S-乙酰基-NHS-MAG_3在反义显像研究中的应用及进展

Application and Development of N-hydroxysuccinimidyl S-acetylmercap to Acetyltriglycline in Antisense Imaging

随着反义显像研究的深入,一种新的双功能螯合剂巯基乙酰三甘氨酰-N-羟基丁二酰亚胺酯(S-乙酰基-NHS-MAG3)受到广泛重视。利用反义寡核苷酸的NHS-MAG3进行S-乙酰基-NHS-MAG3放射性核素标记,得到的标记产物具有较高的标记率、比活度和放化纯度,且体内外稳定性好,与血清蛋白的非特异性结合低;S-乙酰基-NHS-MAG3不会影响反义寡核苷酸的杂交特异性,并能增加标记的反义寡核苷酸在细胞内的积聚,因此,S-乙酰基-NHS-MAG3在反义显像研究中具有重要的应用价值。

With the further research of antisense imaging, N-hydroxysuccinimidyl S-acetylmercap to acetyltriglycline(S-acetyl-NHS-MAG_3) as a novel bifunctional chelator is interested by scientists and used widely. It is proved that the radiolabeled products by the NHS-MAG_3-labeling method show high labeling yield, high specific activities, high radiochemical purity and desi-rable stability in vitro and in vivo. The binding with plasma protein of the labeled products is low. In addition, NHS-MAG_3 will not affect the specificity of hybridization of the antisense oligonucleotides and can increase the accumulation of the labeled antisense oligonucleotides in the cells. The properties NHS-MAG_3 make it suitable for labeling antisense oligo-nucleotides and possible to be a potentially useful radiopharmaceuticals for diagnosis and therapy.