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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
Organophosphorus Inhibition and Characterization of Recombinant Guinea Pig Acetylcholinesterase.
New
Gearhart et al., United States. In Protein Pept Lett, 28 Aug 2015
Historically, the guinea pig has been believed to be the best non-primate model for OP toxicology and medical countermeasure development because, similarly to humans, guinea pigs have low amounts of circulating OP metabolizing carboxylesterase.
Characterization of LipN (Rv2970c) of Mycobacterium Tuberculosis H37Rv and Its Probable Role in Xenobiotic Degradation.
New
Kaur et al., Chandīgarh, India. In J Cell Biochem, 24 Aug 2015
These findings suggested that LipN is a cytosolic, acid inducible carboxylesterase with no positional specificity in demonstrating activity with short carbon chain substrates.
Identification of activating enzymes of a novel FBPase inhibitor prodrug, CS-917.
New
Shinagawa et al., Tokyo, Japan. In Pharmacol Res Perspect, 30 Jun 2015
We identified cathepsin A (CTSA) and elastase 3B (ELA3B) as CS-917 esterases in the small intestine by mass spectrometry, whereas we found CTSA and carboxylesterase 1 (CES1) in monkey liver.
Notum deacylates Wnt proteins to suppress signalling activity.
New
Impact
Vincent et al., Potters Bar, United Kingdom. In Nature, 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.
The Toxicity and Detoxifying Mechanism of Cycloxaprid and Buprofezin in Controlling Sogatella furcifera (Homoptera: Delphacidae).
New
Teng et al., Shanghai, China. In J Insect Sci, Dec 2014
Mean carboxylesterase (CarE) specific activity of nymphal WBPH treated with cycloxaprid and buprofezin was higher than that of control, but there was no significant difference between cycloxaprid and control (no insecticide), and it was significantly higher for buprofezin than those of cycloxaprid and control.
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.
Chromatographic and electrophoretic strategies for the chiral separation and quantification of d- and l-threo methylphenidate in biological matrices.
Review
New
Pond et al., Johnson City, United States. In Biomed Chromatogr, Nov 2014
Furthermore, it was deduced that the stereoselective cleavage of MPH to produce ritalinic acid (RA) by human carboxylesterase results in a higher oral bioavailability of the d-threo enantiomer.
Mesenchymal stem cells as cellular vehicles for prodrug gene therapy against tumors.
Review
New
de Waziers et al., Paris, France. In Biochimie, Oct 2014
This review will summarize the current knowledge about MSCs engineered to express different suicide genes (cytosine deaminase, thymidine kinase, carboxylesterase, cytochrome P450) to elicit a significant antitumor response against brain tumors, ovarian, hepatocellular, pancreatic, renal or medullary thyroid carcinomas, breast or prostate cancer and pulmonary metastases.
The pharmacogenetics of carboxylesterases: CES1 and CES2 genetic variants and their clinical effect.
Review
Paré et al., In Drug Metabol Drug Interact, 2013
Human carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are serine esterases responsible for the hydrolysis of ester and amide bonds present in a number of pharmaceutical products.
Copy-number variations in hepatoblastoma associate with unique clinical features.
Chang et al., Taipei, Taiwan. In Hepatol Int, 2013
The carboxylesterase 4-like (CES4) gene that mapped to 16q12.2 was associated with smaller tumor size at presentation.
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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