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甲硫氨酰腺苷酸类似物作为甲硫氨酰 - tRNA合成酶的抑制剂

Methionyl adenylate analogues as inhibitors of methionyl-tRNA synthetase.

作者信息

Lee J, Kang S U, Kang M K, Chun M W, Jo Y J, Kwak J H, Kim S

机构信息

Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Korea.

出版信息

Bioorg Med Chem Lett. 1999 May 17;9(10):1365-70. doi: 10.1016/s0960-894x(99)00206-1.

DOI:10.1016/s0960-894x(99)00206-1
PMID:10360737
Abstract

Four stable analogues of methionyl adenylate (3-6) were designed as inhibitors of methionyl-tRNA synthetase and synthesized from 2',3'-isopropylideneadenosine. They strongly inhibited aminoacylation activity of methionyl-tRNA synthetases isolated from Escherichia coli, Mycobacterium tuberculosis, Saccharomyces cerevisiae and human. Among the microorganisms tested, however, these chemicals showed the growth inhibition effect only on E. coli.

摘要

设计了四种稳定的甲硫氨酰腺苷类似物(3-6)作为甲硫氨酰-tRNA合成酶的抑制剂,并由2',3'-异丙叉腺苷合成。它们强烈抑制从大肠杆菌、结核分枝杆菌、酿酒酵母和人类中分离出的甲硫氨酰-tRNA合成酶的氨酰化活性。然而,在所测试的微生物中,这些化学物质仅对大肠杆菌显示出生长抑制作用。

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