Design of activatable molecular probes for multimodality imaging of enzyme activity in vivo
【摘要】：Precise measurement of enzyme activity in living systems with molecular imaging probes is highly important in unraveling the functional roles of different enzymes in biological processes. Recent progress have been actively made on the development of a myriad of molecular imaging probes featured with different imaging modalities,including optical imaging, magnetic resonance imaging(MRI), nuclear imaging, and photoacoustic imaging, allowing for non-invasive detection of various enzyme activities in vivo with high sensitivity and high spatial resolution. Among these imaging probes, activatable probes whose imaging signals can be specifically switched from"off"to"on"state upon interaction with a target enzyme of interest are particularly attractive owing to the improved sensitivity and specificity. These probes can be applied for the real-time imaging of enzyme activity as well as for the rapid screening of inhibitors of targeted enzyme both in culture cells and in living animals [1-3]. In this talk, I will briefly discuss the general strategy for the design of activatable probes(Figure 1 a), and give some examples that my lab has been doing to detect different enzymes, such as cathepsin B, caspase-3, and GGT both in live cells and living animals.