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学科主题: 药学
题名:
Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome
作者: Ma, Yuheng; Xu, Bo; Fang, Yuan; Yang, Zhenjun; Cui, Jingrong; Zhang, Liangren; Zhang, Lihe
关键词: 20S proteasome ; inhibitor ; peptide aldehydes ; synthesis ; structure-activity relationship
刊名: MOLECULES
发表日期: 2011-09-01
DOI: 10.3390/molecules16097551
卷: 16, 期:9, 页:7551-7564
收录类别: SCI
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]: ANGSTROM RESOLUTION ; SALINOSPORAMIDE-A ; CRYSTAL-STRUCTURE ; VINYL SULFONES ; BETA-5 SUBUNIT ; BINDING MODE ; BORONIC ACID ; MECHANISM ; COMPLEX ; DESIGN
英文摘要:

Based on the analysis of the crystal structure of MG101 (1) and 20S proteasomes, a new series of peptide aldehyde derivatives were designed and synthesized. Their ability to inhibit 20S proteasome was assayed. Among them, Cbz-Glu(OtBu)-Phe-Leucinal (3c), Cbz-Glu(OtBu)-Leu-Leucinal (3d), and Boc-Ser(OBzl)-Leu-Leucinal (3o) exhibited the most activity, which represented an order of magnitude enhancement compared with MG132 (2). The covalent docking protocol was used to explore the binding mode. The structure-activity relationship of the peptide aldehyde inhibitors is discussed.

语种: 英语
所属项目编号: 20672010
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000295211000027
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/52742
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Ma, Yuheng,Xu, Bo,Fang, Yuan,et al. Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome[J]. MOLECULES,2011,16(9):7551-7564.
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