Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae

doi:10.1021/jm0300532

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 国家新药筛选中心

	Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae
	Luo, QL ; Li, JY; Liu, ZY ; Chen, LL ; Li, J; Qian, Z ; Shen, Q ; Li, Y; Lushington, GH ; Ye, QZ
刊名	JOURNAL OF MEDICINAL CHEMISTRY
	2003-06-19
卷号	46 期号:13 页码:2631-2640
ISSN号	0022-2623
DOI	10.1021/jm0300532
文献子类	Article
英文摘要	A series of pyridine-2-carboxylic acid derivatives were synthesized according to the leads from the screening, and potent inhibitors have been obtained by structural modification. They have shown submicromolar inhibition of the enzymes (for example, for 9n, IC50 = 130 nM for EcMetAP1 and IC50 = 380 nM for ScMetAP1). They represent small-molecule MetAP inhibitors with novel structures different from alkylating fumagillin derivatives and peptidic bestatin-based MetAP inhibitor.
资助项目	NCRR NIH HHS[1 P20 RR15563]
WOS关键词	YEAST ; PROTEINS ; GENE
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000183511500010
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274217]
专题	国家新药筛选中心
通讯作者	Ye, QZ
作者单位	1.Univ Kansas, High Throughput Screening Lab & Mol Graph & Model, Lawrence, KS 66047 USA 2.Lanzhou Univ, Dept Chem, Lanzhou 730000, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Life Sci, Chinese Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Luo, QL,Li, JY,Liu, ZY,et al. Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae[J]. JOURNAL OF MEDICINAL CHEMISTRY,2003,46(13):2631-2640.
APA	Luo, QL.,Li, JY.,Liu, ZY.,Chen, LL.,Li, J.,...&Nan, FJ.(2003).Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae.JOURNAL OF MEDICINAL CHEMISTRY,46(13),2631-2640.
MLA	Luo, QL,et al."Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae".JOURNAL OF MEDICINAL CHEMISTRY 46.13(2003):2631-2640.