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I-124标记小分子探针的合成和构造,用于CAIX表达的非侵入性PET成像

Xianteng Yang¹, Chengxue He², Feng Wang²

¹Department of Orthopedics, Guizhou Provincial People's Hospital, Guiyang, 550002, China.

Molecular imaging and biology

|April 9, 2025

概括

这项研究介绍了I-XYIMSR-01,一种新的分子探针,用于在缺氧瘤中成像碳酸无水酶IX (CAIX). 该探针表现出极好的准和保留,使得有效的长期监测瘤缺氧.

科学领域:

生物医学成像学生物医学成像学
放射化学放射化学是指辐射化学.
在瘤学瘤学.

背景情况:

碳酸无水酶IX (CAIX) 在缺氧瘤中高度表达,促进癌症的进展.
准CAIX是癌症诊断和治疗的一个有希望的策略.

研究的目的:

通过使用PET成像来评估CAIX过度表达瘤中[124I]I-XYIMSR-01的诊断能力和保留.
评估探针在可视化瘤缺氧方面的特异性和有效性.

主要方法:

使用同位素对[^124/125I]I-XYIMSR-01进行放射性标记.
在体外细胞吸收研究以评估CAIX向特异性.
在CAIX表达模型中的体内PET成像和生物分布研究.
免疫组织化学 (IHC) 和HE染色与CAIX表达和缺氧的相关性.

主要成果:

[¹²⁴I]I-XYIMSR-01表现出高的特定活性,纯度和稳定性.
在高CAIX表达细胞 (HT-29) 与低CAIX表达细胞 (HCT116) 相比,CAIX表达细胞的吸收显著更高.
在HT29模型中成功进行体内PET成像,具有高达48小时的清晰分子图像.
良好的瘤-背景信号-噪声比,使消化道瘤的延迟成像成为可能.

结论:

[124 I]I-XYIMSR-01是CAIX的高度特定和有效的分子探针.
该探头可促进低氧瘤的长期动态监测和成像.
它具有作为评估瘤缺氧的诊断工具的潜力.

关键词:

碳酸无水酶IX的使用方法人类结肠癌是人类结肠癌.定子发射断层扫描成像成像 [124/125I]I-XYIMSR- 01 的时间.

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