IR@PKUHSC  > 北京大学药学院
学科主题药学
Synthesis of N-substituted epsilon-hexonolactams as pharmacological chaperones for the treatment of N370S mutant Gaucher disease
Wang, Guan-Nan1,2; Twigg, Gabriele3; Butters, Terry D.3; Zhang, Siwei1,2; Zhang, Liangren1,2; Zhang, Li-He1,2; Ye, Xin-Shan1,2
刊名ORGANIC & BIOMOLECULAR CHEMISTRY
2012
DOI10.1039/c2ob06987c
10期:15页:2923-2927
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]LYSOSOMAL STORAGE DISORDERS ; ACID BETA-GLUCOSIDASE ; HIGHLY POTENT ; RATIONAL DESIGN ; ENZYME-ACTIVITY ; JEWISH PATIENTS ; MUTATIONS ; CONFORMATION ; STRATEGIES ; INHIBITORS
英文摘要

A series of N-substituted e-hexonolactams have been designed and prepared by a concise route with a tandem ring-expansion reaction as the key step. Some of the N-substituted epsilon-hexonolactams show better enhancements to N370S mutant beta-glucocerebrosidase activity than NB-DNJ and NN-DNJ. Both the experimental results and computational studies highlight the importance of the carbonyl group for stabilizing protein folds in the mutant enzyme. The structure-activity relationships are also discussed. These novel N-alkylated iminosugars are promising pharmacological chaperones for the treatment of N370S mutant Gaucher disease.

语种英语
WOS记录号WOS:000301958100002
资助机构National Natural Science Foundation of China ; Ministry of Science and Technology of China ; Oxford Glycobiology Institute
引用统计
被引频次:20[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/66711
专题北京大学药学院
北京大学药学院_药物化学系
作者单位1.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
3.Univ Oxford, Glycobiol Inst, Dept Biochem, Oxford OX1 3QU, England
推荐引用方式
GB/T 7714
Wang, Guan-Nan,Twigg, Gabriele,Butters, Terry D.,et al. Synthesis of N-substituted epsilon-hexonolactams as pharmacological chaperones for the treatment of N370S mutant Gaucher disease[J]. ORGANIC & BIOMOLECULAR CHEMISTRY,2012,10(15):2923-2927.
APA Wang, Guan-Nan.,Twigg, Gabriele.,Butters, Terry D..,Zhang, Siwei.,Zhang, Liangren.,...&Ye, Xin-Shan.(2012).Synthesis of N-substituted epsilon-hexonolactams as pharmacological chaperones for the treatment of N370S mutant Gaucher disease.ORGANIC & BIOMOLECULAR CHEMISTRY,10(15),2923-2927.
MLA Wang, Guan-Nan,et al."Synthesis of N-substituted epsilon-hexonolactams as pharmacological chaperones for the treatment of N370S mutant Gaucher disease".ORGANIC & BIOMOLECULAR CHEMISTRY 10.15(2012):2923-2927.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Wang, Guan-Nan]的文章
[Twigg, Gabriele]的文章
[Butters, Terry D.]的文章
百度学术
百度学术中相似的文章
[Wang, Guan-Nan]的文章
[Twigg, Gabriele]的文章
[Butters, Terry D.]的文章
必应学术
必应学术中相似的文章
[Wang, Guan-Nan]的文章
[Twigg, Gabriele]的文章
[Butters, Terry D.]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。