Weinshilboum R M
Fed Proc. 1986 Jul;45(8):2223-8.
Phenol sulfotransferase (PST) catalyzes the sulfate conjugation of phenolic and catechol drugs and neurotransmitters. All human tissues that have been studied in detail contain at least two forms of PST. One form is thermolabile (TL), catalyzes the sulfate conjugation of micromolar concentrations of dopamine and other phenolic monoamines, and is relatively resistant to inhibition by 2,6-dichloro-4-nitrophenol (DCNP). The other form is thermostable (TS), catalyzes the sulfate conjugation of micromolar concentrations of simple phenols such as p-nitrophenol, and is relatively sensitive to DCNP inhibition. These two forms of PST have been physically separated and partially purified from several human tissues, including an easily accessible tissue, the blood platelet. The biochemical properties of platelet PST are very similar to those of PST in human brain, liver, and small intestine. Individual differences in the basal activity of TS PST in the platelet are correlated with individual variations in the activity of this form of the enzyme in human cerebral cortex (r = .94, n = 15, P less than 0.001). In addition, both platelet TS and TL PST activities are correlated significantly with the extent of sulfate conjugation of orally administered drugs such as acetaminophen and methyldopa. These latter observations are compatible with the conclusions that platelet PST activity may reflect the activity of the enzyme at sites of drug metabolism, and that variation in PST activity is one factor responsible for individual differences in the sulfate conjugation of orally administered drugs.
酚磺基转移酶（PST）催化酚类和儿茶酚类药物及神经递质的硫酸结合反应。所有经过详细研究的人体组织都至少含有两种形式的PST。一种形式是热不稳定型（TL），催化微摩尔浓度的多巴胺和其他酚类单胺的硫酸结合反应，并且相对不易受到2,6 - 二氯 - 4 - 硝基苯酚（DCNP）的抑制。另一种形式是热稳定型（TS），催化微摩尔浓度的简单酚类如对硝基苯酚的硫酸结合反应，并且相对容易受到DCNP的抑制。这两种形式的PST已从包括易于获取的组织血小板在内的多种人体组织中进行了物理分离和部分纯化。血小板PST的生化特性与人类大脑、肝脏和小肠中的PST非常相似。血小板中TS PST基础活性的个体差异与人类大脑皮层中这种酶形式的活性个体差异相关（r = 0.94，n = 15，P < 0.001）。此外，血小板TS和TL PST活性均与口服药物如对乙酰氨基酚和甲基多巴的硫酸结合程度显著相关。这些后期观察结果与以下结论一致：血小板PST活性可能反映药物代谢部位的酶活性，并且PST活性的变化是导致口服药物硫酸结合个体差异的一个因素。
