酯酶的药物代谢与种属差异研究进展

Research Progress of Esterases in Drug Metabolism and Species Difference

羧酸酯酶(CES)、芳基乙酰胺脱乙酰酶(AADAC)、丁酰胆碱酯酶(BCHE)和对氧磷酶(PON)是人体内重要的酯酶,参与药物在体内的代谢、活化解毒,在前药的设计中也起到非常重要的作用。围绕人体内广泛参与药物代谢的酯酶,对其在体内的组织分布、底物和抑制剂的特异性及种属差异研究进展进行综述,为临床前动物模型选择、新药的设计和开发提供参考。

Carboxylesterase,arylacetamide deacetylase,butyrylcholinesterase,paraoxonase are important esterases in the human body,participating in the metabolism,activation and detoxification of drugs in the body,thus with a very important role in the design of prodrugs.This paper focuses on the esterases that are widely involved in drug metabolism in human body,and summarizes their tissue distribution in vivo,substrate and inhibitor and species differences,aiming to provide reference for preclinical selection of animal models,drugs design and development of new drugs.