Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae | |
Luo, QL; Li, JY![]() ![]() ![]() | |
刊名 | JOURNAL OF MEDICINAL CHEMISTRY
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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. |
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