Shikii Kazuaki, Sakurai Satoshi, Utsumi Hiroaki, Seki Hiroko, Tashiro Mitsuru
Chemical Analysis Center, Chiba University, Yayoi, Inage, Chiba 263-8522, Japan.
Anal Sci. 2004 Oct;20(10):1475-7. doi: 10.2116/analsci.20.1475.
19F NMR techniques were employed to characterize the binding property of the widely used general anesthetic halothane with human serum albumin (HSA). It was found that 19F(1H) NOE and 2D 1H-19F HOESY experiments detected intermolecular NOEs between halothane 19F and HSA protons. Measurements of the diffusion coefficients for halothane were also carried out by 1H and 19F NMR, indicating the interaction of halothane with HSA. The present results indicate that these techniques are very suitable to identify a fluorine-containing ligand binding with a protein receptor in the drug-discovery process.
采用19F核磁共振技术来表征广泛使用的全身麻醉剂氟烷与人血清白蛋白(HSA)的结合特性。结果发现,19F(1H) NOE和二维1H-19F HOESY实验检测到氟烷19F与HSA质子之间的分子间NOE。还通过1H和19F核磁共振对氟烷的扩散系数进行了测量,表明氟烷与HSA之间存在相互作用。目前的结果表明,这些技术非常适合在药物发现过程中识别与蛋白质受体结合的含氟配体。