文献类型：期刊文献

英文题名：cNGR-based synergistic-targeted NIR fluorescent probe for tracing and bioimaging of pancreatic ductal adenocarcinoma

作者：Tang, Yan[1];Shao, Andong[2,3];Cao, Jun[4];Li, Hui[1];Li, Qiang[2,3];Zeng, Meiying[1];Liu, Ming[2,3];Cheng, Yingsheng[1];Zhu, Weihong[2,3]

机构：[1]Shanghai Jiao Tong Univ, Dept Radiol, Affiliated Peoples Hosp 6, Shanghai 200233, Peoples R China;[2]East China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Inst Fine Chem, Sch Chem & Mol Engn, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China;[4]Dahua Hosp, Dept Intervent Oncol, Shanghai 200237, Peoples R China

年份：2018

卷号：61

期号：2

起止页码：184

外文期刊名：SCIENCE CHINA-CHEMISTRY

收录：;EI(收录号：20173304049157);WOS:【SCI-EXPANDED(收录号:WOS:000424012300008)】；

基金：This work was supported by the National Basic Research Program of China (2013CB733700), the National Natural Science Foundation of China for Creative Research Groups (21421004), Key Project (21636002), and Distinguished Young Scholars (21325625), NSFC/China, the Oriental Scholarship, Science and Technology Commission of Shanghai Municipality (15XD1501400), the Fundamental Research Funds for the Central Universities (222201717003), and Program of Introducing Talents of Discipline to Universities (B16017).

语种：英文

外文关键词：NIR fluorescence probe; NGR; aminopeptidase N; Caveolin-1; pancreatic ductal adenocarcinoma

摘要：Identification of fluorescent biomarkers with peptide ligand-directed receptors for diagnosis or theranostic of pancreatic ductal adenocarcinoma (PDAC) is still challenging. As potential prognostic/predictive bioimaging targets, both aminopeptidase N (APN, known as CD13) and Caveolin-1 are found as upregulation on the cell membrane surface of PDAC, in which APN is the principal receptor of the cyclic peptide cNGR (Asn-Gly-Arg, NGR) and Caveolin-1 can synergistically mediate endocytosis in this receptor-targeted process. Herein, we conjugate cNGR to dicyanomethylene-4H-pyran (DCM) chromophore to develop a synergistic-targeted near-infrared (NIR) fluorescent probe DCM-cNGR with strongly intrinsic NIR fluorescence, stable optical performance, low cytotoxicity, and rapid accumulation in PANC-1 cells with the synergistic overexpressed APN receptor-targeted and Caveolin-1-mediated endocytosis. As demonstrated, DCM-cNGR can realize noninvasive NIR imaging for targeting PANC-1 tumor in vivo after intravenous injection into PANC-1 xenograft tumor of nude mice, making a great promise to improve the precision diagnosis and therapy of pancreatic cancer with real time tracing and bioimaging of PDAC in vitro and in vivo.