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基于型异构体的辐射追踪器准纤维细胞激活蛋白和整体蛋白α_vβ₃

Kehuang Liu¹, Tao Jiang¹, Wanqian Rao¹

¹Department of Nuclear Medicine, Xiangya Hospital, Central South University, No. 87 Xiangya Road, Changsha City, 410008, Hunan Province, China.

European journal of nuclear medicine and molecular imaging

|January 26, 2024

概括

一种新型的异构体放射追踪剂,68Ga-FAP-RGD,通过向纤维细胞激活蛋白 (FAP) 和整体蛋白αvβ3.3,证明了优异的瘤吸收和保留. 这种双重准的方法显示了改善癌症成像和治疗的前景.

科学领域:

放射性药物化学放射性药物化学
分子成像学分子成像学
癌症治疗治疗癌症治疗

背景情况:

由于多价值性,异构体比单体具有优势,增强瘤向.
纤维细胞激活蛋白 (FAP) 和整合素αvβ3在瘤微环境中过度表达.

研究的目的:

设计和开发一种针对FAP和整蛋白αvβ3.3的新型基异构体.
通过协同的双重准方法来增强瘤的吸收和保留.

主要方法:

从FAP-2286和c ((RGDfK) 中合成FAP-RGD).
使用细胞吸收和竞争性测试对双受体结合的评估.
使用微PET/CT的临床前药理动力学和生物分布研究.
对177Lu-FAP-RGD的抗瘤疗效的评估.
在志愿者和患者中对68Ga-FAP-RGD的临床评估.

主要成果:

68Ga-FAP-RGD对FAP和整体蛋白αvβ3.3都显示出高的结合亲和力.
与单体对应物相比,增强了瘤的吸收和保留.
177Lu-FAP-RGD在体内有效抑制瘤生长.
在临床研究中有利的剂量测量和诊断性能.

结论:

双特异性放射追踪剂68Ga-FAP-RGD由于多价值效应,表现出优异的瘤吸收和保留.
临床前研究表明有利的图像对比度和治疗潜力.
正在进行的优化旨在增强FAP-RGD用于临床内放射治疗.

关键词:

纤维细胞激活蛋白质的激活蛋白质这是一种异构聚合物 (heterodimer).整体素 αvβ3 的含量多价值效应的影响.聚乙烯/聚乙烯/聚乙烯

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