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, Qizhuang Ye, Fa Jun Nan

Research output: Contribution to journalArticle

57 Citations (Scopus)

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

Fingerprint

Aminopeptidases
Methionine
Yeast
Escherichia coli
Inhibitory Concentration 50
Saccharomyces cerevisiae
Derivatives
Screening
Molecules
Enzymes
picolinic acid
fumagillin
ubenimex

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae. / Luo, Qun Li; Li, Jing Ya; Liu, Zhi Ying; Chen, Ling Ling; Li, Jia; Qian, Zhen; Shen, Qiang; Li, Yu; Lushington, Gerald H.; Ye, Qizhuang; Nan, Fa Jun.

In: Journal of Medicinal Chemistry, Vol. 46, No. 13, 19.06.2003, p. 2631-2640.

Research output: Contribution to journalArticle

Luo, QL, Li, JY, Liu, ZY, Chen, LL, Li, J, Qian, Z, Shen, Q, Li, Y, Lushington, GH, Ye, Q & Nan, FJ 2003, 'Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae', Journal of Medicinal Chemistry, vol. 46, no. 13, pp. 2631-2640. https://doi.org/10.1021/jm0300532
Luo, Qun Li ; Li, Jing Ya ; Liu, Zhi Ying ; Chen, Ling Ling ; Li, Jia ; Qian, Zhen ; Shen, Qiang ; Li, Yu ; Lushington, Gerald H. ; Ye, Qizhuang ; Nan, Fa Jun. / Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae. In: Journal of Medicinal Chemistry. 2003 ; Vol. 46, No. 13. pp. 2631-2640.
@article{25ffd5d01358456aaf993c37300ea518,
title = "Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae",
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.",
author = "Luo, {Qun Li} and Li, {Jing Ya} and Liu, {Zhi Ying} and Chen, {Ling Ling} and Jia Li and Zhen Qian and Qiang Shen and Yu Li and Lushington, {Gerald H.} and Qizhuang Ye and Nan, {Fa Jun}",
year = "2003",
month = "6",
day = "19",
doi = "10.1021/jm0300532",
language = "English (US)",
volume = "46",
pages = "2631--2640",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "13",

}

TY - JOUR

T1 - Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae

AU - Luo, Qun Li

AU - Li, Jing Ya

AU - Liu, Zhi Ying

AU - Chen, Ling Ling

AU - Li, Jia

AU - Qian, Zhen

AU - Shen, Qiang

AU - Li, Yu

AU - Lushington, Gerald H.

AU - Ye, Qizhuang

AU - Nan, Fa Jun

PY - 2003/6/19

Y1 - 2003/6/19

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0038792294&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0038792294&partnerID=8YFLogxK

U2 - 10.1021/jm0300532

DO - 10.1021/jm0300532

M3 - Article

VL - 46

SP - 2631

EP - 2640

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 13

ER -