General Method for Labeling siRNA by Click Chemistry with Fluorine-18 for the Purpose of PET Imaging

作者：Mercier Frederic; Paris Jerome; Kaisin Geoffroy; Thonon David; Flagothier Jessica; Teller Nathalie; Lemaire Christian; Luxen Andre^*

来源：Bioconjugate Chemistry, 2011, 22(1): 108-114.

DOI：10.1021/bc100263y

The alkyne-azide Cu(I)-catalyzed Huisgen cycloaddition, a click-type reaction, was used to label a double-stranded oligonucleotide (siRNA) with fluorine-18. An alkyne solid support CPG for the preparation of monostranded oligonucleotides functionalized with alkyne has been developed. Two complementary azide labeling agents (1-(azidomethyl)-4[(18)F]fluorobenzene) and 1-azido-4-(3-[(18)F]fluoropropoxy)benzene have been produced with 41% and 35% radiochemical yields (decay-corrected), respectively. After annealing with the complementary strand, the siRNA was directly labeled by click chemistry with [(18)F]fluoroazide to produce the [(18)F]-radiolabeled siRNA with excellent radiochemical yield and purity.

• 出版日期2011-1