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

Authors
Bernier, S Dubois, DY Therrien, M Lapointe, J Chenevert, R
Citation
S. Bernier et al., Synthesis of glutaminyl adenylate analogues that are inhibitors of glutaminyl-tRNA synthetase, BIOORG MED, 10(21), 2000, pp. 2441-2444
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
21
Year of publication
2000
Pages
2441 - 2444
Database
ISI
SICI code
0960-894X(20001106)10:21<2441:SOGAAT>2.0.ZU;2-O
Abstract
Glutaminol adenylate 5 is a competitive inhibitor of glutaminyl-tRNA synthe tase with respect to glutamine (k(i),= 280 nM) and to ATP (K-i = 860 nM). T he corresponding methyl phosphate ester 4 is a weaker inhibitor (K(i)simila r to 10 muM) with respect to glutamine. (C) 2000 Elsevier Science Ltd. All rights reserved.