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在瘤中用于成像A2AR的先基放射追踪剂的开发
Xueyuan Zeng1, Hongwu Liu1, Guolong Huang1
1State Key Laboratory of Vaccines for Infectious Diseases, Center for Molecular Imaging and Translational Medicine, Xiang An Biomedicine Laboratory, School of Public Health, Xiamen University, Xiamen 361102, China.
Journal of medicinal chemistry
|July 22, 2024
概括
研究人员开发了新的放射性标记物[18F]F-PFP2和[18F]F-PFP4,以可视化瘤中的腺素2A受体 (A2A R). 这些探测器通过成像A2A R表达来指导个性化癌症治疗.
科学领域:
- 放射化学 放射化学是指辐射化学.
- 分子成像学分子成像学
- 在瘤学瘤学.
背景情况:
- 腺二甲受体 (A2A R) 的激活有助于瘤免疫抑制,对免疫治疗结果产生负面影响.
- 有效的A2A R可视化对于预测和改善免疫治疗反应至关重要.
研究的目的:
- 设计和评估新的-18 (18F) 标记探针,用于瘤中A2A R的非侵入性成像.
- 评估这些探针在临床前瘤模型中的诊断潜力.
主要方法:
- 两种新的18F标记探针的合成和特征:[18F]F-PFP2和[18F]F-PFP4.
- 在A2A R阳性 (B16F10黑色素瘤) 和A2A R阴性 (4T1乳腺瘤) 模型中放射性追踪剂吸收的体内评估.
- 在B16F10肺转移模型中评估探针性能.
主要成果:
- 无论是[18F]F-PFP2还是[18F]F-PFP4,在A2A R阳性B16F10瘤中,与A2A R阴性4T1瘤相比,都显示出更高的吸收率.
- [18F]F-PFP2在转移性肺病变中相比正常肺组织 (瘤/肺比率~3) 显示出明显更高的积累.
- 随着时间的推移,在A2A R阳性瘤中,这两种探针的吸收率都增加了.
结论:
- 新的18F标记探针,特别是[18F]F-PFP2,可以有效地可视化瘤中的A2A R表达.
- [18F]F-PFP2有可能开发用于瘤的A2A R向成像系统.
- 这种成像系统可以为个性化癌症治疗,特别是免疫治疗提供关键指导.
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