Van Loon J, Weinshilboum R M
Biochem Genet. 1984 Dec;22(11-12):997-1014. doi: 10.1007/BF00499627.
Phenol sulfotransferase (PST) catalyzes the sulfate conjugation of catechol and phenolic drugs and xenobiotic compounds. Platelets and other tissues contain at least two forms of PST, forms that have been designated the "TL" and the "TS" forms. We measured the thermal stability of platelet TS PST in blood samples from 218 randomly selected unrelated subjects by heating platelet homogenates at 44 degrees C for 15 min. Thermal stability was expressed as the ratio of the enzyme activity remaining after preincubation to that in an unheated sample, a heated/control (H/C) ratio. The frequency distribution of H/C ratios for this population sample was bimodal, with a nadir at an H/C ratio of 0.33. Of the 218 subjects studied, 29 (13.3%) had thermolabile TS PST (H/C less than 0.33). Platelet samples were then obtained from subjects with thermolabile and thermostable TS platelet PST. PST activity in these platelet samples had similar apparent Km constants for substrates. IC50 values for inhibition of TS PST by 2,6-dichloro-4-nitrophenol in these samples were also nearly identical. The results of experiments in which platelet homogenates from subjects with thermolabile and thermostable TS PST were mixed and the results of experiments in which platelet homogenates were subjected to gel filtration chromatography were compatible with the conclusion that individual differences in TS PST thermal stability were properties of PST itself. Finally, there was a significant familial aggregation of the trait of thermolabile TS PST when H/C ratios were measured in platelet homogenates from 231 members of 49 randomly selected families.
苯酚磺基转移酶(PST)催化儿茶酚、酚类药物及外源性化合物的硫酸结合反应。血小板和其他组织至少含有两种形式的PST,即已被命名为“TL”和“TS”的形式。我们通过将血小板匀浆在44℃加热15分钟,测定了218名随机选取的无亲缘关系受试者血液样本中血小板TS PST的热稳定性。热稳定性用预温育后剩余的酶活性与未加热样本中酶活性的比值来表示,即加热/对照(H/C)比值。该群体样本的H/C比值频率分布呈双峰型,在H/C比值为0.33时出现最低点。在研究的218名受试者中,29名(13.3%)具有热不稳定的TS PST(H/C小于0.33)。随后从具有热不稳定和热稳定TS血小板PST的受试者中获取血小板样本。这些血小板样本中PST活性对底物的表观Km常数相似。在这些样本中,2,6 - 二氯 - 4 - 硝基苯酚抑制TS PST的IC50值也几乎相同。将热不稳定和热稳定TS PST受试者的血小板匀浆混合进行实验的结果,以及对血小板匀浆进行凝胶过滤色谱实验的结果,均与以下结论相符:TS PST热稳定性的个体差异是PST自身的特性。最后,当对49个随机选取家庭的231名成员的血小板匀浆测量H/C比值时,热不稳定TS PST这一性状存在显著的家族聚集性。