Three flavonoids targeting the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: Crystal structure characterization with enzymatic inhibition assay
文献类型：期刊论文
| 作者 | Zhang, L; Kong, YH; Wu, DL; Zhang, HT; Wu, J; Chen, J; Ding, JP; Hu, LH; Jiang, HL; Shen, X |
| 刊名 | PROTEIN SCIENCE
 |
| 出版日期 | 2008 |
| 卷号 | 17期号:11页码:1971-1978 |
| 关键词 | HpFabZ quercetin apigenin (S)-sakuranetin complex structure inhibitory mechanism |
| 通讯作者 | Hu, LH (reprint author), Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China.,simmhulh@mail.shcnc.ac.cn ; xshen@mail.shcnc.ac.cn |
| 英文摘要 | Flavonoids are the major functional components of many herbal and insect preparations and demonstrate varied pharmacological functions including antibacterial activity. Here by enzymatic assay and crystal structure analysis, we studied the inhibition of three flavonoids (quercetin, apigenin, and (S)-sakuranetin) against the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori (HpFabZ). These three flavonoids are all competitive inhibitors against HpFabZ by either binding to the entrance of substrate tunnel B (binding model A) or plugging into the tunnel C near the catalytic residues (binding model B) mainly by hydrophobic interaction and hydrogen-bond pattern. Surrounded by hydrophobic residues of HpFabZ at both positions of models A and B, the methoxy group at C-7 of (S)-sakuranetin seems to play an important role for the inhibitor's binding to HpFabZ, partly responsible for the higher inhibitory activity of (S)-sakuranetin than those of quercetin and apigenin against HpFabZ (IC50 in mu M: (S)-sakuranetin, 2.0 +/- 0.1; quercetin: 39.3 +/- 2.7; apigenin, 11.0 +/- 2.5). Our work is expected to supply useful information for understanding the potential antibacterial mechanism of flavonoids. |
| 学科主题 | Biochemistry & Molecular Biology |
| 类目[WOS] | Biochemistry & Molecular Biology |
| 关键词[WOS] | FABZ |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000260423400010 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1455]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Zhang, L,Kong, YH,Wu, DL,et al. Three flavonoids targeting the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: Crystal structure characterization with enzymatic inhibition assay[J]. PROTEIN SCIENCE,2008,17(11):1971-1978. |
| APA | Zhang, L.,Kong, YH.,Wu, DL.,Zhang, HT.,Wu, J.,...&Shen, X.(2008).Three flavonoids targeting the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: Crystal structure characterization with enzymatic inhibition assay.PROTEIN SCIENCE,17(11),1971-1978. |
| MLA | Zhang, L,et al."Three flavonoids targeting the beta-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: Crystal structure characterization with enzymatic inhibition assay".PROTEIN SCIENCE 17.11(2008):1971-1978. |
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