Dual-Functional, Receptor-Targeted Fluorogenic Probe for In Vivo Imaging of Extracellular Protease Expressions

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• 作者：Lei Zhu ; Jin Xie ; Magdalena Swierczewska ; Fan Zhang ; Xin Lin ; Xuexun Fang ; Gang Niu ; Seulki Lee ; Xiaoyuan Chen
• 刊名：Bioconjugate Chemistry
• 出版年：2011
• 出版时间：June 15, 2011
• 年：2011
• 卷：22
• 期：6
• 页码：1001-1005
• 全文大小：843K
• 年卷期：v.22,no.6(June 15, 2011)
• ISSN：1520-4812

文摘

Herein, we report a new type of in vivo fluorogenic probe that enables simultaneous and active targeting of overexpressed receptors, 伪_V尾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 伪_V尾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.