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

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

Author information

1
National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Maryland 20892, United States.

Abstract

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.

PMID:
21574650
PMCID:
PMC3118575
DOI:
10.1021/bc200005w
[Indexed for MEDLINE]
Free PMC Article

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