Chatelain P, Robberecht P, Waelbroeck M, Camus J C, Christophe J
J Membr Biol. 1986;93(1):23-32. doi: 10.1007/BF01871015.
n-Alkanols (from methanol to decanol) have a biphasic effect on rat cardiac adenylate cyclase either basal or stimulated by GTP, GppNHp, NaF or hormones (isoproterenol, glucagon, secretin) in the presence of GTP. At high concentration, all the enzyme activities are inhibited. At low concentration, adenylate cyclase activity is either unchanged or potentiated depending on both the stimulus and the alkanols involved. Potentiation is due to an increase of maximum velocity with no change in the activation constant of the enzyme. Basal activity is unchanged as well as the isoproterenol- and glucagon-stimulated enzyme. The secretin-stimulated enzyme is potentiated. It is the guanyl nucleotide regulatory protein-mediated stimulation of adenylate cyclase which is mainly affected. An attempt was made to relate these effects on adenylate cyclase with physical parameters of the alkanols (partition coefficient). From the data obtained as a function of the alkanol chain-length and of temperature on the adenylate cyclase stimulated by GTP, GppNHp, NaF and permanently activated, it is concluded that the increase in efficacy observed in the presence of alkanol is due to an interaction with the protein moeity particularly with the guanyl nucleotide regulatory protein.
正构烷醇(从甲醇到癸醇)对大鼠心脏腺苷酸环化酶有双相作用,无论是基础状态下的还是在GTP、GppNHp、NaF或激素(异丙肾上腺素、胰高血糖素、促胰液素)存在时由GTP刺激的腺苷酸环化酶。在高浓度时,所有酶活性均被抑制。在低浓度时,腺苷酸环化酶活性要么不变要么增强,这取决于所涉及的刺激因素和烷醇。增强是由于最大速度增加而酶的活化常数不变。基础活性以及异丙肾上腺素和胰高血糖素刺激的酶活性不变。促胰液素刺激的酶活性增强。主要受影响的是鸟苷酸调节蛋白介导的腺苷酸环化酶刺激作用。有人试图将这些对腺苷酸环化酶的作用与烷醇的物理参数(分配系数)联系起来。根据在不同链长的烷醇和温度条件下对由GTP、GppNHp、NaF刺激及永久激活的腺苷酸环化酶所获得的数据得出结论,在烷醇存在下观察到的效力增加是由于与蛋白质部分尤其是与鸟苷酸调节蛋白的相互作用。