Down-regulation of carboxylesterases 1 and 2 plays an important role in prodrug metabolism in immunological liver injury rats

C Zhang, Y Xu, P Gao, J Lu, X Li, D Liu - International …, 2015 - Elsevier
Liver plays a central role in xenobiotics metabolism, thus affecting the in vivo disposition and
therapeutic effects of drugs. Carboxylesterases (CESs), with the main isoforms CES1 and …

Distinct patterns of aging effects on the expression and activity of carboxylesterases in rat liver and intestine

K Ohura, K Tasaka, M Hashimoto, T Imai - Drug Metabolism and Disposition, 2014 - ASPET
The age-associated alteration in expression levels of carboxylesterases (CESs) can affect
both intestinal and hepatic first-pass metabolism after oral administration of xenobiotic esters …

Identification of carboxylesterases expressed in rat intestine and effects of their hydrolyzing activity in predicting first-pass metabolism of ester prodrugs

L Dong, G Jing, Z Chengliang, R Xiuhua… - Die Pharmazie-An …, 2011 - ingentaconnect.com
Carboxylesterases (CESs) located in the intestine play an unique role in the absorption of
many drugs especially ester prodrugs. In order to determine the expression and hydrolyzing …

Analysis of carboxylesterase 2 transcript variants in cynomolgus macaque liver

Y Uno, Y Igawa, M Tanaka, K Ohura, M Hosokawa… - Xenobiotica, 2019 - Taylor & Francis
Carboxylesterase (CES) is important for the detoxification of a wide range of drugs and
xenobiotics. In this study, the hepatic level of CES2 mRNA was examined in cynomolgus …

Lipopolysaccharide down-regulates carbolesterases 1 and 2 and reduces hydrolysis activity in vitro and in vivo via p38MAPK–NF-κB pathway

Z Mao, Y Li, Y Peng, X Luan, H Gui, X Feng, G Hu… - Toxicology letters, 2011 - Elsevier
Carboxylesterases constitute a class of enzymes that hydrolyze drugs containing such
functional groups as carboxylic acid ester, amide, and thioester. Hydrolysis of many drugs is …

Natural products as modulators of CES1 activity

Y Qian, JS Markowitz - Drug Metabolism and Disposition, 2020 - ASPET
Carboxylesterase (CES) 1 is the predominant esterase expressed in the human liver and is
capable of catalyzing the hydrolysis of a wide range of therapeutic agents, toxins, and …

Simultaneous absolute protein quantification of carboxylesterases 1 and 2 in human liver tissue fractions using liquid chromatography-tandem mass spectrometry

Y Sato, A Miyashita, T Iwatsubo, T Usui - Drug Metabolism and Disposition, 2012 - ASPET
The aims of this study were to develop a robust method for simultaneous quantification of
carboxylesterases (CESs) 1 and 2 and to quantify those absolute protein levels in human …

Characterization of recombinant human carboxylesterases: fluorescein diacetate as a probe substrate for human carboxylesterase 2

J Wang, ET Williams, J Bourgea, YN Wong… - Drug Metabolism and …, 2011 - ASPET
Human carboxylesterase (CES) 1 and CES2 are members of the serine hydrolase
superfamily, and both exhibit broad substrate specificity and are involved in xenobiotic and …

Age-and sex-related expression and activity of carboxylesterase 1 and 2 in mouse and human liver

HJ Zhu, DI Appel, Y Jiang, JS Markowitz - Drug metabolism and disposition, 2009 - ASPET
Carboxylesterase (CES) 1 and CES2 are two major hepatic hydrolases responsible for the
metabolism of numerous endogenous and exogenous compounds. In this study, age-and …

Transcription factor-mediated regulation of carboxylesterase enzymes in livers of mice

Y Zhang, X Cheng, L Aleksunes, CD Klaassen - Drug Metabolism and …, 2012 - ASPET
The induction of drug-metabolizing enzymes by chemicals is one of the major reasons for
drug-drug interactions. In the present study, the regulation of mRNA expression of one …