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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Chemical control of metabolically-engineered voltage-gated K+ channels.
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Chemical control of metabolically-engineered voltage-gated K+ channels.

机译:代谢工程化电压门控K +通道的化学控制。

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摘要

Metabolic oligosaccharide engineering is a powerful approach for installing unnatural glycans with unique functional groups into the glycocalyx of living cells and animals. Using this approach, we showed that K(+) channel complexes decorated with thiol-containing sialic acids were irreversibly inhibited with scorpion toxins bearing a pendant maleimide group. Irreversible inhibition required a glycosylated K(+) channel subunit and was completely reversible with mild reductant when the tether connecting the toxin to the maleimide contained a disulfide bond. Cleavage of the disulfide bond not only restored function, but delivered a biotin moiety to the modified K(+) channel subunit, providing a novel approach for preferentially labeling wild type K(+) channel complexes functioning in cells.
机译:代谢寡糖工程技术是一种将具有独特功能基团的非天然聚糖安装到活细胞和动物的糖萼中的强大方法。使用这种方法,我们表明,带有一个含巯基唾液酸的K(+)通道复合物被带有马来酰亚胺侧基的蝎子毒素不可逆地抑制。不可逆的抑制作用需要糖基化的K(+)通道亚基,当将毒素连接到马来酰亚胺的系链包含二硫键时,可以用轻度还原剂完全逆转。二硫键的裂解不仅恢复了功能,而且还向修饰的K(+)通道亚基传递了生物素部分,为优先标记细胞中起作用的野生型K(+)通道复合物提供了一种新方法。

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