利用 sp 杂化开发 α-L-岩藻糖苷酶抑制剂的合成与晶体学研究。
Synthetic and Crystallographic Insight into Exploiting sp Hybridization in the Development of α-l-Fucosidase Inhibitors.
机构信息
School of Molecular Sciences, University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
Present address: School of Chemistry, University College Dublin, Stillorgan Road, Belfield, Dublin, 4, Ireland.
出版信息
Chembiochem. 2019 Jun 3;20(11):1365-1368. doi: 10.1002/cbic.201800710. Epub 2019 Mar 18.
The sugar fucose plays a myriad of roles in biological recognition. Enzymes hydrolyzing fucose from glycoconjugates, α-l-fucosidases, are important targets for inhibitor and probe development. Here we describe the synthesis and evaluation of novel α-l-fucosidase inhibitors, with X-ray crystallographic analysis using an α-l-fucosidase from Bacteroides thetaiotamicron helping to lay a foundation for future development of inhibitors for this important enzyme class.
岩藻糖在生物识别中发挥着多种作用。能够从糖缀合物上水解岩藻糖的酶，即α-L-岩藻糖苷酶，是抑制剂和探针开发的重要靶点。在这里，我们描述了新型α-L-岩藻糖苷酶抑制剂的合成与评价，使用来源于拟杆菌属（Bacteroides thetaiotamicron）的α-L-岩藻糖苷酶的 X 射线晶体结构分析为该重要酶类抑制剂的进一步开发奠定了基础。
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