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Recent developments of transition-state analogue glycosidase inhibitors of non-natural product origin

机译:非天然产物来源的过渡态类似物糖苷酶抑制剂的最新进展

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Glycosidse inhibitors have been subject to extensive interest in the past decade.As glycoside cleavage is a biologically widespread process,glycosidase inhibitors have many potential medical applications,Inhibition of intestinal #alpha#-glycosidases can be used to treat diabetes through the lowering of blood glucose levels,and several #alpha#-glycosidase inhibitors are being marketed against type 2 diabetes.An alternative way of treating diabetes that has been explored recently is through inhibition of glycogenphosphorylase,which also results in a lowering of blood glucose.Glycosidases arealso involved in the trimming of cell-and viral-surface oligosaccharides,which also can be used as a therapeutic target.Inhibition of these glycosidases can disrupt biosynthesis of oigosaccharides and hence cell-cell or cell-virus recognition processes.This principle is used in the anti-influenza neuraminidase inhibitors that have recently been marketed and is also the basis for the potential use of #alpha#-glycosidase inhibitors against HIV,Gauchers disease,hepatitis,and cancer.
机译:在过去的十年中,糖苷酶抑制剂受到了广泛的关注。由于糖苷的裂解是生物学上广泛的过程,糖苷酶抑制剂具有许多潜在的医学应用,肠道#α#糖苷酶的抑制可通过降低血糖来治疗糖尿病。水平和几种针对2型糖尿病的#alpha#-糖苷酶抑制剂正在市场上销售。最近研究出的另一种治疗糖尿病的方法是抑制糖原磷酸化酶,从而降低血糖。糖苷酶也参与其中。修整细胞表面和病毒表面的寡糖,也可以用作治疗靶标。抑制这些糖苷酶可以破坏卵糖的生物合成,从而破坏细胞-细胞或细胞-病毒的识别过程。该原理用于抗流感最近上市的神经氨酸酶抑制剂,也是潜在使用#的基础alpha#-糖苷酶抑制剂,可抵抗HIV,Gauchers病,肝炎和癌症。

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