羧酸酯酶单核苷酸多态性与个体化药物治疗的研究进展

Research progress in carboxylesterases single nucleotide polymorphism and individualized drug therapy

人类羧酸酯酶(carboxylesterases,CESs)属于丝氨酸酯酶超家族,在人体中主要包含羧酸酯酶1(CES1)和2(CES2)2种亚型。CES负责多种药物的代谢,如部分血小板凝集抑制剂、精神兴奋剂、抗肿瘤药等,由于CES的单核苷酸多态性(SNP)在人类基因组中广泛存在,其对药物代谢酶基因的表达和(或)酶活性的高低有着重要影响,从而最终影响着药物在体内的代谢过程。本文综述了CES1和CES2相关SNP所致酶活性的改变,以及由于其多态性导致代谢药物体内过程改变的相关药物基因组学研究,以期为临床治疗和研究提供参考。

Human carboxylesterases （CESs） belong to serine esterases super family. CES1 and CES2 are the two major subtypes in the human body. CES is responsible for the metabolism of a variety of drugs metabolism, such as part of the platelet aggregation inhibitors, mental stimulant drugs, antitumor drugs, and so on. Since CES single nucleotide polymorphism （SNP） is wide-spread in the human genome, and plays an important role in the expression and activity of drug metabolic enzyme, and ultimately affects the drug metabolic process, this review mainly discussed the change of enzyme activity due to CES1 and CES2 SNPs, and summarized the progress in pharmacogenomics studies, and hope to will provide useful reference for clinical treatment and research.