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利用多聚环 RGD 肽类似物的 PET 诊断分子成像整合素 αβ 受体。

PET Diagnostic Molecules Utilizing Multimeric Cyclic RGD Peptide Analogs for Imaging Integrin αβ Receptors.

机构信息

Radiochemical Studies Laboratory, Institute of Nuclear & Radiological Sciences & Technology, Energy & Safety, National Centre for Scientific Research "Demokritos", Ag. Paraskevi Attikis, 15310 Athens, Greece.

Laboratory of Medicinal Chemistry, Department of Pharmacy, Section of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupolis-Zografou, 15771 Athens, Greece.

出版信息

Molecules. 2021 Mar 22;26(6):1792. doi: 10.3390/molecules26061792.

DOI:10.3390/molecules26061792
PMID:33810198
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8005094/
Abstract

Multimeric ligands consisting of multiple pharmacophores connected to a single backbone have been widely investigated for diagnostic and therapeutic applications. In this review, we summarize recent developments regarding multimeric radioligands targeting integrin αβ receptors on cancer cells for molecular imaging and diagnostic applications using positron emission tomography (PET). Integrin αβ receptors are glycoproteins expressed on the cell surface, which have a significant role in tumor angiogenesis. They act as receptors for several extracellular matrix proteins exposing the tripeptide sequence arginine-glycine-aspartic (RGD). Cyclic RDG peptidic ligands c(RGD) have been developed for integrin αβ tumor-targeting positron emission tomography (PET) diagnosis. Several c(RGD) pharmacophores, connected with the linker and conjugated to a chelator or precursor for radiolabeling with different PET radionuclides (F, Cu, and Ga), have resulted in multimeric ligands superior to c(RGD) monomers. The binding avidity, pharmacodynamic, and PET imaging properties of these multimeric c(RGD) radioligands, in relation to their structural characteristics are analyzed and discussed. Furthermore, specific examples from preclinical studies and clinical investigations are included.

摘要

多聚配体由连接在单个骨架上的多个药效团组成，已广泛用于诊断和治疗应用。在这篇综述中，我们总结了最近在使用正电子发射断层扫描（PET）针对癌细胞上的整合素 αβ 受体进行分子成像和诊断应用的多聚放射性配体的研究进展。整合素 αβ 受体是细胞表面表达的糖蛋白，在肿瘤血管生成中具有重要作用。它们作为几种细胞外基质蛋白的受体发挥作用，暴露出三肽序列精氨酸-甘氨酸-天冬氨酸（RGD）。已开发出环状 RGD 肽类配体 c（RGD）用于整合素 αβ 肿瘤靶向正电子发射断层扫描（PET）诊断。几种 c（RGD）药效团与接头连接，并与螯合剂或放射性标记前体缀合，用于不同的 PET 放射性核素（F、Cu 和 Ga）的放射性标记，从而产生比 c（RGD）单体更优越的多聚配体。分析和讨论了这些多聚 c（RGD）放射性配体与结构特征相关的结合亲和力、药效学和 PET 成像特性。此外，还包括临床前研究和临床研究中的具体实例。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7019/8005094/7c058ec44b25/molecules-26-01792-g013.jpg
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