Crystal structure determination of a chimeric FabF by XRD
文献类型：期刊论文
| 作者 | Li, Ke1,2; Li, Li2; Xu, Ye-Chun2
|
| 刊名 | NUCLEAR SCIENCE AND TECHNIQUES
 |
| 出版日期 | 2017-09 |
| 卷号 | 28期号:9 |
| 关键词 | FabF Chimera X-ray diffraction Crystal structure determination |
| ISSN号 | 1001-8042 |
| DOI | 10.1007/s41365-017-0281-0 |
| 文献子类 | Article |
| 英文摘要 | Beta-ketoacyl-acyl-carrier-protein synthase II, an important enzyme in biosynthesis of bacterial fatty acid, is an attractive target in antibacterial drug design. Platensimycin (PTM), produced by Streptomyces platensis, has a strong, broad-spectrum Gram-positive antibacterial activity by selectively targeting to FabF but exhibits no inhibition to the FabF from Streptomyces platensis (spFabF). To study the self-resistance mechanism within the PTM-producing strain and provide hint for development of novel antibiotics, it is imperative to solve the structure of spFabF and elucidate the difference between spFabF and other FabFs which are not resistant to PTM. To this end, we constructed four chimeric FabFs based on the sequence of spFabF and its homologous protein after the expression of wide-type spFabF was failed. The crystal structure of one chimera, js(200)FabF, of 91.2% sequence identity to spFabF, was solved. A structure comparison of js(200)FabF with a PTM-bound FabF suggested that three loops nearby the catalytic site might play key roles in preventing the binding of PTM to spFabF. The results provide an encouraging basis for further studies on the self-resistance mechanism and structure-based design of novel antibiotics targeting FabFs. |
| WOS关键词 | FATTY-ACID SYNTHASE ; STREPTOMYCES-PLATENSIS ; BIOSYNTHESIS ; INHIBITOR |
| 资助项目 | National Natural Science Foundation of China[81502987] ; National Natural Science Foundation of China[81422047] |
| WOS研究方向 | Nuclear Science & Technology ; Physics |
| 语种 | 英语 |
| WOS记录号 | WOS:000408853800004 |
| 出版者 | SPRINGER SINGAPORE PTE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272508]  |
| 专题 | 药物发现与设计中心 |
| 通讯作者 | Xu, Ye-Chun |
| 作者单位 | 1.Shanghai Univ, Coll Sci, 99 Shangda Rd, Shanghai 200444, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Ke,Li, Li,Xu, Ye-Chun. Crystal structure determination of a chimeric FabF by XRD[J]. NUCLEAR SCIENCE AND TECHNIQUES,2017,28(9). |
| APA | Li, Ke,Li, Li,&Xu, Ye-Chun.(2017).Crystal structure determination of a chimeric FabF by XRD.NUCLEAR SCIENCE AND TECHNIQUES,28(9). |
| MLA | Li, Ke,et al."Crystal structure determination of a chimeric FabF by XRD".NUCLEAR SCIENCE AND TECHNIQUES 28.9(2017). |
入库方式： OAI收割
来源：上海药物研究所
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