Paper
7-Hydroxytropolone: an inhibitor of aminoglycoside-2"-O-adenylyltransferase
Published Nov 1, 1982 · N. E. Allen, W. Alborn, J. N. Hobbs
Antimicrobial Agents and Chemotherapy
62
Citations
2
Influential Citations
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.
7-hydroxytropolone effectively inhibits aminoglycoside-2"-O-adenylyltransferase, enabling the uptake of aminoglycosides in resistant bacteria, emphasizing the importance of this enzyme in resistance determinants.
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