Functional Study of Carboxylesterase 1 Protein Isoforms. [PDF]
Proteomics, 2019 Abstract Carboxylesterase 1 (CES1) is a primary human hepatic hydrolase involved in hydrolytic biotransformation of numerous medications. Considerable interindividual variability in CES1 expression and activity has been consistently reported. Four isoforms of the CES1 protein are produced by alternative splicing (AS).
Wang X, Shi J, Zhu HJ.
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Association of Oseltamivir Activation with Gender and Carboxylesterase 1 Genetic Polymorphisms. [PDF]
Basic Clin Pharmacol Toxicol, 2016 AbstractOseltamivir, an inactive anti‐influenza virus prodrug, is activated (hydrolysed) in vivo by carboxylesterase 1 (CES1) to its active metabolite oseltamivir carboxylate. CES1 functions are significantly associated with certain CES1 genetic variants and some non‐genetic factors. The purpose of this study was to investigate the effect of gender and
Shi J +6 more
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Confounding Effect of Hepatic Carboxylesterase 1 (CES1) Variability on Clopidogrel Oxidation. [PDF]
Mol PharmClopidogrel, a frequently used prodrug, is converted to its active metabolite through the intermediate 2-oxo-clopidogrel by cytochrome P450 (CYP) enzymes, which accounts for only 5%-15% of its metabolism. Majority of the clopidogrel dose (85%-90%) is extensively hydrolyzed to its inactive metabolite, clopidogrel carboxylic acid by carboxylesterase 1 ...
Subash S +8 more
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Effect of carboxylesterase 1 S75N on clopidogrel therapy among acute coronary syndrome patients [PDF]
Scientific Reports, 2017 Carboxylesterase 1 (CES1) hydrolyzes the prodrug clopidogrel to an inactive carboxylic acid metabolite. The effects of CES1 S75N (rs2307240,C>T) on clopidogrel response among 851 acute coronary syndrome patients who came from the north, central and south
Fei-Yan Xiao +8 more
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The novel carboxylesterase 1 variant c.662A>G may decrease the bioactivation of oseltamivir in humans. [PDF]
PLoS ONE, 2017 Human carboxylesterase 1 (CES1) is a serine esterase that hydrolyses various exogenous and endogenous compounds including oseltamivir, a prodrug used to treat influenza. A novel CES1 c.662A>G single nucleotide polymorphism (SNP) was predicted to decrease
Jaeseong Oh +7 more
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Structure-Activity Relationships of Pentacyclic Triterpenoids as Potent and Selective Inhibitors against Human Carboxylesterase 1 [PDF]
Frontiers in Pharmacology, 2017 Human carboxylesterase 1 (hCE1), one of the most important serine hydrolases distributed in liver and adipocytes, plays key roles in endobiotic homeostasis and xenobiotic metabolism.
Li-Wei Zou +14 more
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Randomized evaluation of the loss‐of‐function carboxylesterase 1 (CES1) G143E variant on clopidogrel and ticagrelor pharmacodynamics [PDF]
Clinical and Translational ScienceAntiplatelet therapy with a P2Y12 receptor inhibitor, in combination with aspirin, is standard of care for medical management of patients with coronary artery disease, and flexibility in prescribing options among these medications offers great potential ...
Joshua P. Lewis +9 more
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Carboxylesterase 1 and Precision Pharmacotherapy
, 2021 Carboxylesterase 1 (CES1) is a major phase I drug-metabolizing enzyme, responsible for 80-95% of total hydrolytic activity in human livers. CES1 plays a crucial role in the metabolism of a wide range of drugs, pesticides, environmental pollutants, and endogenous compounds.
Lucy Her
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Carboxylesterase 1 and Precision Pharmacotherapy: Pharmacogenetics and Nongenetic Regulators. [PDF]
Drug Metab Dispos, 2020 Carboxylesterase (CES) 1 is the most abundant drug-metabolizing enzyme in human livers, comprising approximately 1% of the entire liver proteome. CES1 is responsible for 80%-95% of total hydrolytic activity in the liver and plays a crucial role in the metabolism of a wide range of drugs (especially ester-prodrugs), pesticides, environmental pollutants,
Her L, Zhu HJ.
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The COVID‐19 Medicine Remdesivir Is Therapeutically Activated by Carboxylesterase‐1, and Excessive Hydrolysis Increases Cytotoxicity [PDF]
Hepatology Communications, 2021 Yue Shen, William Eades, Bingfang Yan
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