Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine gamma-Lyase
文献类型：期刊论文
| 作者 | Hu, Youtian2; Wang, Lu3; Han, Xu4,5; Zhou, Yueyang2; Zhang, Tonghui2; Wang, Li2; Hong, Ting1,2; Zhang, Wei6; Guo, Xun-Xiang2; Sun, Jielin2 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2019-02-14 |
| 卷号 | 62期号:3页码:1677-1683 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.8b01720 |
| 通讯作者 | Yu, Jing(jingyu@sjtu.edu.cn) ; Liu, Hong(hliu@simm.ac.cn) ; Wu, Fang(fang.wu@sjtu.edu.cn) |
| 英文摘要 | We identify three submicromolar inhibitors with new chemical scaffolds for cystathionine gamma-lyase (CSE) by a tandem-well-based high-throughput assay. NSC4056, the most potent inhibitor with an IC50 of 0.6 mu M, which is also known as aurintricarboxylic acid, selectively binds to Arg and Tyr residues of CSE active site and preferably inhibits the CSE activity in cells rather than cystathionine beta-synthase (CBS), the other H2S-generating enzyme. Moreover, NSC4056 effectively rescues hypotension in hemorrhagic shock rats. |
| WOS关键词 | HYDROGEN-SULFIDE ; AURINTRICARBOXYLIC ACID ; ASSAY ; INFLAMMATION ; MODULATION ; MEDIATOR |
| 资助项目 | National Natural Science Foundation[31500635] ; National Natural Science Foundation[31870763] ; National Natural Science Foundation[21834005] ; National Natural Science Foundation[81620108027] ; National Natural Science Foundation[21632008] ; Research Fund for Young Scientist of Shanghai Jiao Tong University[15X100040050] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000459223600038 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290476]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Yu, Jing; Liu, Hong; Wu, Fang |
| 作者单位 | 1.Jiangxi Univ Tradit Chinese Med, Sci & Technol Coll, Nanchang 330004, Jiangxi, Peoples R China 2.Shanghai Jiao Tong Univ, Shanghai Ctr Syst Biomed, Minist Educ, Key Lab Syst Biomed, Shanghai 200240, Peoples R China 3.Shanghai Jiao Tong Univ, Sch Life Sci & Biotechnol, Inst Mechanobiol & Med Engn, Shanghai 200240, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Materia Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 5.Chinese Acad Sci, Shanghai Inst Materia Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 6.Shanghai Jiao Tong Univ, Sch Life Sci & Biotechnol, Sheng Yushou Ctr Cell Biol & Immunol, State Key Lab Microbial Metab, Shanghai 200240, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hu, Youtian,Wang, Lu,Han, Xu,et al. Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine gamma-Lyase[J]. JOURNAL OF MEDICINAL CHEMISTRY,2019,62(3):1677-1683. |
| APA | Hu, Youtian.,Wang, Lu.,Han, Xu.,Zhou, Yueyang.,Zhang, Tonghui.,...&Wu, Fang.(2019).Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine gamma-Lyase.JOURNAL OF MEDICINAL CHEMISTRY,62(3),1677-1683. |
| MLA | Hu, Youtian,et al."Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine gamma-Lyase".JOURNAL OF MEDICINAL CHEMISTRY 62.3(2019):1677-1683. |
入库方式： OAI收割
来源：上海药物研究所
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