Science China Chemistry

, Volume 61, Issue 2, pp 184–191 | Cite as

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

  • Yan Tang
  • Andong Shao
  • Jun Cao
  • Hui Li
  • Qiang Li
  • Meiying Zeng
  • Ming Liu
  • Yingsheng ChengEmail author
  • Weihong ZhuEmail author


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.


NIR fluorescence probe NGR aminopeptidase N Caveolin-1 pancreatic ductal adenocarcinoma 


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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).

Supplementary material

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


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Copyright information

© Science China Press and Springer-Verlag GmbH Germany, part of Springer Nature 2017

Authors and Affiliations

  • Yan Tang
    • 1
  • Andong Shao
    • 2
  • Jun Cao
    • 3
  • Hui Li
    • 1
  • Qiang Li
    • 2
  • Meiying Zeng
    • 1
  • Ming Liu
    • 2
  • Yingsheng Cheng
    • 1
    Email author
  • Weihong Zhu
    • 2
    Email author
  1. 1.Department of RadiologyShanghai Jiao Tong University Affiliated Sixth People’s HospitalShanghaiChina
  2. 2.Key Laboratory for Advanced Materials and Institute of Fine Chemicals, Shanghai Key Laboratory of Functional Materials Chemistry, School of Chemistry and Molecular EngineeringEast China University of Science and TechnologyShanghaiChina
  3. 3.Department of Interventional OncologyDahua HospitalShanghaiChina

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