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Bioorg Med Chem Lett. 2000 Nov 6;10(21):2441-4.

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

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  • 1Département de Chimie, Centre de Recherche sur la Fonction, la Structure et l'Ingénierie des Protéines (CREFSIP), Faculté des Sciences et de Génie, Université Laval, Québec, Canada.


Glutaminol adenylate 5 is a competitive inhibitor of glutaminyl-tRNA synthetase with respect to glutamine (Ki = 280 nM) and to ATP (Ki = 860 nM). The corresponding methyl phosphate ester 4 is a weaker inhibitor (Ki approximately 10 microM) with respect to glutamine.

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