Chemistry Division, School of Life Sciences, University of Sussex, Brighton, UK.
Org Biomol Chem. 2011 Aug 21;9(16):5625-9. doi: 10.1039/c1ob05384a. Epub 2011 Jun 30.
The synthesis of conjugates of phospha-oseltamivir to the well established reporter groups fluorescein and biotin and an approach to multimeric inhibitors is described. We report powerful inhibition of the influenza neuraminidase by these probes and quantify fluorescence quenching during binding of the fluorescein conjugate through titration with the neuraminidase. Thus, we show that they could be useful tools to efficiently inhibit, detect and quantify the virus and the neuraminidase in biological systems.
描述了将磷酰奥司他韦与荧光素和生物素等成熟的报告基团缀合的方法,以及一种多聚抑制剂的方法。我们报告了这些探针对流感神经氨酸酶的强大抑制作用,并通过用神经氨酸酶滴定定量测量荧光素缀合物结合过程中的荧光猝灭,从而证明它们可以成为有效抑制、检测和定量生物体系中病毒和神经氨酸酶的有用工具。