Brestkin A P, Zhukovskiĭ Iu G, Rozengart E V
Ukr Biokhim Zh (1978). 1987 Sep-Oct;59(5):77-81.
Determination of inhibitory constants and antienzymic activity of reversible retardants of different type of action by the generalized inhibitory constant K sigma is estimated, results being presented. To determine more precisely the values of inhibitory constants of the competitive (Ki), noncompetitive (K'i) inhibition and of the generalized K sigma it is suggested to conduct linearization of the experimental data in coordinates: 1/K sigma, s; 1/[S], where K sigma, s is a total inhibitory constant whose value depends on the substrate [S] concentration and to make calculations by the least-square method with the allowance for principal intervals of the Km values and the maximal rate of the enzymic reaction V. Comparative calculations are made by a computer using the BASIC/RT-60 language programme through the example of the acetyl choline acetyl hydrolase (EC 3.1.1.7) interaction with the quaternary phosphonium salts--reversible retardants of this enzyme.
通过广义抑制常数(K_{\sigma})估算不同作用类型的可逆抑制剂的抑制常数及抗酶活性,并给出结果。为更精确地确定竞争性抑制((K_{i}))、非竞争性抑制((K_{i}'))的抑制常数以及广义抑制常数(K_{\sigma})的值,建议对实验数据进行坐标线性化:(1/K_{\sigma}),(s);(1/[S]),其中(K_{\sigma}),(s)是总抑制常数,其值取决于底物([S])浓度,并采用最小二乘法进行计算,同时考虑(K_{m})值的主要区间和酶促反应的最大速率(V)。以乙酰胆碱乙酰水解酶(EC 3.1.1.7)与季鏻盐(该酶的可逆抑制剂)的相互作用为例,使用BASIC/RT - 60语言程序通过计算机进行比较计算。