Sc-HOPO：一种用于基于放射性锝的放射性药物的潜在构建体。
Sc-HOPO: A Potential Construct for Use in Radioscandium-Based Radiopharmaceuticals.
机构信息
Ph.D. Program in Chemistry, The Graduate Center of the City University of New York, New York, New York10016, United States.
Department of Chemistry, City University of New York Hunter College, 695 Park Avenue, New York, New York10065, United States.
出版信息
Inorg Chem. 2023 Dec 18;62(50):20567-20581. doi: 10.1021/acs.inorgchem.2c03931. Epub 2023 Feb 1.
Abstract
Three isotopes of scandium─Sc, Sc, and Sc─have attracted increasing attention as potential candidates for use in imaging and therapy, respectively, as well as for possible theranostic use as an elementally matched pair. Here, we present the octadentate chelator 3,4,3-(LI-1,2-HOPO) (or HOPO), an effective chelator for hard cations, as a potential ligand for use in radioscandium constructs with simple radiolabeling under mild conditions. HOPO forms a 1:1 Sc-HOPO complex that was fully characterized, both experimentally and theoretically. [Sc]Sc-HOPO exhibited good stability in chemical and biological challenges over 7 days. In healthy mice, [Sc]Sc-HOPO cleared the body rapidly with no signs of demetalation. HOPO is a strong candidate for use in radioscandium-based radiopharmaceuticals.
摘要
三种钪同位素——Sc、Sc 和 Sc——分别作为成像和治疗的潜在候选物，以及作为一种元素匹配对的潜在治疗诊断用途，引起了越来越多的关注。在这里，我们介绍了一种八齿配体 3,4,3-(LI-1,2-HOPO)（或 HOPO），它是一种有效的硬阳离子螯合剂，作为一种有潜力的配体，可用于在温和条件下进行简单放射性标记的放射性钪构建。HOPO 形成了 1:1 的 Sc-HOPO 配合物，通过实验和理论进行了充分的表征。[Sc]Sc-HOPO 在化学和生物学挑战下的 7 天内表现出良好的稳定性。在健康小鼠中，[Sc]Sc-HOPO 迅速清除体内，没有脱金属迹象。HOPO 是用于放射性钪放射性药物的有力候选物。
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