7-羟基托酚酮：一种氨基糖苷-2″-O-腺苷酰转移酶抑制剂。
7-Hydroxytropolone: an inhibitor of aminoglycoside-2"-O-adenylyltransferase.
作者信息
Allen N E, Alborn W E, Hobbs J N, Kirst H A
出版信息
Antimicrob Agents Chemother. 1982 Nov;22(5):824-31. doi: 10.1128/AAC.22.5.824.
Abstract
Aminoglycoside-2"-O-adenylyltransferase was inhibited by 7-hydroxytropolone. Inhibition was competitive with respect to the cosubstrate ATP and appeared to require the unique vicinal arrangement of oxygens found in 7-hydroxytropolone. Combinations of 7-hydroxytropolone plus the appropriate aminoglycoside substrates were active against resistant bacteria possessing the adenylyltransferase. No potentiation was observed against other aminoglycoside-resistant or -susceptible strains. The fact that the inhibition of an aminoglycoside-modifying enzyme overcomes the poor uptake of aminoglycosides in resistant strains points to the singular importance of the inactivating enzyme as a determinant of resistance.
摘要
7-羟基托酚酮可抑制氨基糖苷-2″-O-腺苷酰转移酶。这种抑制作用对共底物ATP而言是竞争性的，并且似乎需要7-羟基托酚酮中独特的邻位氧排列。7-羟基托酚酮与合适的氨基糖苷底物组合对携带腺苷酰转移酶的耐药菌具有活性。未观察到对其他氨基糖苷耐药或敏感菌株有增效作用。氨基糖苷修饰酶的抑制克服了耐药菌株中氨基糖苷摄取不良这一事实，表明失活酶作为耐药决定因素具有独特的重要性。
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Letter: Kanamycin phosphotransferase. I. Mechanism of cross resistance between kanamycin and lividomycin.信函：卡那霉素磷酸转移酶。I. 卡那霉素与青紫霉素之间的交叉耐药机制。
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