Development of cell-impermeable coelenterazine derivatives
Development of cell-impermeable coelenterazine derivatives
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DOI：
10.1039/c3sc51985f
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发表时间：
2013-01-01
期刊：
影响因子：
8.4
通讯作者：
Kikuchi, Kazuya
中科院分区：
文献类型：
--
作者：
Lindberg, Eric;Mizukami, Shin;Kikuchi, Kazuya
我们描述了第一个细胞膜不可渗透的腔肠素衍生物（CoelPhos）的发展。CoelPhos是通过腔肠素与含有末端阴离子膦酸酯部分的连接体进行烷基化而构建的。CoelPhos与Gaussia荧光素酶（GLuc）的生物发光活性与海肾荧光素酶相比显示出显著更高的活性。在活细胞的成像研究中，外膜结合的GLuc用CoelPhos清晰成像。另一方面，细胞内定位的GLuc没有检测到信号，证明了这种新型腔肠动物底物衍生物的不渗透性。CoelPhos作为一种新的生物发光工具，用于监测细胞表面界面的动态融合事件具有潜在的实用性。
We describe the development of the first cell-membrane impermeable coelenterazine derivative (CoelPhos). CoelPhos was constructed by the alkylation of coelenterazine with a linker containing a terminal anionic phosphonate moiety. The bioluminescence activity of CoelPhos with Gaussia luciferase (GLuc) showed a significantly higher activity in comparison with Renilla luciferase. In imaging studies with living cells, outer membrane bound GLuc was clearly imaged with CoelPhos. On the other hand no signal could be detected with intracellularly localized GLuc, demonstrating the impermeability of this novel coelenterate substrate derivative. CoelPhos has potential utility as a new bioluminogenic tool for the monitoring of dynamic fusion events at the cell-surface interface.