| ABSTRACT Carboxylesterase (CES) is an important class of phaseⅠdrug metabolizing enzymes. Numerous clinically prescribed anticancer prodrugs, carbamateand pyrethroid insecticides, environmental toxicants, and procarcinogens are substrates for CES. Studies have shown that many members of the nuclear receptor (NR) family are involved in the regulation of human and animal liver and intestines expression and activity of CES. In recent years, by using gene knockout mice and transgenic mouse models, pregnane X receptor protein (PXR, NR1I2) and constitutive androstane receptor protein (CAR, NR1I3) mediated regulation of CES are progressively elucidated, studies on other NR mediated regulation of CES also have a breakthrough. Because NR plays an important role in the regulation of the expression and activity of CES, knowing how NR regulates CES has important implications for drug development and clinical medicine. However，current researches in this area are mostly limited to the rodent models. Knockout mice, humanized mouse models and clinical trials can be used for follow up studies. This review will summarize the current state of knowledge regarding NR mediated regulation of CES in human and animals and highlight their importance in drug metabolism and drug drug interactions. |
