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在中枢神经系统内预定目标成像中对四氨酸标记物的评估

Martin R Edelmann^1,2, Christoph Bredack³, Sara Belli⁴

¹Roche Pharma Research and Early Development, Roche Innovation Center Basel, Therapeutic Modalities, Small Molecule Research, Isotope Synthesis, F. Hoffmann-La Roche Ltd, Basel CH-4070, Switzerland.

Bioconjugate chemistry

|September 15, 2023

概括

使用生物对等点击化学的预定向策略通过分离抗体和放射性同位素半衰期来改善成像. 这项研究开发了用于18F-PET成像和3H放射性连接体的新型四素,其中一个显示有希望的中枢神经系统透.

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.
有机合成有机合成

背景情况:

预定目标策略将抗体和放射性同位素的半衰期分开,以减少辐射负担.
生物直角点击化学,特别是四素 (Tz) 和跨环子素 (TCO) 反应,可以实现精确的准.
这种方法对于成像分子标志物至关重要,仅小分子无法访问它们.

研究的目的:

合成和描述新型四衍生物作为成像剂.
评估它们在使用-18 (18F) 或 (3H) 进行放射性标记方面的潜力.
为了确定中枢神经系统 (CNS) 位子发射断层扫描 (PET) 成像的候选人.

主要方法:

11个冷Tz成像剂候选物的合成和表征.
评估pH依赖的化学稳定性 (pH6.5-8).
在体外测定被动透性,微体稳定性和P-糖蛋白传输.
针对系统清除和中枢神经系统透的小鼠的药理学研究.
用18F和3H进行放射性标记.
在小鼠中的生物分布研究.

主要成果:

两种氨酸被成功标记为18F.
一种标有18F标签的四氨酸在小鼠中证明了大脑透.
一个Tz被成功标记为三,并显示了与TCO修饰的抗体具有生物对等点击反应.
选择的Tzs在生理学pH范围内表现出稳定性和良好的体外特性.

结论:

确定了一种新型的四素作为一种潜在的18F标记的中枢神经系统-PET成像剂.
确定了第二个四素作为3H-放射性联体,用于与修饰抗体的生物对等反应.
这些发现推进了用于增强分子成像的预定向策略,特别是在中枢神经系统应用中.

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