Carboxylesterase inhibitors

MJ Hatfield, PM Potter - Expert opinion on therapeutic patents, 2011 - Taylor & Francis
Introduction: Carboxylesterases play major roles in the hydrolysis of numerous
therapeutically active compounds. This is, in part, due to the prevalence of the ester moiety …

The role of human carboxylesterases in drug metabolism: have we overlooked their importance?

S Casey Laizure, V Herring, Z Hu… - … : The Journal of …, 2013 - Wiley Online Library
Carboxylesterases are a multigene family of mammalian enzymes widely distributed
throughout the body that catalyze the hydrolysis of esters, amides, thioesters, 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 …

Discovery of hCES2A inhibitors from Glycyrrhiza inflata via combination of docking-based virtual screening and fluorescence-based inhibition assays

YQ Song, XQ Guan, ZM Weng, JL Liu, J Chen… - Food & function, 2021 - pubs.rsc.org
Human carboxylesterase 2 (hCES2A) is a key target to ameliorate the intestinal toxicity
triggered by irinotecan that causes severe diarrhea in 50%–80% of patients receiving this …

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 …

Pentacyclic triterpenoid acids in Styrax as potent and highly specific inhibitors against human carboxylesterase 1A

L Wang, XQ Guan, RJ He, WW Qin, Y Xiong, F Zhang… - Food & function, 2020 - pubs.rsc.org
Human carboxylesterase 1A1 (hCES1A) is a promising target for the treatment of
hyperlipidemia and obesity-associated metabolic diseases. To date, the highly specific and …

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 …

[HTML][HTML] Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism

C Gan, J Wang, A Martínez-Chávez… - … Pharmaceutica Sinica B, 2023 - Elsevier
Abstract The mammalian carboxylesterase 1 (Ces1/CES1) family comprises several
enzymes that hydrolyze many xenobiotic chemicals and endogenous lipids. To investigate …

Systematic identification and characterization of carboxylesterases in cynomolgus macaques

Y Uno, S Uehara, M Hosokawa, T Imai - Drug Metabolism and Disposition, 2014 - ASPET
Carboxylesterase (CES) is important for detoxification of a wide range of drugs and
xenobiotics and catalyzes cholesterol and fatty acid metabolism. Cynomolgus macaques are …

Combined ensemble docking and machine learning in identification of therapeutic agents with potential inhibitory effect on human CES1

E Briand, R Thomsen, K Linnet, HB Rasmussen… - Molecules, 2019 - mdpi.com
The human carboxylesterase 1 (CES1), responsible for the biotransformation of many
diverse therapeutic agents, may contribute to the occurrence of adverse drug reactions and …