Integrin-targeted trifunctional probe for cancer cells: a "seeing and counting" approach.

We report the design and synthesis of a trifunctional probe for seeing and counting cancer cells using both fluorescence imaging (FI) and inductively coupled plasma mass spectrometry (ICPMS) for the first time. It consisted of a guiding cyclic RGD peptide unit to catch cancer cells via targeting the α(v)β(3) integrin overexpressed on their surface, a 5-amino-fluorescein moiety for FI using confocal laser scanning microscopy (CLSM) as well as a 2-aminoethyl-monoamide-DOTA group for loading stable europium ion and subsequent ICPMS quantification of the cancer cells without the use of radioactive isotopes. In addition to FI, the LOD (3σ) of the α(v)β(3) integrin was down to 69.2-309.4 amol per cell depending on the type of the α(v)β(3)-positive cancer cells when using ICPMS and those of the cancer cell number reached 17-75. This probe developed enables us not only to see but also to count the α(v)β(3)-positive cancer cells ultrasensitively, paving a new way for early diagnosis of cancer.