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VyPAL2酸阿斯巴拉基尼尔结合酶可实现多功能工作流程,用于基于单域抗体的放射性标记

Sofie Declercq¹, Wei Min Chen², Abbas El Sahili²

¹Molecular Imaging and Therapy MITH Research Group, Vrije Universiteit Brussel VUB, Laarbeeklaan 103, 1090 Jette, Belgium.

Journal of controlled release : official journal of the Controlled Release Society

|November 1, 2025

概括

VyPAL2酶能够快速地对单域抗体 (sdAbs) 进行特定部位的放射标记,用于先进的核成像. 这种高效的酶策略通过减少脏保留和增强瘤向来改善放射性药物开发.

科学领域:

生物结合化学生物结合化学
放射性药物开发放射性药物开发
分子成像学分子成像学

背景情况:

越来越多的人对精确的以蛋白质为基础的治疗药物的需求.
需要针对抗体制定高效的,特定于某个部位的结合策略.
放射性药物应用中常规合方法的局限性.

研究的目的:

评估VyPAL2,一种快速联酶,用于单域抗体 (sdAbs) 的特定位点放射标记.
开发用于核成像和治疗的sdAbs功能化的快速酶策略.
为了比较酵素修饰的追踪剂与常规合物的体内性能.

主要方法:

使用VyPAL2和人类谷氨基基环酶 (hQPCT) 进行两种不同的结合策略:"准备和配对"和"融合和使用".
设计了一种具有C端NQL标签的抗hPDL1sdaB,用于酶修饰.
执行了用于点击放射化的甲基四手柄和用于加-68标签的NOTA化剂的特定位点绑定.

主要成果:

这两种策略都在25°C以高纯度 (>99%) 和回收 (55-65%) 的情况下,在15分钟内产生了功能化的sdAbs.
放射性标记的sdAbs显示出高放射性化学纯度 (>95%),优异的摩尔活性 (高达37 GBq/μmol),并保持了目标亲和力 (KD 3-4 nM).
在体内研究表明,hPDL1阳性瘤的脏保留和特异性积累显著减少,实现高瘤与背景比率.

结论:

VyPAL2介导的结为sdAb功能化提供了一种快速,强大和特定站点的方法.
这种酶方法促进了下一代基于蛋白质的放射性药物的开发,这些放射性药物具有改进的药物动力学特征.
该战略对推动核成像和有针对性的治疗应用具有重大前景.

关键词:

酶性结合酶化结合.免疫-PET成像成像技术类亚斯巴拉基尼尔连酶 (VyPAL2)精准医学是一门精准的医学.放射性药物放射性药物放射性药物单域抗体是一种单域抗体.特定地点的生物结合.热门节目热门节目热门节目

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