Li Ying, Liu Zhibo, Harwig Curtis W, Pourghiasian Maral, Lau Joseph, Lin Kuo-Shyan, Schaffer Paul, Benard Francois, Perrin David M
Chemistry Department, 2036 Main Mall, University of British Columbia Vancouver, B.C., Canada V6T-1Z1.
Am J Nucl Med Mol Imaging. 2013;3(1):57-70. Epub 2013 Jan 5.
A clickable alkyne-modified arylborimidine is rapidly converted in 15 minutes to a highly polar (18)F-aryltrifluoroborate anion ((18)F-ArBF(3) (-)) at high specific activity. Following labeling, the alkyne-(18)F-ArBF(3) (-) was conjugated to the peptide bombesin (BBN) within 25 minutes in a second step without need for prior work-up making this one-pot-two-step method easy, user-friendly, and generally applicable. Bombesin was chosen to provide functional PET images of prostate cancer xenografts in mice of which there are few. Whereas BBN is labeled to provide some of the first in vivo tumor images based on this technique, click-labeling is recognized for its generality and broad substrate scope. Hence these results are likely to be useful for click labeling most peptides and other biomolecules.
一种可点击的炔烃修饰的芳基硼亚胺在15分钟内迅速转化为具有高比活度的高极性（18）F-芳基三氟硼酸盐阴离子（（18）F-ArBF₃⁻）。标记后，炔烃-（18）F-ArBF₃⁻在第二步中于25分钟内与蛙皮素（BBN）偶联，无需事先进行后处理，使得这种一锅两步法简便、用户友好且普遍适用。选择蛙皮素是为了在小鼠体内提供很少见的前列腺癌异种移植瘤的功能性PET图像。虽然基于该技术对BBN进行标记以提供一些首批体内肿瘤图像，但点击标记因其通用性和广泛的底物范围而得到认可。因此，这些结果可能对大多数肽和其他生物分子的点击标记很有用。
