Inhibition of eukaryotic ribonuclease P activity by aminoglycosides: kinetic studies

FEBS Letters

Stathopoulos, Constantinos¹  Tekos, Apostolos¹  Drainas, Denis¹  Tsagla, Antigoni¹ 

[1] Department of Biochemistry, School of Medicine, University of Patras, 26500 Patras, Greece

关键词: RNase P;    Ribozyme;    Antibiotic;   

DOI  :  10.1016/S0014-5793(00)02190-6

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The effect of several aminoglycoside antibiotics on ribonuclease P (RNase P) was investigated using an in vitro experimental system from Dictyostelium discoideum. Detailed kinetic analysis showed that all aminoglycosides tested (tobramycin, gentamicin, kanamycin, paromomycin, neomycin) behave as classical non-competitive inhibitors, with neomycin being the strongest inhibitor. The inhibition effect is attributed to the electrostatic competition of the cationic aminoglycosides with magnesium ions required for catalysis. Increasing Mg²⁺ ion concentrations reduced the effect of aminoglycosides on RNase P activity. Detailed kinetic analysis showed that aminoglycosides compete with Mg²⁺ for common binding sites on RNase P holoenzyme.

【 授权许可】

Unknown