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Carboxylesterase 1 (CES1) genetic polymorphisms and oseltamivir activation

European Journal of Clinical Pharmacology, 2012
Carboxylesterase 1 (CES1) is the major hepatic hydrolytic enzyme responsible for the metabolism of many therapeutic agents, toxins, and endogenous compounds existing as esters, amides, thioesters, and carbamates. CES1 is coded by the CES1 gene in humans, which consists of three isoforms: CES1A1, CES1A2, and CES1A3.
Hao-Jie, Zhu, John S, Markowitz
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Human Carboxylesterases: An Update on CES1, CES2 and CES3

Protein & Peptide Letters, 2009
Carboxylesterases belong to Phase I group of drug metabolizing enzymes. They hydrolyze a variety of drug esters, amides, carbamates and similar structures. There are five 'carboxylesterase' genes listed in the Human Genome Organization database. In this review, we will focus on the CES1, CES2 and CES3 genes and their protein products that have been ...
Sonal P, Sanghani   +3 more
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Es-x/Ces1 prevents triacylglycerol accumulation in McArdle-RH7777 hepatocytes

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2009
Mouse esterase-x/carboxylesterase 1 (Es-x/Ces1) is a close homolog of triacylglycerol hydrolase/carboxylesterase 3 (TGH/Ces3). Es-x possesses a conserved esterase/lipase active site motif, suggesting that like TGH it could play a role in hepatic triacylglycerol (TG) metabolism.
Kerry W S, Ko   +2 more
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Carbonate‐Based Fluorescent Chemical Tool for Uncovering Carboxylesterase 1 (CES1) Activity Variations in Live Cells

ChemBioChem, 2022
AbstractCarboxylesterase 1 (CES1) plays a key role in the metabolism of endogenous biomolecules and xenobiotics including a variety of pharmaceuticals. Despite the established importance of CES1 in drug metabolism, methods to study factors that can vary CES1 activity are limited with only a few suitable for use in live cells.
Anchal Singh   +4 more
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Genetic variation in human carboxylesterase CES1 confers resistance to hepatic steatosis

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2018
Obesity often leads non-alcoholic fatty liver disease, insulin resistance and hyperlipidemia. Expression of carboxylesterase CES1 is positively correlated with increased lipid storage and plasma lipid concentration. Here we investigated structural and metabolic consequences of a single nucleotide polymorphism in CES1 gene that results in p.Gly143Glu ...
Jihong, Lian   +8 more
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Individualization of Treatments with Drugs Metabolized by CES1: Combining Genetics and Metabolomics

Pharmacogenomics, 2015
CES1 is involved in the hydrolysis of ester group-containing xenobiotic and endobiotic compounds including several essential and commonly used drugs. The individual variation in the efficacy and tolerability of many drugs metabolized by CES1 is considerable. Hence, there is a large interest in individualizing the treatment with these drugs. The present
Rasmussen, H.B.   +18 more
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Reappraisal of the Genetic Diversity and Pharmacogenetic Assessment of CES1

Pharmacogenomics, 2017
The CES1 gene encodes a hydrolase that metabolizes important drugs. Variants generated by exchange of segments with CES1P1 complicate genotyping of CES1. Using a highly specific procedure we examined DNA samples from 200 Caucasians and identified 46 single nucleotide variants (SNVs) in CES1 and 21 SNVs in CES1A2, a hybrid composed of CES1 and CES1P1 ...
Laura Ferrero-Miliani   +7 more
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Pharmacogenetic study of CES1 gene and enalapril efficacy

Journal of Applied Genetics
Enalapril is an orally administered angiotensin-converting enzyme inhibitor which is widely prescribed to treat hypertension, chronic kidney disease, and heart failure. It is an ester prodrug that needs to be activated by carboxylesterase 1 (CES1). CES1 is a hepatic hydrolase that in vivo biotransforms enalapril to its active form enalaprilat in order ...
Misbah Hussain   +5 more
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Presence and inter-individual variability of carboxylesterases (CES1 and CES2) in human lung

Biochemical Pharmacology, 2018
Lungs are pharmacologically active organs and the pulmonary drug metabolism is of interest for inhaled drugs design. Carboxylesterases (CESs) are enzymes catalyzing the hydrolysis of many structurally different ester, amide and carbamate chemicals, including prodrugs.
Gabriele Morena   +5 more
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Carboxylesterase 1 (Ces1): from monocyte marker to major player

Journal of Clinical Pathology, 2010
There are few, if any, enzymes that have been studied by, and have importance in, so many and varied disciplines as has monocyte esterase/Ces 1. In this review its involvement in the fields of histochemistry, haematology, toxicology, pharmacology, therapeutics, and tumour cell killing, immune surveillance and malignant disease, is briefly described.
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