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肽类正电子发射断层显像(PET)成像:近期进展综述及放射性金属标记肽类在医学领域的未来展望

Peptide PET Imaging: A Review of Recent Developments and a Look at the Future of Radiometal-Labeled Peptides in Medicine.

作者信息

Shabsigh Majed, Solomon Lee A

机构信息

Department of Chemistry and Biochemistry, George Mason University, Fairfax, Virginia 22030, United States.

出版信息

Chem Biomed Imaging. 2024 Aug 23;2(9):615-630. doi: 10.1021/cbmi.4c00030. eCollection 2024 Sep 23.

Abstract

The development of peptide-based, radiometal-labeled PET imaging agents has seen an increase in attention due to the favorable properties the peptide backbone exhibits. These include high selectivity and affinity to proteins and cells directly linked to various types of cancers. In addition, rapid clearance from circulation and low toxicity allow for unique approaches to engineering a viable peptide-based imaging agent. Utilizing peptides as the backbone allows for various modifications to improve metabolic stability, target cell affinity, and image quality and imaging capabilities and reduce toxicity. Select radiolabeled peptides have already been FDA approved, with many more in late-stage trials. This review summarizes the current state of the radiometal-labeled PET peptide imaging field as well as explores methods used by researchers to modify peptides, concluding with a look at the future of peptide-based therapy and diagnostics.

摘要

基于肽的放射性金属标记正电子发射断层扫描(PET)成像剂的开发受到了越来越多的关注,因为肽主链具有良好的特性。这些特性包括对与各类癌症直接相关的蛋白质和细胞具有高选择性和亲和力。此外,从循环系统中快速清除以及低毒性使得开发可行的基于肽的成像剂有了独特的方法。利用肽作为主链可以进行各种修饰,以提高代谢稳定性、靶细胞亲和力、图像质量和成像能力,并降低毒性。一些放射性标记的肽已经获得了美国食品药品监督管理局(FDA)的批准,还有更多的肽正处于后期试验阶段。这篇综述总结了放射性金属标记PET肽成像领域的现状,并探讨了研究人员用于修饰肽的方法,最后展望了基于肽的治疗和诊断的未来。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c891/11503725/1ae3ae066dec/im4c00030_0001.jpg

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