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题名: Natural biflavones as novel inhibitors of cathepsin B and K
作者: Zeng, G. -Z.; Pan, X. -L.; Tan, N. -H.; Xiong, J.; Zhang, Y. M.
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
关键词: biflavones ; inhibitors ; cathepsin B ; cathepsin K ; docking
英文摘要: Cathepsin B and K, two important members in lysosomal proteases, involve in many serious human diseases, such as tumor and osteoporosis. In order to find their novel inhibitors, we performed the inhibition assays of cathepsin B and cathepsin K in vitro, randomly screened compounds from plants, and found six biflavones, named AMF1-5 and HIF, can potently inhibit cathepsin B and cathepsin K, especially AMF4 and HIF with IC50 of 0.62 and 0.58 W against cathepsin B. They are novel inhibitors for cathepsin B and K. Inhibition and flexible docking studies indicated that these biflavones are reversible inhibitors of cathepsin B, and their binding patterns and interaction modes with cathepsin B made them more specific to cathepsin B endopeptidase. (c) 2006 Elsevier Masson SAS. All rights reserved.
出版日期: 2006-11-01
卷号: 41, 期号:11, 页码:1247-1252
DOI标识: 10.1016/j.ejmech.2006.06.002
语种: 英语
ISSN号: 0223-5234
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/2149
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources W China, Kunming Inst Bot, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China

Recommended Citation:
Zeng, GZ; Pan, XL; Tan, NH; Xiong, J; Zhang, YM.Natural biflavones as novel inhibitors of cathepsin B and K,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2006,41(11):1247-1252
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