18F标记的胰岛素：一种将正电子发射体引入肽和蛋白质的辅基方法。
18F-labeled insulin: a prosthetic group methodology for incorporation of a positron emitter into peptides and proteins.
作者信息
Shai Y, Kirk K L, Channing M A, Dunn B B, Lesniak M A, Eastman R C, Finn R D, Roth J, Jacobson K A
机构信息
Laboratory of Chemistry and Diabetes Branch, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, Maryland 20892.
出版信息
Biochemistry. 1989 May 30;28(11):4801-6. doi: 10.1021/bi00437a042.
Abstract
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.
摘要
在本研究中，我们合成了高比放射性的18F标记胰岛素。采用了一种新的辅基方法，其中[18F]氟化物取代了4-（溴甲基）-苯甲胺中间体的溴基团。4-（氟甲基）苯甲酰产物化学性质稳定。通过与人类细胞上的胰岛素受体结合以及刺激大鼠脂肪细胞中的葡萄糖代谢进行体外测量，18F标记胰岛素保留了天然胰岛素的基本生物学特性。整个过程可以快速进行，以产生纯度足以进行体内研究的产物。该方法似乎适用于多种肽。
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