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羟基吡啶酮作为一种极具前景的靶向诊断和治疗放射性药物平台。

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals.

机构信息

HTA Co., Ltd., Beijing 102413, China.

China Isotope & Radiation Corporation, Beijing 100089, China.

出版信息

Molecules. 2021 Nov 19;26(22):6997. doi: 10.3390/molecules26226997.

DOI:10.3390/molecules26226997
PMID:34834087
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8619595/
Abstract

Hydroxypyridinones (HOPOs) have been used in the chelation therapy of iron and actinide metals. Their application in metal-based radiopharmaceuticals has also been increasing in recent years. This review article focuses on how multidentate HOPOs can be used in targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals. The general structure of radiometal-based targeted radiopharmaceuticals, a brief description of siderophores, the basic structure and properties of bidentate HOPO, some representative HOPO multidentate chelating agents, radiopharmaceuticals based on HOPO multidentate bifunctional chelators for gallium-68, thorium-227 and zirconium-89, as well as the future prospects of HOPO multidentate bifunctional chelators in other metal-based radiopharmaceuticals are described and discussed in turn. The HOPO metal-based radiopharmaceuticals that have shown good prospects in clinical and preclinical studies are gallium-68, thorium-227 and zirconium-89 radiopharmaceuticals. We expect HOPO multidentate bifunctional chelators to be a very promising platform for building novel targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals.

摘要

羟基吡啶酮（HOPO）已被用于铁和锕系金属的螯合疗法。近年来，其在基于金属的放射性药物中的应用也在不断增加。本文综述了多齿 HOPO 如何用于靶向放射性金属的诊断和治疗放射性药物。重点介绍了基于放射性金属的靶向放射性药物的一般结构、铁载体的简要描述、双齿 HOPO 的基本结构和性质、一些代表性的 HOPO 多齿螯合剂、基于 HOPO 多齿双功能螯合剂的镓-68、钍-227 和锆-89 放射性药物，以及 HOPO 多齿双功能螯合剂在其他基于金属的放射性药物中的未来前景。在临床前研究中显示出良好前景的基于 HOPO 的金属放射性药物有镓-68、钍-227 和锆-89 放射性药物。我们预计 HOPO 多齿双功能螯合剂将成为构建新型靶向放射性金属诊断和治疗放射性药物的极具前景的平台。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/1f83c89abd26/molecules-26-06997-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/69cb1bca9c16/molecules-26-06997-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/9fc3d9b0d8b2/molecules-26-06997-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/de7925976313/molecules-26-06997-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/43676ded9f91/molecules-26-06997-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/dc53e7682644/molecules-26-06997-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/b9d437eefac7/molecules-26-06997-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/87c73a3c5730/molecules-26-06997-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/82aefa93067c/molecules-26-06997-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/744444021f09/molecules-26-06997-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/1f83c89abd26/molecules-26-06997-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/69cb1bca9c16/molecules-26-06997-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/ca70ffdf8f6f/molecules-26-06997-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/c6bd621bb061/molecules-26-06997-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/d96f9352864f/molecules-26-06997-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/9fc3d9b0d8b2/molecules-26-06997-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/de7925976313/molecules-26-06997-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/43676ded9f91/molecules-26-06997-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/dc53e7682644/molecules-26-06997-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/b9d437eefac7/molecules-26-06997-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/87c73a3c5730/molecules-26-06997-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/82aefa93067c/molecules-26-06997-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/744444021f09/molecules-26-06997-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bae4/8619595/1f83c89abd26/molecules-26-06997-g013.jpg

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3
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