结构多样化的F-标记d-TCO衍生物的表征作为生物直角预定向成像的PET探针
Karuna Adhikari1, Jonatan Dewulf2, Christel Vangestel3,2
1Laboratory of Medicinal Chemistry, University of Antwerp, Antwerp 2610, Belgium.
ACS omega
|October 23, 2023
概括
研究人员开发了新型-18标记的cis-dioxolane-fused trans-cyclooctene (d-TCO) 衍生物,用于瘤学中预定向正子发射断层扫描 (PET) 成像. 这些新型的放射标志物显示出通过生物对角结合来改善瘤可视化的前景.
科学领域:
- 放射化学和核医学 放射化学和核医学
- 生物对角化学 生物对角化学
- 瘤成像学成像学
背景情况:
- 使用反向电子需求的预定向成像Diels-Alder (IEDDA) 循环加法在跨循环 octene (TCO) 和四 (Tz) 之间是瘤学中不断增长的策略.
- 目前的方法主要使用放射性标记的四,放射性标记的TCOs的可用性有限.
- 扩大基于TCO的放射追踪器的工具箱对于推进预定向成像和治疗至关重要.
研究的目的:
- 开发新的,结构多样化的18F标记的cis-dioxolane-fused TCO (d-TCO) 衍生品.
- 评估这些d-TCOs在体内生物对角联结和正子发射断层扫描 (PET) 预定向成像方面的潜力.
- 扩大用于预定向瘤学应用的可用放射性标记TCO选项.
主要方法:
- 一系列d-TCO衍生物的合成和反应性测试对四素.
- 基于光的预定向阻断研究的开发,用于在没有先前放射化学开发的情况下进行体内结合评估.
- 开发和评估两种新的18F标记的d-TCO放射性追踪剂,包括在结直肠癌小鼠模型中的体外稳定性,药理动力学和体内PET成像.
主要成果:
- 所有合成的d-TCO衍生物都表现出与四素的快速反应动力学.
- 两种d-TCO化合物表现出优异的体内结合,具有高阻断效率 (95%和97%).
- 标有18F标记的追踪剂[18F]MICA-214显示出有利的药理动力学,并使小鼠能够进行特定的瘤可视化,与对照组相比,预定向组的瘤吸收率显著更高.
结论:
- 成功合成了一系列多样化的快速反应的化d-TCOs.
- 开发的18F标记d-TCO追踪器 ([18F]MICA-214) 显示了在结直肠癌模型中预定向PET成像的潜力.
- 为了提高瘤与背景的比率,需要进一步优化,但以18F标记的d-TCO在预定向策略的水友性和快速生物结合方面具有优势.
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