Deoxyelephantopin inhibits cancer cell proliferation and functions as a selective partial agonist against PPAR gamma
文献类型：期刊论文
| 作者 | Zou, Gang2; Gao, Zhenting2; Wang, Jidong1; Zhang, Yu1; Ding, Hong1 ; Huang, Jin2; Chen, Lili1; Guo, Yuewei1; Jiang, Hualiang1,2; Shen, Xu1,2
|
| 刊名 | BIOCHEMICAL PHARMACOLOGY
 |
| 出版日期 | 2008-03-15 |
| 卷号 | 75期号:6页码:1381-1392 |
| 关键词 | deoxyelephantopin PPAR gamma partial agonist surface plasmon resonance molecular docking |
| ISSN号 | 0006-2952 |
| DOI | 10.1016/j.bcp.2007.11.021 |
| 文献子类 | Article |
| 英文摘要 | Deoxyelephantopin (ESD) was reported to potentiate apoptosis, inhibit invasion and abolish osteoclastogenesis but no target protein was disclosed. Here, we discovered that ESD could significantly inhibit the proliferation of different cancer cells and induce apoptosis and cell cycle arrest at G(2)/M phase in HeLa cell. Moreover, biochemical and biophysical assays revealed that ESD acted as a specific partial agonist against PPAR gamma. Molecular docking with site-directed mutagenesis analyses indicated that ESD functioned as a partial agonist of PPAR gamma by adopting a distinct binding mode to PPAR gamma compared with rosiglitazone. The PPAR gamma knockdown results indicated that the inhibition of ESD against the cancer cell proliferation is more possibly through PPAR gamma-independent pathway and our findings might supply potent binding features for ESD/PPAR gamma interaction at atomic level, and shed light on the potential acting target information for this natural compound. (c) 2007 Elsevier Inc. All rights reserved. |
| WOS关键词 | ACTIVATED-RECEPTOR-GAMMA ; POTENT ANTIDIABETIC THIAZOLIDINEDIONE ; HUMAN BREAST-CANCER ; IN-VITRO ; TERMINAL DIFFERENTIATION ; SIGNALING PATHWAY ; NUCLEAR RECEPTORS ; LIGAND-BINDING ; COLON-CANCER ; APOPTOSIS |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000254687800014 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272958]  |
| 专题 | 天然药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药理学第三研究室 |
| 通讯作者 | Guo, Yuewei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, Shanghai 210203, Peoples R China; 2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zou, Gang,Gao, Zhenting,Wang, Jidong,et al. Deoxyelephantopin inhibits cancer cell proliferation and functions as a selective partial agonist against PPAR gamma[J]. BIOCHEMICAL PHARMACOLOGY,2008,75(6):1381-1392. |
| APA | Zou, Gang.,Gao, Zhenting.,Wang, Jidong.,Zhang, Yu.,Ding, Hong.,...&Shen, Xu.(2008).Deoxyelephantopin inhibits cancer cell proliferation and functions as a selective partial agonist against PPAR gamma.BIOCHEMICAL PHARMACOLOGY,75(6),1381-1392. |
| MLA | Zou, Gang,et al."Deoxyelephantopin inhibits cancer cell proliferation and functions as a selective partial agonist against PPAR gamma".BIOCHEMICAL PHARMACOLOGY 75.6(2008):1381-1392. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。