Sulfone-Based Probes Unraveled Dihydrolipoamide S-Succinyltransferase as an Unprecedented Target in Phytopathogens
文献类型：期刊论文
| 作者 | Chen, Biao1; Long, Qingsu1; Zhao, Yongliang1; Wu, Yuanyuan1; Ge, Shasha1; Wang, Peiyi1; Yang, Cai-Guang2 ; Chi, Yonggui1; Song, Baoan1; Yang, Song1,3
|
| 刊名 | JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
 |
| 出版日期 | 2019-06-26 |
| 卷号 | 67期号:25页码:6962-6969 |
| 关键词 | bactericide 0 target DLST covalent inhibitor energy production |
| ISSN号 | 0021-8561 |
| DOI | 10.1021/acs.jafc.9b02059 |
| 文献子类 | Article |
| 英文摘要 | Target validation of current drugs remains the major challenge for target-based drug discovery, especially for agrochemical discovery. The bactericide 0 represents a novel lead structure and has shown potent efficacy against those diseases that are extremely difficult to control, such as rice bacterial leaf blight. However, no detailed target analysis of this bactericide has been reported. Here, we developed a panel of 0-derived probes 1-6, in which a conservative modification (alkyne tag) was introduced to keep the antibacterial activity of 0 and provide functionality for target identification via click chemistry. With these cell-permeable probes, we were able to discover dihydrolipoamide S-succinyltransferase (DLST) as an unprecedented target in living cells. The probes showed good preference for DLST, especially probe 1, which demonstrated distinct selectivity and reactivity. Also, we reported 0 as the first covalent DLST inhibitor, which has been used to confirm the involvement of DLST in the regulation of energy production. |
| WOS关键词 | PROTEIN ; DERIVATIVES ; INHIBITION |
| WOS研究方向 | Agriculture ; Chemistry ; Food Science & Technology |
| 语种 | 英语 |
| WOS记录号 | WOS:000473251400006 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309430]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Song, Baoan; Yang, Song |
| 作者单位 | 1.Guizhou Univ, Minist Educ, Key Lab Green Pesticide & Agr Bioengn, Lab Breeding Base Green Pesticide & Agr Bioengn, Guiyang 550025, Guizhou, Peoples R China; 2.Chinese Acad Sci, Lab Chem Biol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.East China Univ Sci & Technol, Coll Pharm, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Biao,Long, Qingsu,Zhao, Yongliang,et al. Sulfone-Based Probes Unraveled Dihydrolipoamide S-Succinyltransferase as an Unprecedented Target in Phytopathogens[J]. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,2019,67(25):6962-6969. |
| APA | Chen, Biao.,Long, Qingsu.,Zhao, Yongliang.,Wu, Yuanyuan.,Ge, Shasha.,...&Yang, Song.(2019).Sulfone-Based Probes Unraveled Dihydrolipoamide S-Succinyltransferase as an Unprecedented Target in Phytopathogens.JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,67(25),6962-6969. |
| MLA | Chen, Biao,et al."Sulfone-Based Probes Unraveled Dihydrolipoamide S-Succinyltransferase as an Unprecedented Target in Phytopathogens".JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY 67.25(2019):6962-6969. |
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。