Fucosyltransferase-specific inhibition via next generation of fucose mimetics.
Fucosyltransferase-specific inhibition via next generation of fucose mimetics.
复制标题
通过下一代岩藻糖模拟物进行岩藻糖基转移酶特异性抑制。
DOI：
10.1039/d0cc04847j
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发表时间：
2021
期刊：
影响因子：
--
通讯作者：
Martin KC
中科院分区：
文献类型：
--
作者：
Martin KC
定制修饰细胞表面聚糖的能力为治疗各种疾病带来了巨大的希望。我们提出了一种L-岩藻糖的糖模拟物，其显著抑制FTVI和FTVII产生sLeX，但对FTIX产生LeX没有影响。因此，我们的研究结果表明，可以实现sLex显示的选择性抑制，STD-NMR研究令人惊讶地揭示，模拟物不与GDP-岩藻糖在酶结合位点的竞争。
The ability to custom-modify cell surface glycans holds great promise for treatment of a variety of diseases. We propose a glycomimetic of L-fucose that markedly inhibits the creation of sLeX by FTVI and FTVII, but has no effect on creation of LeX by FTIX. Our findings thus indicate that selective suppression of sLex display can be achieved, and STD-NMR studies surprisingly reveal that the mimetic does not compete with GDP-fucose at the enzymatic binding site.