Synthesis of glutaminyl adenylate analogues that are inhibitors of glutaminyl-tRNA synthetase

被引：22

作者：

Bernier, S ^{[1
]}

Dubois, DY ^{[1
]}

Therrien, M ^{[1
]}

Lapointe, J ^{[1
]}

Chênevert, R ^{[1
]}

机构：

[1] Univ Laval, Fac Sci & Genie, Ctr Rech Fonct Struct & Ingn Prot, CREFSIP,Dept Biochim & Microbiol,Dept Chim, Laval, PQ G1K 7P4, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 21期

基金：

加拿大自然科学与工程研究理事会;

关键词：

D O I：

10.1016/S0960-894X(00)00478-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Glutaminol adenylate 5 is a competitive inhibitor of glutaminyl-tRNA synthetase with respect to glutamine (k(i),= 280 nM) and to ATP (K-i = 860 nM). The corresponding methyl phosphate ester 4 is a weaker inhibitor (K(i)similar to 10 muM) with respect to glutamine. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2441 / 2444

页数：4

共 26 条

[21] Characterization of isoleucyl-tRNA synthetase from Staphylococcus aureus -: I:: Kinetic mechanism of the substrate activation reaction studied by transient and steady-state techniques [J].