Different inhibitory effects in rat and human carboxylesterases

S Takahashi, M Katoh, T Saitoh, M Nakajima… - Drug metabolism and …, 2009 - ASPET
In vitro inhibition studies on drug-metabolizing enzyme activity are useful for understanding
drug-drug interactions and for drug development. However, the profile of the inhibitory …

Allosteric kinetics of human carboxylesterase 1: species differences and interindividual variability

S Takahashi, M Katoh, T Saitoh, M Nakajima… - Journal of …, 2008 - Elsevier
Esterified drugs such as imidapril, derapril, and oxybutynin hydrolyzed by carboxylesterase
1 (CES1) are extensively used in clinical practice. The kinetics using the CES1 substrates …

[HTML][HTML] In vitro evaluation of the inhibitory potential of pharmaceutical excipients on human carboxylesterase 1A and 2

C Zhang, Y Xu, Q Zhong, X Li, P Gao, C Feng, Q Chu… - Plos one, 2014 - journals.plos.org
Two major forms of human carboxylesterase (CES), CES1A and CES2, dominate the
pharmacokinetics of most prodrugs such as imidapril and irinotecan (CPT-11). Excipients …

Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro

X Yanjiao, Z Chengliang, L Xiping, W Tao… - Drug Metabolism and …, 2013 - Elsevier
Human carboxylesterase (CES) 1A and CES2, two major forms of human CES, dominate the
pharmacokinetics of most prodrugs such as imidapril and irinotecan (CPT-11) …

Regulations of xenobiotics and endobiotics on carboxylesterases: a comprehensive review

Y Xu, C Zhang, W He, D Liu - European journal of drug metabolism and …, 2016 - Springer
Carboxylesterases (CESs) play major roles in catalyzing the hydrolysis of a wide range of
ester-and amide-containing compounds. CESs dominate both the biotransformation of …

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 …

Effects of steric hindrance and electron density of ester prodrugs on controlling the metabolic activation by human carboxylesterase

M Takahashi, I Hirota, T Nakano, T Kotani… - Drug metabolism and …, 2021 - Elsevier
Carboxylesterase (CES) plays an important role in the hydrolysis metabolism of ester–type
drugs and prodrugs. In this study, we investigated the change in the hydrolysis rate of hCE1 …

Strain and sex differences in drug hydrolase activities in rodent livers

F Kisui, T Fukami, M Nakano, M Nakajima - European Journal of …, 2020 - Elsevier
Abstract Carboxylesterase (CES) 1, CES2, and arylacetamide deacetylase (AADAC) are the
major drug hydrolases in humans, and they have different substrate preferences. Because …

Identification of di-(2-ethylhexyl) phthalate-induced carboxylesterase 1 in C57BL/6 mouse liver microsomes: purification, cDNA cloning, and baculovirus-mediated …

T Furihata, M Hosokawa, N Koyano, T Nakamura… - Drug metabolism and …, 2004 - ASPET
Several mouse carboxylesterase (CES) isozymes have been identified, but information
about their roles in drug metabolism is limited. In this study, we purified and characterized a …

Human carboxylesterase isozymes: catalytic properties and rational drug design

T Imai - Drug metabolism and pharmacokinetics, 2006 - jstage.jst.go.jp
Human carboxylesterase 1 (hCE-1, CES1A1, HU1) and carboxylesterase 2 (hCE-2, hiCE,
HU3) are a serine esterase involved in both drug metabolism and activation. Although both …