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Carboxylesterase 1

Carboxylesterase, REH
This gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or transesterification of various xenobiotics, such as cocaine and heroin, and endogenous substrates with ester, thioester, or amide bonds. They may participate in fatty acyl and cholesterol ester metabolism, and may play a role in the blood-brain barrier system. This enzyme is the major liver enzyme and functions in liver drug clearance. Mutations of this gene cause carboxylesterase 1 deficiency. Three transcript variants encoding three different isoforms have been found for this gene. [provided by RefSeq, Jun 2010] (from NCBI)
Top mentioned proteins: ESI, ACID, CAN, acetylcholinesterase, HAD
Papers using Carboxylesterase antibodies
Gene set enrichment analysis: A knowledge-based approach for interpreting genome-wide expression profiles.
Supplier
Jeang K. T., In PLoS ONE, 2004
... Total RNA was isolated from biological replicates of E/R-silenced REH (n = 3) and AT-2 (n = 3) cells obtained from independent KD experiments by Trizol reagent (Life Technologies, Carlsbad, CA) ...
Papers on Carboxylesterase
Efficient Hepatic Delivery by Tenofovir Alafenamide (GS-7340): Implications for Hepatitis B Virus Therapy.
New
Ray et al., In Antimicrob Agents Chemother, 13 May 2015
While cathepsin A is known to be the major enzyme hydrolyzing TAF in HIV-target cells including lymphocytes and macrophages, TAF was primarily hydrolyzed by carboxylesterase 1 (CES1) in primary human hepatocytes, with cathepsin A making a small contribution.
Pharmacokinetic characterization of BMS-936561, an anti-CD70 antibody-drug conjugate, in preclinical animal species and prediction of its pharmacokinetics in humans.
New
Zheng et al., Princeton, United States. In Biopharm Drug Dispos, 13 May 2015
MED-A is a carbamate prodrug that is activated by carboxylesterase to its active form, MED-B, to exert its DNA alkylation activity.
A Novel Reaction Mediated by Human Aldehyde Oxidase: Amide Hydrolysis of GDC-0834.
New
Halladay et al., Washington, D.C., United States. In Drug Metab Dispos, 06 May 2015
Aldehyde oxidase (AO) and carboxylesterase (CES) were putatively identified as the enzymes responsible following cytosolic fractionation and MS-proteomics analysis of the enzymatically active fractions.
Two homologous carboxylesterase genes from Locusta migratoria with different tissue expression patterns and roles in insecticide detoxification.
New
Zhang et al., Taiyuan, China. In J Insect Physiol, 01 May 2015
UNASSIGNED: Carboxylesterases (CarEs) play a crucial role in detoxification of xenobiotics and resistance to insecticides in insects.
Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: In vitro, in situ intestinal perfusion, and portal vein cannulation models.
New
Mandlekar et al., Bengaluru, India. In Biopharm Drug Dispos, 01 May 2015
Enalapril, a carboxyl ester prodrug, is reported to be metabolized by human carboxylesterase-1 (CES1) but not by carboxylesterase-2 (CES2) to its active metabolite enalaprilat.
Notum deacylates Wnt proteins to suppress signalling activity.
New
Impact
Vincent et al., Potters Bar, United Kingdom. In Nature, 12 Apr 2015
Kinetic and mass spectrometric analyses of human proteins show that Notum is a carboxylesterase that removes an essential palmitoleate moiety from Wnt proteins and thus constitutes the first known extracellular protein deacylase.
A comprehensive review of UDP-glucuronosyltransferase and esterases for drug development.
Review
New
Nakajima et al., Nagoya, Japan. In Drug Metab Pharmacokinet, Feb 2015
In the field of esterases, it is becoming clear that enzymes other than carboxylesterase are involved in drug hydrolysis.
Pharmacokinetic drug interactions with clopidogrel: updated review and risk management in combination therapy.
Review
New
Zhou et al., Hangzhou, China. In Ther Clin Risk Manag, Dec 2014
The mechanism of the DDIs with clopidogrel involves modulating CYP enzymes (eg, CYP2B6, CYP2C8, CYP2C19, and CYP3A4), paraoxonase-1, hepatic carboxylesterase 1, P-glycoprotein, and organic anion transporter family member 1B1.
Oxidative stress-mediated cytotoxicity and metabolism of T-2 toxin and deoxynivalenol in animals and humans: an update.
Review
New
Yuan et al., Jingzhou, China. In Arch Toxicol, Jul 2014
Similarly to carboxylesterase, CYP3A29 possesses the hydrolytic ability in pigs to convert T-2 toxin to NEO.
Vinyl acetate monomer (VAM) genotoxicity profile: relevance for carcinogenicity.
Review
Albertini, Burlington, United States. In Crit Rev Toxicol, 2013
It is also DNA reactive and mutagenic, but only after its carboxylesterase mediated conversion to acetaldehyde (AA), a metabolic reaction that also produces acetic acid and protons.
Investigation binding patterns of human carboxylesterase I (hCES I) with broad substrates by MD simulations.
Review
Li et al., Dalian, China. In Curr Top Med Chem, 2012
Human carboxylesterase I (hCES 1) plays an important role in the metabolism and activation of prodrugs, such as, the hydrolysis of a variety of drugs of prodrugs featuring an ester, amide or carbamate function.
Metabolomics identifies an inflammatory cascade involved in dioxin- and diet-induced steatohepatitis.
Impact
Gonzalez et al., Bethesda, United States. In Cell Metab, 2012
Serum metabolomics identified azelaic acid monoesters as significantly increased metabolites after TCDD treatment, due to downregulation of hepatic carboxylesterase 3 (CES3, also known as triglyceride hydrolase) expression in an arylhydrocarbon receptor (AhR)-dependent manner in mice.
Identification of a novel intracellular cholesteryl ester hydrolase (carboxylesterase 3) in human macrophages: compensatory increase in its expression after carboxylesterase 1 silencing.
GeneRIF
Ghosh et al., Richmond, United States. In Am J Physiol Cell Physiol, 2012
This study provides the first evidence of functional compensation whereby increased expression of CES3 restores intracellular cholesteryl ester hydrolytic activity and free cholesterol efflux in CES1-deficient cells.
Carboxylesterase 1 polymorphism impairs oseltamivir bioactivation in humans.
GeneRIF
Niemi et al., Helsinki, Finland. In Clin Pharmacol Ther, 2012
Genetic variability in Carboxylesterase 1 affects the pharmacokinetics of oseltamivir and indicate that CES1 plays an important role in the bioactivation of oseltamivir in humans.
Examination of the carboxylesterase phenotype in human liver.
GeneRIF
Xie et al., United States. In Arch Biochem Biophys, 2012
tested the hypothesis that an individual's CES phenotype can be characterized by reporter substrates/probes that interrogate native CES1 and CES2 activities in liver and immunoblotting methods
A discriminative analytical method for detection of CES1A1 and CES1A2/CES1A3 genetic variants.
GeneRIF
Markowitz et al., Gainesville, United States. In Pharmacogenet Genomics, 2012
The comparison of the genotyping results between this novel assay and those previously reported methods highlighted the necessity of applying the discriminative genotyping assay in pharmacogenetic studies involving CES1 gene.
Depot-specific expression of lipolytic genes in human adipose tissues--association among CES1 expression, triglyceride lipase activity and adiposity.
GeneRIF
Ishibashi et al., Tochigi, Japan. In J Atheroscler Thromb, 2010
High mRNA levels of CES1 is associated with adiposity and lipolysis, thereby contributing to the development of obesity-associated phenotypes.
Loss of TGH/Ces3 in mice decreases blood lipids, improves glucose tolerance, and increases energy expenditure.
Impact
Lehner et al., Edmonton, Canada. In Cell Metab, 2010
Here we show that ablation of carboxylesterase 3 (Ces3)/triacylglycerol hydrolase (TGH) expression in mice (Tgh(-/-)) results in decreased plasma triacylglycerol, apolipoprotein B, and fatty acid levels in both fasted and fed states.
Enzyme-catalyzed activation of anticancer prodrugs.
Review
Impact
Vermeulen et al., Amsterdam, Netherlands. In Pharmacol Rev, 2004
The following endogenous enzymes are discussed: aldehyde oxidase, amino acid oxidase, cytochrome P450 reductase, DT-diaphorase, cytochrome P450, tyrosinase, thymidylate synthase, thymidine phosphorylase, glutathione S-transferase, deoxycytidine kinase, carboxylesterase, alkaline phosphatase, beta-glucuronidase and cysteine conjugate beta-lyase.
Modulation of irinotecan metabolism by ketoconazole.
Impact
Sparreboom et al., Rotterdam, Netherlands. In J Clin Oncol, 2002
RESULTS: With ketoconazole coadministration, the relative formation of APC was reduced by 87% (P =.002), whereas the relative exposure to the carboxylesterase-mediated SN-38 as expected on the basis of dose (area under the plasma concentration-time curve normalized to dose) was increased by 109% (P =.004).
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