Merali Zahra, Ross Stephanie, Paré Guillaume
Drug Metabol Drug Interact. 2014;29(3):143-51. doi: 10.1515/dmdi-2014-0009.
Human carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are serine esterases responsible for the hydrolysis of ester and amide bonds present in a number of pharmaceutical products. Several common genetic variants of the CES1 and CES2 genes have been shown to influence drug metabolism and clinical outcomes. Polymorphisms of the CES1 gene have been reported to affect the metabolism of dabigatran etexilate, methylphenidate, oseltamivir, imidapril, and clopidogrel, whereas variants of the CES2 gene have been found to affect aspirin and irinotecan. Although the findings of these studies may be preliminary, they demonstrate the potential clinical utility of CES polymorphisms; however, more research is required, especially with respect to CES2. In this review, we outline the functional, molecular, and genetic properties of CES1 and CES2, and highlight recent studies that have shown relations between CES1 and CES2 variants and contemporary pharmacotherapy.
人羧酸酯酶1(CES1)和羧酸酯酶2(CES2)是丝氨酸酯酶,负责水解多种药物产品中的酯键和酰胺键。CES1和CES2基因的几种常见基因变异已被证明会影响药物代谢和临床结果。据报道,CES1基因的多态性会影响达比加群酯、哌甲酯、奥司他韦、咪达普利和氯吡格雷的代谢,而CES2基因的变异则被发现会影响阿司匹林和伊立替康。尽管这些研究的结果可能是初步的,但它们证明了CES基因多态性的潜在临床应用价值;然而,还需要更多的研究,特别是关于CES2的研究。在这篇综述中,我们概述了CES1和CES2的功能、分子和遗传特性,并重点介绍了最近显示CES1和CES2变异与当代药物治疗之间关系的研究。