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European Journal of Nuclear Medicine and Molecular Imaging
Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging 8/2022

02.03.2022 | Original Article

A self-triggered radioligand therapy agent for fluorescence imaging of the treatment response in prostate cancer

verfasst von: Hongchuang Xu, Yanpu Wang, Jingming Zhang, Xiaojiang Duan, Ting Zhang, Xuekang Cai, Hyunsoo Ha, Youngjoo Byun, Yan Fan, Zhi Yang, Yiguang Wang, Zhaofei Liu, Xing Yang

Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging | Ausgabe 8/2022

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Abstract

Purpose

Radioligand therapy (RLT) targeting prostate-specific membrane antigen (PSMA) is emerging as an effective treatment option for metastatic castration-resistant prostate cancer (mCRPC). An imaging-based method to quantify early treatment responses can help to understand and optimize RLT.

Methods

We developed a self-triggered probe 2 targeting the colocalization of PSMA and caspase-3 for fluorescence imaging of RLT-induced apoptosis.

Results

The probe binds to PSMA potently with a Ki of 4.12 nM, and its fluorescence can be effectively switched on by caspase-3 with a Km of 67.62 μM. Cellular and in vivo studies demonstrated its specificity for imaging radiation-induced caspase-3 upregulation in prostate cancer. To identify the detection limit of our method, we showed that probe 2 could achieve 1.79 times fluorescence enhancement in response to 177Lu-RLT in a medium PSMA-expressing 22Rv1 xenograft model.

Conclusion

Probe 2 can potently bind to PSMA, and the fluorescence signal can be sensitively switched on by caspase-3 both in vitro and in vivo. This method may provide an effective tool to investigate and optimize PSMA-RLT.
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Metadaten
Titel
A self-triggered radioligand therapy agent for fluorescence imaging of the treatment response in prostate cancer
verfasst von
Hongchuang Xu
Yanpu Wang
Jingming Zhang
Xiaojiang Duan
Ting Zhang
Xuekang Cai
Hyunsoo Ha
Youngjoo Byun
Yan Fan
Zhi Yang
Yiguang Wang
Zhaofei Liu
Xing Yang
Publikationsdatum
02.03.2022
Verlag
Springer Berlin Heidelberg
Erschienen in
European Journal of Nuclear Medicine and Molecular Imaging / Ausgabe 8/2022
Print ISSN: 1619-7070
Elektronische ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-022-05743-7

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