Specific Detection of Integrin αvβ3 by Light-Up Bioprobe with Aggregation-Induced Emission Characteristics

Specific bioprobes with fluorescence turn-on response are highly desirable for high contrast biosensing and imaging. In this work, we developed a new generation bioprobe by integrating tetraphenylsilole, a fluorogenic unit with aggregation-induced emission (AIE) characteristic, with cyclic arginine glycine aspartic acid tripeptide (cRGD), a targeting ligand to integrin alpha(v)beta(3) receptor. Emission of the AIE probe is switched on upon its specific binding to integrin alpha(v)beta(3), which allows quantitative detection of integrin alpha(v)beta(3) in solution and real-time imaging of the binding process between cRGD and integrin alpha(v)beta(3) on cell membrane. The probe can be used for tracking integrin alpha(v)beta(3) and for identifying integrin alpha(v)beta(3)-positive cancer cells.