中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Natural biflavones as novel inhibitors of cathepsin B and K

文献类型:期刊论文

作者Zeng, G. -Z.; Pan, X. -L.; Tan, N. -H.; Xiong, J.; Zhang, Y. M.
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2006-11-01
卷号41期号:11页码:1247-1252
关键词Biflavones Inhibitors Cathepsin b Cathepsin k Docking
ISSN号0223-5234
DOI10.1016/j.ejmech.2006.06.002
文献子类Article
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.
学科主题Chemistry ; Medicinal
WOS关键词LYSOSOMAL CYSTEINE PROTEASES ; SUBSTRATE-SPECIFICITY ; CRYSTAL-STRUCTURE ; OCCLUDING LOOP ; ENDOPEPTIDASE ; PEPTIDES ; CANCER ; ASSAYS
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000242454100003
公开日期2011-11-24
源URL[http://ir.kib.ac.cn:8080/handle/151853/2149]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
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
推荐引用方式
GB/T 7714
Zeng, G. -Z.,Pan, X. -L.,Tan, N. -H.,et al. Natural biflavones as novel inhibitors of cathepsin B and K[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2006,41(11):1247-1252.
APA Zeng, G. -Z.,Pan, X. -L.,Tan, N. -H.,Xiong, J.,&Zhang, Y. M..(2006).Natural biflavones as novel inhibitors of cathepsin B and K.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,41(11),1247-1252.
MLA Zeng, G. -Z.,et al."Natural biflavones as novel inhibitors of cathepsin B and K".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 41.11(2006):1247-1252.

入库方式: OAI收割

来源:昆明植物研究所

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