A natural product-like inhibitor of NEDD8-activating enzyme

被引:75
|
作者
Leung, Chung-Hang [1 ]
Chan, Daniel Shiu-Hin [2 ]
Yang, Hui [2 ]
Abagyan, Ruben [3 ]
Lee, Simon Ming-Yuen [4 ]
Zhu, Guo-Yuan [1 ]
Fong, Wang-Fun [1 ]
Ma, Dik-Lung [2 ]
机构
[1] Hong Kong Baptist Univ, Sch Chinese Med, Ctr Canc & Inflammat Res, Kowloon Tong, Hong Kong, Peoples R China
[2] Hong Kong Baptist Univ, Dept Chem, Kowloon Tong, Hong Kong, Peoples R China
[3] Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, San Diego, CA 92103 USA
[4] Univ Macau, Inst Chinese Med Sci, Taipa, Macao, Peoples R China
关键词
DISCOVERY; CULLIN; NEDD8; BIFLAVONOIDS; LIGAND;
D O I
10.1039/c0cc04927a
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The natural product-like 6,6 ''-biapigenin has been identified as only the second inhibitor of NEDD8-activating enzyme using virtual screening. This compound was active in enzyme and cell-based assays, with potency in the micromolar range.
引用
收藏
页码:2511 / 2513
页数:3
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