Miliutin A A, Okun' I M, Aksentsev S L, Arinchin N I, Konev S V
Biofizika. 1976 Nov;21(6):1120-2.
d-tubocurarine and procaine have been shown to inhibit the acetylcholinesterase of rat brain homogenate by coupled and non-competitive mechanism respectively, which suggests binding to enzyme peripheral sites. Judging by values of Hill coefficient negative cooperativity in interactions between procaine sites is characteristic of all ages (n=0,8 and 0,53 for young and old rats) while such cooperativity for d-tubocurarine sites appears only at old age (n=1 and 0,6 for young and old animals). Values of Ki changed in opposite directions for each of the substances with aging. Modification of the enzyme membrane microenvironment with aging was suggested as a reason for differences in enzyme allosteric behaviour.
已证明筒箭毒碱和普鲁卡因分别通过偶联和非竞争性机制抑制大鼠脑匀浆的乙酰胆碱酯酶，这表明它们与酶的外周位点结合。从希尔系数值判断，普鲁卡因位点之间相互作用的负协同性在所有年龄段均有特征（幼鼠和老年大鼠分别为n = 0.8和0.53），而筒箭毒碱位点的这种协同性仅在老年时出现（幼龄和老龄动物分别为n = 1和0.6）。随着衰老，每种物质的Ki值朝相反方向变化。衰老导致的酶膜微环境改变被认为是酶变构行为差异的原因。
