Discovery of seven-membered ring berberine analogues as highly potent and specific hCES2A inhibitors

Y Yang, Y Xiong, G Zhu, M Sun, K Zou, Y Zhao… - Chemico-Biological …, 2023 - Elsevier
Abstract Human carboxylesterase 2A (hCES2A) is a key serine hydrolase responsible for
the metabolic clearance of large number of compounds bearing the ester-or amide-bond (s) …

Analysis of mammalian carboxylesterase inhibition by trifluoromethylketone-containing compounds

RM Wadkins, JL Hyatt, CC Edwards, L Tsurkan… - Molecular …, 2007 - ASPET
Carboxylesterases (CE) are ubiquitous enzymes that hydrolyze numerous ester-containing
xenobiotics, including complex molecules, such as the anticancer drugs irinotecan (CPT-11) …

Selective inhibitors of human liver carboxylesterase based on a β-lapachone scaffold: novel reagents for reaction profiling

MJ Hatfield, J Chen, EM Fratt, L Chi… - Journal of medicinal …, 2017 - ACS Publications
Carboxylesterases (CEs) are ubiquitous enzymes that are responsible for the metabolism of
xenobiotics, including drugs such as irinotecan and oseltamivir. Inhibition of CEs …

Hydrolysis by carboxylesterase and disposition of prodrug with ester moiety

T Imai - Yakugaku Zasshi: Journal of the Pharmaceutical …, 2007 - europepmc.org
Prodrug is a useful approach for improving the bioavailability of therapeutic agents through
increased passive transport. Carboxylesterases (CESs, EC. 3.1. 1.1.) that show ubiquitous …

Inhibition of human carboxylesterases hCE1 and hiCE by cholinesterase inhibitors

LG Tsurkan, MJ Hatfield, CC Edwards, JL Hyatt… - Chemico-biological …, 2013 - Elsevier
Carboxylesterases (CEs) are ubiquitously expressed proteins that are responsible for the
detoxification of xenobiotics. They tend to be expressed in tissues likely to be exposed to …

Discovery of novel selective inhibitors of human intestinal carboxylesterase for the amelioration of irinotecan-induced diarrhea: synthesis, quantitative structure-activity …

RM Wadkins, JL Hyatt, KJP Yoon, CL Morton… - Molecular …, 2004 - ASPET
The dose-limiting toxicity of the highly effective anticancer agent 7-ethyl-10-[4-(1-piperidino)-
1-piperidino] carbonyloxy-camptothecin (irinotecan; CPT-11) is delayed diarrhea. This is …

In silico design and evaluation of carboxylesterase inhibitors

SV Stoddard, X Yu, PM Potter… - Journal of Pesticide …, 2010 - jstage.jst.go.jp
Carboxylesterases (CEs) are important enzymes that catalyze biological detoxification,
hydrolysis of certain pesticides, and metabolism of many esterified drugs. The development …

Carboxylesterase 2 production and characterization in human cells: new insights into enzyme oligomerization and activity

J Lamego, B Cunha, C Peixoto, MF Sousa… - Applied microbiology …, 2013 - Springer
Abstract Carboxylesterase 2 (CES2), the main carboxylesterase expressed in human
intestine, is an increasingly important enzyme in anti-cancer combined therapies for the …

Discovery of dihydrooxazolo [2, 3-a] isoquinoliniums as highly specific inhibitors of hCE2

L Ding, L Wang, K Zou, B Li, Y Song, Q Zhang… - RSC …, 2019 - pubs.rsc.org
Human carboxylesterase 2 (hCE2) is one of the most abundant esterases distributed in
human small intestine and colon, which participates in the hydrolysis of a variety of ester …

Fluorogenic Chemical Tools to Shed Light on CES1-Mediated Adverse Drug Interactions

CJ Karns, TP Spidle, E Adusah, M Gao… - Chemical …, 2024 - pubs.rsc.org
Studying factors that cause interindividual variability of carboxylesterase 1 (CES1) activity is
currently difficult due to limited methods. Here, fluorogenic tools for measuring CES1 activity …