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学科主题: 药学
题名:
Rational Design and Synthesis of Highly Potent Pharmacological Chaperones for Treatment of N370S Mutant Gaucher Disease
作者: Wang, Guan-Nan1,2; Reinkensmeier, Gabriele3; Zhang, Si-Wei1,2; Zhou, Jian1,2; Zhang, Liang-Ren1,2; Zhang, Li-He1,2; Butters, Terry D.3; Ye, Xin-Shan1,2
刊名: JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2009-05-28
DOI: 10.1021/jm801506m
卷: 52, 期:10, 页:3146-3149
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: LYSOSOMAL STORAGE DISORDERS ; ACID BETA-GLUCOSIDASE ; JEWISH PATIENTS ; INHIBITORS ; DERIVATIVES ; MUTATIONS ; MIGLUSTAT ; INCREASE
英文摘要:

Highly potent N-substituted delta-lactams have been rationally designed and synthesized by a concise route with a one-pot tandem reaction as key step. These iminosugars show weak inhibition of wildtype beta-glucocerebrosidase but 3- to 6-fold increases in mutant enzyme activity (N370S).

语种: 英语
项目资助者: National Natural Science Foundafion of China ; Ministry of Science and Technology of China ; Oxford Glycobiology Institute
WOS记录号: WOS:000266296200003
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64829
Appears in Collections:北京大学药学院_期刊论文

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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, Dept Biochem, Glycobiol Inst, Oxford OX1 3QU, England

Recommended Citation:
Wang, Guan-Nan,Reinkensmeier, Gabriele,Zhang, Si-Wei,et al. Rational Design and Synthesis of Highly Potent Pharmacological Chaperones for Treatment of N370S Mutant Gaucher Disease[J]. JOURNAL OF MEDICINAL CHEMISTRY,2009,52(10):3146-3149.
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