A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging

Jingming Zhang, Anastasia Rakhimbekova, Xiaojiang Duan, Qingqing Yin, Catherine A. Foss, Yan Fan, Yangyang Xu, Xuesong Li, Xuekang Cai, Zsofia Kutil, Pengyuan Wang, Zhi Yang, Ning Zhang, Martin G. Pomper, Yiguang Wang (), Cyril Bařinka () and Xing Yang ()
Additional contact information
Jingming Zhang: Peking University First Hospital
Anastasia Rakhimbekova: Institute of Biotechnology of the Czech Academy of Sciences, BIOCEV
Xiaojiang Duan: Peking University First Hospital
Qingqing Yin: Peking University
Catherine A. Foss: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine
Yan Fan: Peking University First Hospital
Yangyang Xu: Peking University First Hospital
Xuesong Li: Peking University First Hospital
Xuekang Cai: Peking University First Hospital
Zsofia Kutil: Institute of Biotechnology of the Czech Academy of Sciences, BIOCEV
Pengyuan Wang: Peking University First Hospital
Zhi Yang: Peking University Cancer Hospital & Institute
Ning Zhang: Peking University First Hospital
Martin G. Pomper: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine
Yiguang Wang: Peking University
Cyril Bařinka: Institute of Biotechnology of the Czech Academy of Sciences, BIOCEV
Xing Yang: Peking University First Hospital

Nature Communications, 2021, vol. 12, issue 1, 1-11

Abstract: 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.

Date: 2021
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DOI: 10.1038/s41467-021-25746-6

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