Fluorine‐18 labelled aldehydes as prosthetic groups for oxime coupling with a FVIIa protein,Journal of Labelled Compounds and Radiopharmaceuticals

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Fluorine‐18 labelled aldehydes as prosthetic groups for oxime coupling with a FVIIa protein
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2021-01-27 , DOI: 10.1002/jlcr.3900
Troels E Jeppesen _{1,

2} , Jesper B Kristensen ₃ , Carsten Behrens ₃ , Jacob Madsen _{1,

2} , Andreas Kjaer _{1,

2}

Affiliation

18 F-labelled aldehydes can be utilized for oxime coupling with chemically sensitive proteins, such as coagulation factor VII (FVII), if they are sufficiently reactive and can react in an aqueous solvent. New 18 F-labelled non-volatile aldehyde prosthetic groups derived from [18 F]F-Py-TFP and spirocyclic iodonium (III)ylide precursors for late stage 18 F-labelling were developed. These precursors were characterized, 18 F-labelled and compared in reactivity for oxime coupling. Oxime coupling was performed on an amino-oxy modified inhibited factor VII (FVIIai-ONH2 ) in low concentration to prove the applicability of the proposed method.

中文翻译：

氟-18标记的醛作为与 FVIIa 蛋白肟偶联的辅基

18 F-标记的醛可用于与化学敏感蛋白质（例如凝血因子 VII (FVII)）进行肟偶联，前提是它们具有足够的反应性并且可以在水性溶剂中反应。开发了源自[ 18 F]F-Py-TFP 和螺环碘鎓(III)叶立德前体的新型 18 F 标记的非挥发性醛辅基，用于后期 18 F 标记。对这些前体进行表征、 18 F 标记并比较肟偶联的反应性。对低浓度的氨基氧修饰的抑制因子 VII (FVIIai-ONH2 ) 进行肟偶联，以证明该方法的适用性。

更新日期：2021-01-27

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