore. After activation caused by APN, the prodrug releases free melphalan that inhibits tumor cell growth. Simultaneously, the reaction blocks the PET process and switches on the fluorescence, which can be used for cancer diagnosis. NBFMel is successfully utilized to report the presence of tumor and for in situ tracking of drug release in tumor-bearing mouse models. Moreover, NBFMel demonstrates efficient tumor inhibition when intravenously injected into mice. Therefore, the APN-activated theranostic prodrug provides a new platform for in vivo cancer diagnosis and targeted anticancer chemotherapy.