Cancer Imaging and Diagnostics

About

INVENTION Two types of peptide-conjugated aggregation-induced emission (AIE) fluorogen probes, namely a c-RGD conjugated tetraphenylsilole (TPS-2cRGD) probe and a DEVD peptide-conjugated tetraphenylethene (TPE) probe (AcDEVDK-TPE) have been designed. These probes are initially non-fluorescent due to their good water solubility. Upon addition of the corresponding proteins, specific binding between TPS-2cRGD and integrin αVβ3 can significantly restrict the molecular rotations of silole core, leading to fluorescence turn-on of the probe. These fluorescence turn-on features allow protein detection both in solution and in cells. Preliminary testing shows that TPS-2cRGD probe could not only be used for detection of integrin αVβ3-positive cancer cells but also has the potential to trace the internalization of integrin αVβ3 in real-time manner. Additionally, AcDEVDK-TPE is not only capable of monitoring the activities of caspase-3/caspase-7 but would also be suitable for cell apoptosis study. This invention is fundamental and would open up a new avenue for the development of AIE-active biocompatible probes for clinical cancer imaging and diagnostics. Key Benefits Conventional commercial fluorescent probes have the problem of self-quenching and high fluorescent background. This series of fluorescence turn-on probes have the following competitive advantages when compared with the conventional probes: Easy to synthesize Low preparation cost High fluorescence contrast High sensitivity Stable at ambient conditions Easy to store Market for this invention is promising. Collaboration partners could be medical device manufacturers which focus on fluorescence imaging technology.