Inhibition of Na,K‐ATPase by a new ATP analog, adenosine‐5‐N′‐(2,4‐dinitro‐5‐fluorophenyl)phosphohydrazide

FEBS Letters

Skačkova, Dagmar²  Khropov, Yuri¹  Buranova, Ludmila³  Lopina, Olga³ 

[1] Department of Biochemistry, Moscow State University, Moscow, USSR;Department of Biophysics, J. Komenski University, Bratislava, Czechoslovakia;Institute of Biochemistry, USSR Academy of Sciences, Moscow, USSR

关键词: Na;    K-ATPase;    ATP analog;    Irreversible inhibition;    DNPH-AMP;    adenosine-5-N′-(2;    4-dinitro-5-fluorophenyl) phosphohydrazide;    MOPS;    N-morpholinopropanesulfonic acid;    NBS6ITP;    6-[(3-carboxy-4-nitrophenyl)thiol]-9-β-D-ribifuranosylpurine triphosphate;   

DOI  :  10.1016/0014-5793(91)80483-J

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A new ATP analog, adenosine-5-N′-(2,4-dinitro-5-fluorophenyl) phosphohydrazide (DNPH-AMP), has been synthesized, which is an irreversible inhibitor of Na,K-ATPase. Interaction of the analog with the enzyme in the presence or K⁺ is describe by the scheme:, and corresponding kinetic constant k₃ and K_i are found equal to 2.5 min⁻¹ and 1.6 mM. In the presence of Na⁺ the time course enzyme inactivation by DNPH-AMP is a biphasic curve in the semilogarithmic plot, The k₃ and K_i values calculated for this case according to Fritzsch (Fritzch (1985) J. Theor. biol, 117 397) are equal to 2.45 min⁻¹ and 2.5 mM, respectively. ATP transforms the K* -type or Na,K-ATPase inactivation into the one that takes place in the presence of Na*.

【 授权许可】

Unknown