Veklich T O, Shkrabak O A, Rodik R V, Kal'chenko V I, Kosterin S O
Ukr Biokhim Zh (1999). 2011 Mar-Apr;83(2):36-44.
The inhibitory action of calixarene C-107 (5,17-diamino(2-pyridyl)methylphosphono- 11,23-di-tret-butyl-26,28-dihydroxy-25,27-dipropoxy-calix[4]arene) on Na+, K(+)-ATPase activity kinetic properties of myometrium perforated plasma membrane was investigated. It has been shown that the calixarene C-107 inhibiting Na+, K(+)-ATPase does not change the kinetic parameters (Km, nH) of reaction velocity dependence on substrate concentration. The constant Ka of enzyme activation by MgCl2 has complex dependence on calixarene C-107 concentration: it increases twice with growth of calixarene concentration up to 50 nM and decreases to the control level with further growth of calixarene concentration. The Hill cooperativity coefficient nH of activation by MgCl2 does not vary in the presence of calixarene C-107. Both ATP and MgCl2 have no influence on Na+, K(+)-ATPase constant of inhibition by calixarene C-107, but an increase of concentration of the mentioned physiological compounds causes the growth of cooperativity coefficient nH of enzymatic reaction inhibition by calixaren C-107.
研究了杯芳烃C-107（5,17-二氨基（2-吡啶基）甲基膦酰基-11,23-二叔丁基-26,28-二羟基-25,27-二丙氧基杯[4]芳烃）对子宫肌层穿孔质膜Na +，K（+）-ATP酶活性动力学特性的抑制作用。结果表明，抑制Na +，K（+）-ATP酶的杯芳烃C-107不会改变反应速度对底物浓度的动力学参数（Km，nH）。MgCl2对酶的激活常数Ka对杯芳烃C-107浓度具有复杂的依赖性：随着杯芳烃浓度增加至50 nM，其增加两倍，而随着杯芳烃浓度进一步增加，其降低至对照水平。在存在杯芳烃C-107的情况下，MgCl2激活的希尔协同系数nH不变。ATP和MgCl2对杯芳烃C-107抑制Na +，K（+）-ATP酶的常数均无影响，但上述生理化合物浓度的增加会导致杯芳烃C-107对酶促反应抑制的协同系数nH增加。
