Abstract
Surgery is an efficient way to treat localized prostate cancer (PCa), however, it is challenging to demarcate rapidly and accurately the tumor boundary intraoperatively, as existing tumor detection methods are seldom performed in real-time. To overcome those limitations, we develop a fluorescent molecular rotor that specifically targets the prostate-specific membrane antigen (PSMA), an established marker for PCa. The probes have picomolar affinity (IC50 = 63-118 pM) for PSMA and generate virtually instantaneous onset of robust fluorescent signal proportional to the concentration of the PSMA-probe complex. In vitro and ex vivo experiments using PCa cell lines and clinical samples, respectively, indicate the utility of the probe for biomedical applications, including real-time monitoring of endocytosis and tumor staging. Experiments performed in a PCa xenograft model reveal suitability of the probe for imaging applications in vivo.
Highlights
Surgery is an efficient way to treat localized prostate cancer (PCa), it is challenging to demarcate rapidly and accurately the tumor boundary intraoperatively, as existing tumor detection methods are seldom performed in real-time
These have been successfully modified by YenPang Hsu et al and Fluorescent molecular rotors (FMRs) with wavelengths closer to the nearinfrared region have been generated
We aimed at the design of activatable probes by linking a benzonitrile fluorescent rotor to the Lys-Urea-Glu scaffold, a wellestablished prostate-specific membrane antigen (PSMA)-targeting moiety used clinically for PCa imaging and radiotherapy[39]
Summary
Surgery is an efficient way to treat localized prostate cancer (PCa), it is challenging to demarcate rapidly and accurately the tumor boundary intraoperatively, as existing tumor detection methods are seldom performed in real-time. The fluorescence response of FMRs is more sensitive and faster compared with other on-off probes mediated by specific chemical reactions[22], enabling real-time and in situ detection In this regard, some FMRs have been developed for sensing viscosity in the microenvironment, such as derivatives of julolidine (DCVJ, CCVJ)[23,24], meso-phenyl-substituted derivatives of BODIPY25–27, porphyrin derivatives[28], and merocyanine dyes[29]. We reveal the underlying mechanism of the fluorescent activation upon probePSMA binding These probes are successfully applied to real-time monitoring of PSMA-mediated endocytosis, rapid prostate cancer tissue staining, and in vivo imaging of PCa
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