A PARACEST MRI contrast agent to detect enzyme activity
A PARACEST MRI contrast agent to detect enzyme activity
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DOI：
10.1021/ja063874f
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发表时间：
2006-11-01
影响因子：
15
通讯作者：
Pagel, Marty D.
中科院分区：
文献类型：
--
作者：
Yoo, Byunghee;Pagel, Marty D.
合成了一种“智能”PARACEST MRI 造影剂来检测 caspase-3，这是细胞凋亡的重要生物标志物。众所周知的 caspase-3 底物 DEVD (Asp-Glu-Val-Asp) 使用锚定在聚合物载体上的镧系配体一侧臂上的氨基进行延伸。 DEVD-(Tm-DOTA) 的酰胺显示出 PARACEST 效应，MR 饱和度为 -51 ppm。 DEVD-(Tm-DOTA) 酰胺被 caspase-3 成功裂解，暴露出游离胺基，这表明 PARACEST 在 +8 ppm 处饱和。 caspase-3的酶活性可以通过这种生物转化引起的PARACEST效应的变化来检测。
A “smart” PARACEST MRI contrast agent was synthesized to detect caspase-3, which is an important biomarker in apoptosis. The well-known caspase-3 substrate, DEVD (Asp-Glu-Val-Asp), was elongated using the amino group on one sidearm of lanthanide ligand anchored on the polymer support. The amide of DEVD-(Tm-DOTA) showed a PARACEST effect with MR saturation at −51 ppm. DEVD-(Tm-DOTA) amide was successfully cleaved by caspase-3, exposing the free amine group, which showed PARACEST with saturation at +8 ppm. The enzymatic activity of caspase-3 can be detected by the change in PARACEST effect caused by this biotransformation.