Structural and mechanistic basis for a new mode of glycosyltransferase inhibition.

Structural and mechanistic basis for a new mode of glycosyltransferase inhibition.
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DOI:
10.1038/nchembio.343
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发表时间:
2010-05
影响因子:
14.8
通讯作者:
Wagner, Gerd K.
Wagner, Gerd K.
中科院分区:
生物学1区
文献类型:
--
作者:
Pesnot, Thomas;Jorgensen, Rene;Palcic, Monica M.;Wagner, Gerd K.

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糖基转移酶是碳水化合物活性酶,在许多重要的生物过程中发挥重要作用。我们开发了一种新型半乳糖基转移酶供体类似物,它将代表性靶酶锁定在催化失活构象中,从而几乎完全消除了糖转移。其他半乳糖基转移酶的结果表明,这种新颖且独特的糖基转移酶抑制模式很可能也普遍适用于这个非常重要的酶家族的其他成员。
Glycosyltransferases are carbohydrate-active enzymes with essential roles in numerous important biological processes. We have developed a novel donor analogue for galactosyltransferases which locks a representative target enzyme in a catalytically inactive conformation, thus almost completely abolishing sugar transfer. Results with other galactosyltransferases suggest that this novel and unique mode of glycosyltransferase inhibition is, very likely, generally applicable to other members of this very important enzyme family also.
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