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Review Article

放射性标记的GRPR拮抗剂用于弥散性前列腺癌的成像-标记化学对靶向性质的影响

卷 27, 期 41, 2020

页: [7090 - 7111] 页: 22

弟呕挨: 10.2174/0929867327666200312114902

价格: $65

摘要

背景：胃泌素释放肽受体（GRPR）表达的放射性核素分子成像有望使无视的前列腺癌可视化，这是无与伦比的机会，由于体积小，邻近的良性组织或具有挑战性的位置，否则传统成像将无法检测到。为此目的，实现高成像对比度是必不可少的，用于前列腺癌分子成像的任何探针的分子设计应旨在获得尽可能高的肿瘤-器官比率。目的：这篇简短的综述总结了当前在前列腺癌中使用的主要成像方式，特别着重于放射性核素分子成像。重点主要放在放射性金属标记化学问题及其对放射性PRGR拮抗剂的靶向特性和生物分布的影响上，以对弥散性前列腺癌进行成像。 方法：对PubMed / MEDLINE和Scopus图书馆数据库进行全面的文献检索，以找到相关文章。 结果：放射性核素，螯合剂和所需的标记化学试剂的组合对稳定性，结合亲和力和内在化率，与正常组织和血液蛋白的脱靶相互作用，与酶的相互作用，活性吸收和排泄物的保留具有显着影响。放射性标记的轰击蛋白拮抗剂类似物在肿瘤中的器官和活性吸收。 结论：标记化学对基于GRPR靶向肽的成像探针的生物分布特征具有非常强的影响，在设计用于高对比度分子成像的靶向探针时需要考虑标记化学。考虑到体内相互作用的复杂性，目前尚无法准确预测最佳标记方法。因此，详细的体内表征和优化对于成像剂的合理设计至关重要。

关键词: 前列腺癌，分子成像，胃泌素释放肽受体，GRPR拮抗剂，放射性标记，放射性核素分子成像。

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