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Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome
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
2011-09-01
DOI10.3390/molecules16097551
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
WOS记录号WOS:000295211000027
项目编号20672010
资助机构National Natural Science Foundation of China
引用统计
被引频次:7[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/400002259/52742
专题北京大学药学院
北京大学药学院_药物化学系
北京大学药学院_分子与细胞药理学系
北京大学临床肿瘤学院_肿瘤放疗科
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
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.
APA Ma, Yuheng.,Xu, Bo.,Fang, Yuan.,Yang, Zhenjun.,Cui, Jingrong.,...&Zhang, Lihe.(2011).Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome.MOLECULES,16(9),7551-7564.
MLA Ma, Yuheng,et al."Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome".MOLECULES 16.9(2011):7551-7564.
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