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

Qun Li Luo, Jing Ya Li, Zhi Ying Liu, Ling Ling Chen, Jia Li, Zhen Qian, Qiang Shen, Yu Li, Gerald H. Lushington, Qi Zhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

59 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)2631-2640
Number of pages10
JournalJournal of Medicinal Chemistry
Volume46
Issue number13
DOIs
StatePublished - Jun 19 2003
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    Luo, Q. L., Li, J. Y., Liu, Z. Y., Chen, L. L., Li, J., Qian, Z., Shen, Q., Li, Y., Lushington, G. H., Ye, Q. Z., & Nan, F. J. (2003). Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae. Journal of Medicinal Chemistry, 46(13), 2631-2640. https://doi.org/10.1021/jm0300532