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Design, Synthesis and Structural Analysis of Glucocerebrosidase Imaging Agents
Chemistry - A European Journal ( IF 4.3 ) Pub Date : 2021-09-27 , DOI: 10.1002/chem.202102359
Rhianna J Rowland 1 , Yurong Chen 2 , Imogen Breen 1 , Liang Wu 1 , Wendy A Offen 1 , Thomas J Beenakker 2 , Qin Su 3 , Adrianus M C H van den Nieuwendijk 2 , Johannes M F G Aerts 3 , Marta Artola 3 , Herman S Overkleeft 2 , Gideon J Davies 1
Affiliation  

Tagged cyclophellitols offer a powerful activity-based probe (ABP) approach to the study of glycosidase activities. Here, a range of cyclophellitol epoxide and aziridine inhibitors and ABPs were synthesised and investigated on the 3D structure of human β-glucocerebrosidase (GBA), demonstrating their mechanism-based mode of action. We envisage these inactivators will serve useful in the study of GBA in relation to Gaucher Disease.
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中文翻译:

葡萄糖脑苷脂酶显像剂的设计、合成和结构分析

标记的环酚为研究糖苷酶活性提供了一种强大的基于活性的探针 (ABP) 方法。在这里,合成了一系列环酚醇环氧化物和氮丙啶抑制剂和 ABP,并研究了人类 β-葡萄糖脑苷脂酶 (GBA) 的 3D 结构,证明了它们基于机制的作用模式。我们设想这些灭活剂将有助于研究与戈谢病相关的 GBA。
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更新日期:2021-11-30
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