Emodin targets the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: enzymatic inhibition assay with crystal structural and thermodynamic characterization
文献类型：期刊论文
| 作者 | Chen, Jing1 ; Zhang, Liang1; Zhang, Yu1; Zhang, Haitao1; Du, Jiamu2; Ding, Jianping2; Guo, Yuewei1; Jiang, Hualiang1; Shen, Xu1
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| 刊名 | BMC MICROBIOLOGY
 |
| 出版日期 | 2009-05-12 |
| 卷号 | 9 |
| ISSN号 | 1471-2180 |
| DOI | 10.1186/1471-2180-9-91 |
| 文献子类 | Article |
| 英文摘要 | Background: The natural product Emodin demonstrates a wide range of pharmacological properties including anticancer, anti-inflammatory, antiproliferation, vasorelaxant and anti-H. pylori activities. Although its H. pylori inhibition was discovered, no acting target information against Emodin has been revealed to date. Results: Here we reported that Emodin functioned as a competitive inhibitor against the recombinant beta-hydroxyacyl-ACP dehydratase from Helicobacter pylori (HpFabZ), and strongly inhibited the growth of H. pylori strains SS1 and ATCC 43504. Surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) based assays have suggested the kinetic and thermodynamic features of Emodin/HpFabZ interaction. Additionally, to inspect the binding characters of Emodin against HpFabZ at atomic level, the crystal structure of HpFabZ-Emodin complex was also examined. The results showed that Emodin inhibition against HpFabZ could be implemented either through its occupying the entrance of the tunnel or embedding into the tunnel to prevent the substrate from accessing the active site. Conclusion: Our work is expected to provide useful information for illumination of Emodin inhibition mechanism against HpFabZ, while Emodin itself could be used as a potential lead compound for further anti-bacterial drug discovery. |
| WOS关键词 | TYROSINE KINASE INHIBITOR ; POLYGONUM-HYPOLEUCUM OHWI ; FATTY-ACID BIOSYNTHESIS ; CANCER CELLS ; BREAST-CANCER ; DNA-DAMAGE ; FABZ ; PROLIFERATION ; ERADICATION ; FLAVONOIDS |
| 资助项目 | National Natural Science Foundation of China[30525024] ; National Natural Science Foundation of China[90713046] ; National Natural Science Foundation of China[20721003] ; CAS Foundation[KSCX2-YW-R-18] |
| WOS研究方向 | Microbiology |
| 语种 | 英语 |
| WOS记录号 | WOS:000266803000001 |
| 出版者 | BMC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279242]  |
| 专题 | 药物安全性评价中心 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 药物发现与设计中心 天然药物化学研究室 药理学第三研究室 |
| 通讯作者 | Guo, Yuewei |
| 作者单位 | 1.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Jing,Zhang, Liang,Zhang, Yu,et al. Emodin targets the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: enzymatic inhibition assay with crystal structural and thermodynamic characterization[J]. BMC MICROBIOLOGY,2009,9. |
| APA | Chen, Jing.,Zhang, Liang.,Zhang, Yu.,Zhang, Haitao.,Du, Jiamu.,...&Shen, Xu.(2009).Emodin targets the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: enzymatic inhibition assay with crystal structural and thermodynamic characterization.BMC MICROBIOLOGY,9. |
| MLA | Chen, Jing,et al."Emodin targets the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: enzymatic inhibition assay with crystal structural and thermodynamic characterization".BMC MICROBIOLOGY 9(2009). |
入库方式： OAI收割
来源：上海药物研究所
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