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

• 来源期刊: 中国科学:化学（英文版）
• 年，卷（期）: 2018,（2）
• 页码范围: 184-191
• 页数: 8页
• 语种: 英文

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.