一般描述
羧酸酯酶2人类基因定位于人类染色体16q22.1。
羧酸酯酶属于α/β水解酶折叠家族，参与药物代谢和活化。存在于结肠、肝脏、小肠、心脏、脑和睾丸中。小肠的水解酶活性归因于人的羧酸酯酶2。它在103和267个残基处有两个糖基化位点，分子量为60 kDa。
应用
人的羧酸酯酶2已用于：
- 在体外基于酶的抑制剂筛选测定
- 在以发射比率双光子探针（SE1）的底物选择性测定
- 在各种基于4-硝基苯基和1-萘基的底物的酶测定中作为标准品
具有高催化活性，非常适合用于强大的高通量筛选分析，包括药物间相互作用研究以及用于评估前药和非CYP消除途径的药代动力学研究。
羧酸酯酶2可能在多种含酯药物和前体药物的生物转化中起关键作用。
生化/生理作用
人的羧酸酯酶2确定了含有大醇和小酰基的位点。由于在活性位点存在构象干扰，它显示出较少的酯交换活性。
可水解酯和酰胺键的丝氨酸酯酶家族成员。羧基酯酶2是一种内质网结合的水解酶，在异源生物解毒和活化含酯治疗剂中起关键作用。羧基酯酶2也可参与海洛因和可卡因等药物的解毒过程。该酶被认为在脂质代谢中起作用。
单位定义
一个单位将在37℃、pH 7.4下每分钟从4-硝基苯乙酸酯生产1纳摩尔的4-硝基苯酚。
WGK
nwg
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
常规特殊物品
T Satoh et al.
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S Omedes et al.
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Human liver carboxylesterase. Purification and molecular properties.
W Junge et al.
Archives of biochemistry and biophysics, 165(2), 749-763 (1974-12-01)
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