%0 Journal Article
%A Zhu, Lei
%A Xie, Jin
%A Swierczewska, Magdalena
%A Zhang, Fan
%A Lin, Xin
%A Fang, Xuexun
%A Niu, Gang
%A Lee, Seulki
%A Chen, Xiaoyuan
%D 2011
%T Dual-Functional, Receptor-Targeted Fluorogenic Probe for In Vivo Imaging of Extracellular Protease Expressions
%U https://acs.figshare.com/articles/journal_contribution/Dual_Functional_Receptor_Targeted_Fluorogenic_Probe_for_In_Vivo_Imaging_of_Extracellular_Protease_Expressions/2641801
%R 10.1021/bc200005w.s001
%2 https://ndownloader.figshare.com/files/4294036
%K MMP
%K 87MG
%K vivo fluorogenic probe
%K Extracellular Protease ExpressionsHerein
%K extracellular proteases
%K receptor binding affinity
%K α V β3 integrins
%K tumor regions
%K α V β3 integrin
%X 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 αVβ3 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.
%I ACS Publications