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

Bioconjug Chem. 2011 Jun 15;22(6):1001-5. doi: 10.1021/bc200005w. Epub 2011 May 24.


Herein, we report a new type of in vivo fluorogenic probe that enables simultaneous and active targeting of overexpressed receptors, α(V)β(3) 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 α(V)β(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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Fluorescent Dyes / analysis*
  • Fluorescent Dyes / chemistry*
  • Integrin alphaVbeta3 / chemistry
  • Integrin alphaVbeta3 / metabolism*
  • Matrix Metalloproteinases / chemistry
  • Matrix Metalloproteinases / metabolism*
  • Mice
  • Molecular Imaging / methods*
  • Molecular Structure
  • Neoplasms, Experimental / metabolism
  • Peptides, Cyclic / chemistry
  • Stereoisomerism


  • Fluorescent Dyes
  • Integrin alphaVbeta3
  • Peptides, Cyclic
  • cyclic arginine-glycine-aspartic acid peptide
  • Matrix Metalloproteinases