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Development of Preladenant-Based Radiotracers for Imaging A2AR in Tumors
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-07-22 , DOI: 10.1021/acs.jmedchem.4c01015 Xueyuan Zeng 1 , Hongwu Liu 1 , Guolong Huang 1 , Yanjie Wang 1 , Wuhao Zhou 1 , Yike Wang 1 , Xuedong Chen 1 , Xingxing Cheng 1 , Rongqiang Zhuang 1 , Jindian Li 2 , Jianyang Fang 1 , Lumei Huang 1 , Xianzhong Zhang 3 , Zhide Guo 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-07-22 , DOI: 10.1021/acs.jmedchem.4c01015 Xueyuan Zeng 1 , Hongwu Liu 1 , Guolong Huang 1 , Yanjie Wang 1 , Wuhao Zhou 1 , Yike Wang 1 , Xuedong Chen 1 , Xingxing Cheng 1 , Rongqiang Zhuang 1 , Jindian Li 2 , Jianyang Fang 1 , Lumei Huang 1 , Xianzhong Zhang 3 , Zhide Guo 1
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Activation of the adenosine 2A receptor (A2AR) can lead to tumor immunosuppression, which results in poor prognosis of immunotherapy. The aim of this study was to design novel 18F-labeled probes ([18F]F-PFP2 and [18F]F-PFP4) to visualize A2AR in the tumor. The uptake of radioprobes in A2AR-negative 4T1 breast tumor was lower than that of A2AR-positive B16F10 melanoma at 1 h p.i. (1.22 ± 0.36% ID/g vs 2.80 ± 0.72% ID/g), 2 h p.i. (1.09 ± 0.20% ID/g vs 2.93 ± 0.76% ID/g) and 3 h p.i. (0.89 ± 0.27% ID/g vs 2.73 ± 0.58% ID/g), respectively. B16F10 lung metastasis models were employed to expand the application scenarios, observing significantly higher uptake of [18F]F-PFP2 in metastatic lesions compared to normal lung tissue (5.55 ± 2.18% ID/g vs 1.89 ± 0.65% ID/g, tumor/lung ratio ∼3). It is given that [18F]F-PFP2 might lay the foundation for establishing an A2AR-targeted imaging evaluation system for tumors, which will provide more precise guidance for personalized treatment.
中文翻译：
基于 Preladenant 的放射性示踪剂的开发，用于肿瘤中 A2AR 成像
腺苷2A受体（A 2A R）的激活可导致肿瘤免疫抑制，从而导致免疫治疗预后不良。本研究的目的是设计新型18 F 标记探针（[ 18 F]F-PFP 2和 [ 18 F]F-PFP 4 ）以可视化肿瘤中的 A 2A R。注射后 1 小时，A 2A R 阴性 4T1 乳腺肿瘤中放射性探针的摄取低于 A 2A R 阳性 B16F10 黑色素瘤（注射后 1 小时为 1.22 ± 0.36% ID/g vs 2.80 ± 0.72% ID/g），注射后 2 小时(1.09 ± 0.20% ID/g vs 2.93 ± 0.76% ID/g) 和 3 h pi (0.89 ± 0.27% ID/g vs 2.73 ± 0.58% ID/g)。采用B16F10肺转移模型扩大了应用场景，观察到转移病灶中[ 18 F]F-PFP 2的摄取明显高于正常肺组织（5.55 ± 2.18% ID/g vs 1.89 ± 0.65% ID/g，肿瘤/肺比率∼3)。认为[ 18 F]F-PFP 2可能为建立A 2A R靶向肿瘤影像评估体系奠定基础，为个体化治疗提供更精准的指导。
更新日期：2024-07-22
中文翻译：
基于 Preladenant 的放射性示踪剂的开发，用于肿瘤中 A2AR 成像
腺苷2A受体（A 2A R）的激活可导致肿瘤免疫抑制，从而导致免疫治疗预后不良。本研究的目的是设计新型18 F 标记探针（[ 18 F]F-PFP 2和 [ 18 F]F-PFP 4 ）以可视化肿瘤中的 A 2A R。注射后 1 小时，A 2A R 阴性 4T1 乳腺肿瘤中放射性探针的摄取低于 A 2A R 阳性 B16F10 黑色素瘤（注射后 1 小时为 1.22 ± 0.36% ID/g vs 2.80 ± 0.72% ID/g），注射后 2 小时(1.09 ± 0.20% ID/g vs 2.93 ± 0.76% ID/g) 和 3 h pi (0.89 ± 0.27% ID/g vs 2.73 ± 0.58% ID/g)。采用B16F10肺转移模型扩大了应用场景，观察到转移病灶中[ 18 F]F-PFP 2的摄取明显高于正常肺组织（5.55 ± 2.18% ID/g vs 1.89 ± 0.65% ID/g，肿瘤/肺比率∼3)。认为[ 18 F]F-PFP 2可能为建立A 2A R靶向肿瘤影像评估体系奠定基础，为个体化治疗提供更精准的指导。
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