Dual-functional, receptor-targeted fluorogenic probe for in vivo imaging of extracellular protease expressions |
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Authors: | Zhu Lei Xie Jin Swierczewska Magdalena Zhang Fan Lin Xin Fang Xuexun Niu Gang Lee Seulki Chen Xiaoyuan |
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Institution: | National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Maryland 20892, United States. |
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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. |
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