Dual-functional, receptor-targeted fluorogenic probe for in vivo imaging of extracellular protease expressions

Lei Zhu, Jin Xie, Magdalena Swierczewska, Fan Zhang, Xin Lin, Xuexun Fang, Gang Niu, Seulki Lee, Xiaoyuan Chen

Research output: Contribution to journalArticle


Herein, we report a new type of in vivo fluorogenic probe that enables simultaneous and active targeting of overexpressed receptors, αVβ3 integrins, and extracellular proteases, matrix metalloproteinases (MMPs), in the tumor regions. This c(RGDyK)-conjugated MMP fluorogenic probe efficiently targets the tumor regions with high retention time while maintaining receptor binding affinity and substrate activity. The probe minimizes nonspecific accumulation, thus demonstrating improved tumor-to-background signal ratio (T/N) in both αVβ 3 integrin- and MMP-overexpressing U87MG tumor-bearing mouse model. This strategy can be easily tuned for a wide array of applications targeting various receptors and extracellular proteases in vivo.

Original languageEnglish (US)
Pages (from-to)1001-1005
Number of pages5
JournalBioconjugate Chemistry
Issue number6
Publication statusPublished - Jun 15 2011
Externally publishedYes


ASJC Scopus subject areas

  • Biotechnology
  • Bioengineering
  • Organic Chemistry
  • Pharmaceutical Science
  • Biomedical Engineering
  • Pharmacology

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