Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine gamma-Lyase

doi:10.1021/acs.jmedchem.8b01720

	Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine gamma-Lyase
	Hu, Youtian 1; Wang, Lu 2; Han, Xu 3,4; Zhou, Yueyang 1; Zhang, Tonghui 1; Wang, Li 1; Hong, Ting 1,5; Zhang, Wei 6; Guo, Xun-Xiang 1; Sun, Jielin 1
刊名	JOURNAL OF MEDICINAL CHEMISTRY
	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.
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关键词	HYDROGEN-SULFIDE ; AURINTRICARBOXYLIC ACID ; ASSAY ; INFLAMMATION ; MODULATION ; MEDIATOR
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000459223600038
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/290476]
专题	中国科学院上海药物研究所
通讯作者	Yu, Jing; Liu, Hong; Wu, Fang
作者单位	1.Shanghai Jiao Tong Univ, Shanghai Ctr Syst Biomed, Minist Educ, Key Lab Syst Biomed, Shanghai 200240, Peoples R China 2.Shanghai Jiao Tong Univ, Sch Life Sci & Biotechnol, Inst Mechanobiol & Med Engn, Shanghai 200240, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Materia Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Materia Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 5.Jiangxi Univ Tradit Chinese Med, Sci & Technol Coll, Nanchang 330004, Jiangxi, 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.