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Novel PET Imaging Probe for Quantitative Detection of Senescence In Vivo
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-03-20 , DOI: 10.1021/acs.jmedchem.4c00179 Xin Xiang 1 , Chuning Dong 1 , Lianbo Zhou 1 , Jun Liu 2 , Zachary M Rabinowitz 2 , Yuzhao Zhang 2 , Honghui Guo 1 , Feng He 1 , Xingdou Chen 1 , Yunhua Wang 1 , Lina Cui 2 , Xiaowei Ma 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-03-20 , DOI: 10.1021/acs.jmedchem.4c00179 Xin Xiang 1 , Chuning Dong 1 , Lianbo Zhou 1 , Jun Liu 2 , Zachary M Rabinowitz 2 , Yuzhao Zhang 2 , Honghui Guo 1 , Feng He 1 , Xingdou Chen 1 , Yunhua Wang 1 , Lina Cui 2 , Xiaowei Ma 1
Affiliation
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Real-time detection of cellular senescence remains a clinical challenge. Here, we aimed to develop a positron emission tomography (PET) imaging probe targeting senescence-associated β-galactosidase (SA-β-Gal), the most widely used biomarker of cellular senescence, and investigate its performance for real-time in vivo quantitative detection of cellular senescence. A stable PET imaging agent [68Ga]Ga-BGal was obtained with a high labeling yield (90.0 ± 4.3%) and a radiochemical purity (>95%). [68Ga]Ga-BGal displayed high sensitivity and specificity for β-Gal both in vitro and in vivo. The reaction and uptake of the probe correlated with the β-Gal concentration and reaction time. In PET imaging, high β-Gal-expressing CT26.CL25 tumors and doxorubicin-treated HeLa tumors showed high signals from [68Ga]Ga-BGal, while a low signal was observed in CT26.WT and untreated HeLa tumors. In summary, we showcased successful PET imaging of senescence in preclinical models using probe [68Ga]Ga-BGal. This finding holds the potential for translating senescence imaging into clinical applications.
中文翻译：
用于体内衰老定量检测的新型 PET 成像探针
细胞衰老的实时检测仍然是临床挑战。在这里，我们的目标是开发一种针对衰老相关β-半乳糖苷酶（SA-β-Gal）（细胞衰老最广泛使用的生物标志物）的正电子发射断层扫描（PET）成像探针，并研究其实时体内定量的性能检测细胞衰老。获得了稳定的PET显像剂[ 68 Ga]Ga-BGal，具有高标记率（90.0±4.3%）和放射化学纯度（>95%）。 [ 68 Ga]Ga-BGal在体外和体内均表现出对 β-Gal 的高敏感性和特异性。探针的反应和摄取与β-Gal浓度和反应时间相关。在PET成像中，高β-Gal表达的CT26.CL25肿瘤和阿霉素治疗的HeLa肿瘤显示来自[ 68 Ga]Ga-BGal的高信号，而在CT26.WT和未治疗的HeLa肿瘤中观察到低信号。总之，我们展示了使用探针[ 68 Ga]Ga-BGal 在临床前模型中成功进行衰老 PET 成像。这一发现具有将衰老成像转化为临床应用的潜力。
更新日期：2024-03-20
中文翻译：
用于体内衰老定量检测的新型 PET 成像探针
细胞衰老的实时检测仍然是临床挑战。在这里，我们的目标是开发一种针对衰老相关β-半乳糖苷酶（SA-β-Gal）（细胞衰老最广泛使用的生物标志物）的正电子发射断层扫描（PET）成像探针，并研究其实时体内定量的性能检测细胞衰老。获得了稳定的PET显像剂[ 68 Ga]Ga-BGal，具有高标记率（90.0±4.3%）和放射化学纯度（>95%）。 [ 68 Ga]Ga-BGal在体外和体内均表现出对 β-Gal 的高敏感性和特异性。探针的反应和摄取与β-Gal浓度和反应时间相关。在PET成像中，高β-Gal表达的CT26.CL25肿瘤和阿霉素治疗的HeLa肿瘤显示来自[ 68 Ga]Ga-BGal的高信号，而在CT26.WT和未治疗的HeLa肿瘤中观察到低信号。总之，我们展示了使用探针[ 68 Ga]Ga-BGal 在临床前模型中成功进行衰老 PET 成像。这一发现具有将衰老成像转化为临床应用的潜力。
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