F-18-LABELED INSULIN - A PROSTHETIC GROUP METHODOLOGY FOR INCORPORATION OF A POSITRON EMITTER INTO PEPTIDES AND PROTEINS
F-18-LABELED INSULIN - A PROSTHETIC GROUP METHODOLOGY FOR INCORPORATION OF A POSITRON EMITTER INTO PEPTIDES AND PROTEINS
复制标题
DOI：
10.1021/bi00437a042
复制
发表时间：
1989-05-30
期刊：
影响因子：
2.9
通讯作者：
JACOBSON, KA
中科院分区：
文献类型：
--
作者：
SHAI, Y;KIRK, KL;JACOBSON, KA
在本研究中，我们合成18F标记的高比放射性胰岛素。使用了一种新的辅基方法，其中[18 F]氟化物取代4-（溴甲基）苯甲酰胺中间体的溴基。4-（氟甲基）苯甲酰基产物是化学稳定的。18F标记的胰岛素保留了天然胰岛素的基本生物学特性，如通过与人细胞上的胰岛素受体结合和刺激大鼠脂肪细胞中的葡萄糖代谢在体外测量的。整个过程可以快速进行，以产生足够纯度的产物，以允许体内研究。该方法似乎适用于各种各样的肽。
In the present study we synthesize 18F-labeled insulin of high specific radioactivity. A new prosthetic group methodology, in which [18F]fluoride displaces a bromide group of 4-(bromomethyl)benzoylamine intermediates, was used. The 4-(fluoromethyl)benzoyl product was chemically stable. 18F-labeled insulin retains the essential biological properties of native insulin, as measured in vitro by binding to insulin receptors on human cells and stimulation of glucose metabolism in rat adipocytes. The overall process can be carried out speedily to yield a product of sufficient purity to permit in vivo studies. The method appears to be applicable to a wide variety of peptides.