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基于位点特异性π钳介导的镓和氟正电子发射断层显像（PET）放射性药物的放射性合成

Site-specific π-clamp-mediated radiosynthesis of Ga and F PET radiopharmaceuticals.

作者信息

Yue Thomas T C, Teh Jin Hui, Aboagye Eric, Ma Michelle T, Pham Truc T, Long Nicholas J

机构信息

Department of Chemistry, Molecular Sciences Research Hub, Imperial College London, White City Campus, Wood Lane, London W120BZ, UK.

School of Biomedical Engineering and Imaging Sciences, King's College London, 4th Floor Lambeth Wing, St. Thomas' Hospital, London SE17EH, UK.

出版信息

Chem Commun (Camb). 2025 Jan 7;61(4):732-735. doi: 10.1039/d4cc05223d.

DOI:10.1039/d4cc05223d
PMID:39661407
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11633826/
Abstract

The π-clamp-mediated conjugation method, which enables site-specific modification of cysteine residues, is a promising strategy for developing well-defined radiolabelled biomolecules for positron emission tomography (PET) imaging. We have applied this method to site-specifically attach the macrocyclic chelators "NODA" and "NODAGA" to the somatostatin receptor 2-targeted peptide, octreotate. The resulting novel NODA-octreotate and NODAGA-octreotate compounds can be radiolabelled with either [F]AlF or [Ga]Ga respectively. PET imaging shows that the [Ga]Ga-labelled derivative exhibits high stability and favourable pharmacokinetic properties.

摘要

π-钳介导的偶联方法能够实现半胱氨酸残基的位点特异性修饰，是开发用于正电子发射断层扫描（PET）成像的明确放射性标记生物分子的一种有前景的策略。我们已将此方法应用于将大环螯合剂“NODA”和“NODAGA”位点特异性连接到靶向生长抑素受体2的肽奥曲肽上。所得的新型NODA-奥曲肽和NODAGA-奥曲肽化合物可分别用[F]AlF或[Ga]Ga进行放射性标记。PET成像显示，[Ga]Ga标记的衍生物具有高稳定性和良好的药代动力学性质。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/9be705f64147/d4cc05223d-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/69f04cf2f9c1/d4cc05223d-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/79345d3ea25c/d4cc05223d-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/9be705f64147/d4cc05223d-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/69f04cf2f9c1/d4cc05223d-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/79345d3ea25c/d4cc05223d-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ebe/11633826/9be705f64147/d4cc05223d-f2.jpg

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