Bioactivity-Guided Discovery of Human Carboxylesterase Inhibitors from the Roots of Paeonia lactiflora

JF Zhang, WC Zhong, YC Li, YQ Song… - Journal of Natural …, 2020 - ACS Publications
In a continuing search for potential inhibitors against human carboxylesterases 1A1 and 2A1
(hCES1A1 and hCES2A1), an EtOAc extract of the roots of Paeonia lactiflora showed strong …

Carboxylesterase activities and protein expression in rabbit and pig ocular tissues

A Hammid, JK Fallon, T Lassila, G Salluce… - Molecular …, 2021 - ACS Publications
Hydrolytic reactions constitute an important pathway of drug metabolism and a significant
route of prodrug activation. Many ophthalmic drugs and prodrugs contain ester groups that …

Carboxylesterases are uniquely expressed among tissues and regulated by nuclear hormone receptors in the mouse

RD Jones, AM Taylor, EY Tong, JJ Repa - Drug Metabolism and Disposition, 2013 - ASPET
Carboxylesterases (CES) are a well recognized, yet incompletely characterized family of
proteins that catalyze neutral lipid hydrolysis. Some CES have well-defined roles in …

The emerging role of human esterases

T Fukami, T Yokoi - Drug metabolism and pharmacokinetics, 2012 - jstage.jst.go.jp
In this review, novel aspects of the role of esterases, which contribute to the metabolism of
10% of therapeutic drugs, are described. Esterases hydrolyze the compounds that contain …

Inhibition of human carboxylesterases by ginsenosides: structure–activity relationships and inhibitory mechanism

ZH Sun, J Chen, YQ Song, TY Dou, LW Zou, DC Hao… - Chinese Medicine, 2019 - Springer
Background Human carboxylesterases (hCES) are key serine hydrolases responsible for
the hydrolysis of a wide range of endogenous and xenobiotic esters. Although it has been …

The impact of human CES1 genetic variation on enzyme activity assessed by ritalinic acid/methylphenidate ratios

C Stage, K Dalhoff, HB Rasmussen… - Basic & clinical …, 2019 - Wiley Online Library
The present clinical trial investigated the impact of selected SNPs in CES1 on the metabolic
activity of the enzyme. For this purpose, we used methylphenidate (MPH) as a …

Mammalian carboxylesterase 3: comparative genomics and proteomics

RS Holmes, LA Cox, JL VandeBerg - Genetica, 2010 - Springer
At least five families of mammalian carboxylesterases (CES) catalyse the hydrolysis or
transesterification of a wide range of drugs and xenobiotics and may also participate in fatty …

Is genetic variability in carboxylesterase-1 and carboxylesterase-2 drug metabolism an important component of personalized medicine?

SC Laizure, RB Parker - Xenobiotica, 2020 - Taylor & Francis
The carboxylesterase drug hydrolysis pathway has been used extensively to improve the
oral availability of drugs under the assumption that the high capacity and low substrate …

[HTML][HTML] Two CES1 gene mutations lead to dysfunctional carboxylesterase 1 activity in man: clinical significance and molecular basis

HJ Zhu, KS Patrick, HJ Yuan, JS Wang… - The American Journal of …, 2008 - cell.com
The human carboxylesterase 1 (CES1) gene encodes for the enzyme carboxylesterase 1, a
serine esterase governing both metabolic deactivation and activation of numerous …

clinical paths for soluble epoxide hydrolase inhibitors

JD Imig, C Morisseau - Frontiers in Pharmacology, 2020 - frontiersin.org
Soluble epoxide hydrolase (sEH) is an enzyme that contributes importantly to metabolism of
endogenous, biologically active arachidonic acid derived epoxyeicosatrienoic acids …