Property Summary

NCBI Gene PubMed Count 82
PubMed Score 677.23
PubTator Score 500.07

Knowledge Summary

Patent

No data available

Expression

  Differential Expression (4)

Disease log2 FC p
lung adenocarcinoma -1.600 9.2e-08
lung carcinoma -4.100 6.8e-45
non-small cell lung carcinoma -2.000 6.1e-31
psoriasis -1.600 9.8e-48

MLP Assay (2)

AID Type Active / Inconclusive / Inactive Description
463149 other 3 / 0 / 21 Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: Fluorescence-based biochemical gel-based ABPP inhibition and selectivity
588807 other 12 / 0 / 31 Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition and selectivity in a complex proteome for ABHD10

Gene RIF (53)

PMID Text
26657071 The structure and activity of glycosylated and aglycosylated human CES1 has been determined.
26340669 decreases of CES and CYP3A4 expression and enzymatic activities induced by Fluoxetine are through decreasing PXR and increasing DEC1 in HepG2 cells
25704243 CES1 c.428G>A single nucleotide variation increases clopidogrel active metabolite concentrations and antiplatelet effects by reducing clopidogrel hydrolysis to inactive metabolites
24563511 CEH is an important regulator in enhancing cholesterol elimination.
24350812 study found an association between two CES1 SNP markers and the occurrence of sadness as a side effect of short-acting methylphenidate
24212379 After oral administration of dabigatran etexilate to humans, DABE is hydrolyzed by intestinal CES2 to the intermediate M2 metabolite followed by hydrolysis of M2 to DAB in the liver by CES1.
24170778 The conversion of 2-oxo-ticlopidine to M1 was further confirmed with recombinant paraoxonase 1 (PON1) and CES1.
24141856 CES1 plays a role in the metabolism of several drugs.
23936796 PMPMEase overexpression in colorectal cancer and cancer cell death stemming from its inhibition is an indication of its possible role in cancer progression and a target for chemopreventive agents
23658012 carboxylesterase I controls RhoA methylation
23468884 Carboxylesterase 1 gene duplication and mRNA expression in adipose tissue are linked to obesity and metabolic function.
23275066 Deficient CES1 catalytic activity resulting from CES1 inhibition.
23111421 Genetic variation in CES1 may be an important determinant of the efficacy of clopidogrel.
22943824 The CES1 SNP rs8192950 AC genotype and rs1968753 GG genotype might be the candidates for risk prediction of antituberculosis drug-induced hepatotoxicity.
22700792 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.
22688218 An influence of carboxylesterase 1 -75 T>G polymorphism on the worsening of appetite reduction with MPH treatment in youths with ADHD.
22588607 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.
22525521 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
22237548 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.
21081832 High mRNA levels of CES1 is associated with adiposity and lipolysis, thereby contributing to the development of obesity-associated phenotypes.
20975297 Dysregulation of genes such as CES1 and APOE seems to be associated with some physiopathological markers of insulin resistance and cardiovascular risk factors in obesity.
20649590 Report CES1 mediated hydrolysis of heroin, cocaine and CPT-11.
20530478 The knockdown of CES1 with siRNA resulted in lower levels of HCV replication, and up-regulation of CES1 was observed to favor HCV propagation, implying an important role for this host cell protein.
20529763 Observational study of gene-disease association. (HuGE Navigator)
20195289 Observational study of gene-disease association. (HuGE Navigator)
19932971 Molecular dynamics results emphasize properties of the CES1 catalytic cavity, confirming that CES1 prefers substrates with relatively smaller and somewhat polar alkyl/aryl groups and larger hydrophobic acyl moieties.
19733552 We observed an association with the rare 143Glu-variant: 5 patients in the responder group carrying the Glu-allele required lower doses of MPH for symptom reduction.
19733552 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
19715681 Luciferase assays revealed that the antioxidant response element (ARE) at -2025 in the CES1A1 gene was responsible for the transactivation by Nrf2
19658107 The high-resolution proteomic approach demonstrates that hCE1 is a good candidate for further validation as a serologic glycoprotein biomarker for HCC.
19508181 A comparison of the substrate specificity of CES1 versus CES2 reveals broad but distinct substrate preferences.
19343046 Observational study of gene-disease association. (HuGE Navigator)
19332024 CES1 expression was linked to body fat and adipocyte fat content but not to lipolytic activity.
19185566 CES1 mutations Gly143Glu and Asp260fs are essentially dysfunctional enzymes with regard to the conversion of trandolapril to its more active metabolite trandolaprilat.
18983829 Carboxylesterases play critical roles in drug metabolism and insecticide detoxication; findings show large variability among different age groups or even within the same age group.
18794728 pharmacogenomic characterization of human carboxylesterase 1A1, 1A2, and 1A3 genes
18599737 hepatic CEH regulates the last step of RCT by promoting the flux of cholesterol entering the liver via SR-BI and increasing hepatic bile acid output [cholesteryl ester hydrolase]
18485328 In vitro functional studies demonstrated the catalytic functions of both p.Gly143Glu and p.Asp260fs are substantially impaired, resulting in a complete loss of hydrolytic activity toward methylphenidate.
18485328 Observational study of genotype prevalence. (HuGE Navigator)
18328811 SNP haplotype in the CES1A2 promoter affects the Sp1 binding and transcriptional regulation; it well agreed with the efficacy of the medication of imidapril.
18305377 Carboxylesterase 1A1 mRNA expression level is much higher than the expression of carboxylesterase 1A2 mRNA in the liver and lung.
17764701 comparative analysis of CES1 and CES2 in liver and small intestine of humans, monkeys, dogs, rabbits and rats
17537833 IL-6 alters the cellular responsiveness to clopidogrel, irinotecan, and oseltamivir by suppressing the expression of CES1.
16971496 Cholesteryl ester hydrolase expression in human macrophages is potential target for attenuation of foam cell formation and regression of atherosclerotic plaques.
16962139 Using multisite promiscuity, carboxylesterase 1 appears structurally capable of assembling several catalytic events, depending upon the physiological state of the cellular environment.
16419644 Observational study of gene-environment interaction and pharmacogenomic / toxicogenomic. (HuGE Navigator)
16282638 Findings indicate that F417 but not L418, L420, or C390 participates in substrate hydrolysis by triacylglycerol hydrolase.
15931389 Altered expression is associated with therapy failure and death in patients with multiple types of cancer.
15475733 Observational study of gene-disease association. (HuGE Navigator)
15475243 Observational study of genotype prevalence. (HuGE Navigator)
12960109 Observational study of gene-environment interaction and pharmacogenomic / toxicogenomic. (HuGE Navigator)
12773168 A serine esterase involved in both drug metabolism and activation.
12679808 crystal structure bound to analogs of cocaine and heroin

AA Sequence

MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQP      1 - 70
AEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIH     71 - 140
GGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGG    141 - 210
NPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSA    211 - 280
VMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGI    281 - 350
NKQEFGWLIPMQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDL    351 - 420
IADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEI    421 - 490
RLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAKKAVEKPP    491 - 560
QTEHIEL                                                                   561 - 567
//

Text Mined References (90)

PMID Year Title
26657071 2015 Comparison of the Structure and Activity of Glycosylated and Aglycosylated Human Carboxylesterase 1.
26340669 2016 Fluoxetine reduces CES1, CES2, and CYP3A4 expression through decreasing PXR and increasing DEC1 in HepG2 cells.
25944712 2015 N-terminome analysis of the human mitochondrial proteome.
25704243 2015 Carboxylesterase 1 c.428G>A single nucleotide variation increases the antiplatelet effects of clopidogrel by reducing its hydrolysis in humans.
24563511 2014 Liver-specific transgenic expression of cholesteryl ester hydrolase reduces atherosclerosis in Ldlr-/- mice.
24350812 2013 Methylphenidate side effect profile is influenced by genetic variation in the attention-deficit/hyperactivity disorder-associated CES1 gene.
24275569 2014 An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome.
24212379 2014 Identification of carboxylesterase-dependent dabigatran etexilate hydrolysis.
24170778 2014 Multiple cytochrome P450 isoforms are involved in the generation of a pharmacologically active thiol metabolite, whereas paraoxonase 1 and carboxylesterase 1 catalyze the formation of a thiol metabolite isomer from ticlopidine.
24141856 2014 In vitro drug metabolism by human carboxylesterase 1: focus on angiotensin-converting enzyme inhibitors.
23936796 2013 Polyisoprenylated methylated protein methyl esterase is both sensitive to curcumin and overexpressed in colorectal cancer: implications for chemoprevention and treatment.
23658012 2013 Control of RhoA methylation by carboxylesterase I.
23468884 2013 Carboxylesterase 1 gene duplication and mRNA expression in adipose tissue are linked to obesity and metabolic function.
23467860 2013 Genetic determinants of dabigatran plasma levels and their relation to bleeding.
23275066 2013 Carboxylesterase 1 as a determinant of clopidogrel metabolism and activation.
23111421 2013 The functional G143E variant of carboxylesterase 1 is associated with increased clopidogrel active metabolite levels and greater clopidogrel response.
22943824 2012 [The relationship between carboxylesterase 1 gene polymorphisms and susceptibility to antituberculosis drug-induced hepatotoxicity].
22700792 2012 Identification of a novel intracellular cholesteryl ester hydrolase (carboxylesterase 3) in human macrophages: compensatory increase in its expression after carboxylesterase 1 silencing.
22688218 2013 Association of a carboxylesterase 1 polymorphism with appetite reduction in children and adolescents with attention-deficit/hyperactivity disorder treated with methylphenidate.
22588607 2012 Carboxylesterase 1 polymorphism impairs oseltamivir bioactivation in humans.
22525521 2012 Examination of the carboxylesterase phenotype in human liver.
22237548 2012 A discriminative analytical method for detection of CES1A1 and CES1A2/CES1A3 genetic variants.
21492153 2011 Analysis of proteomic changes induced upon cellular differentiation of the human intestinal cell line Caco-2.
21081832 2011 Depot-specific expression of lipolytic genes in human adipose tissues--association among CES1 expression, triglyceride lipase activity and adiposity.
20975297 2010 A dysregulation in CES1, APOE and other lipid metabolism-related genes is associated to cardiovascular risk factors linked to obesity.
20931200 2010 Recommended nomenclature for five mammalian carboxylesterase gene families: human, mouse, and rat genes and proteins.
20649590 2010 Biochemical and molecular analysis of carboxylesterase-mediated hydrolysis of cocaine and heroin.
20530478 2010 Activity-based protein profiling identifies a host enzyme, carboxylesterase 1, which is differentially active during hepatitis C virus replication.
20529763 2010 Evaluation of candidate genes for cholinesterase activity in farmworkers exposed to organophosphorus pesticides: association of single nucleotide polymorphisms in BCHE.
20422440 2010 Mammalian carboxylesterase 3: comparative genomics and proteomics.
20195289 2010 Genetic variation in carboxylesterase genes and susceptibility to isoniazid-induced hepatotoxicity.
19932971 2010 In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations.
19733552 2009 Carboxylesterase 1 gene polymorphism and methylphenidate response in ADHD.
19715681 2010 Transcriptional regulation of human carboxylesterase 1A1 by nuclear factor-erythroid 2 related factor 2 (Nrf2).
19658107 2009 Human plasma carboxylesterase 1, a novel serologic biomarker candidate for hepatocellular carcinoma.
19508181 2009 Human carboxylesterases: an update on CES1, CES2 and CES3.
19487248 2009 Age- and sex-related expression and activity of carboxylesterase 1 and 2 in mouse and human liver.
19343046 2009 Association study between single-nucleotide polymorphisms in 199 drug-related genes and commonly measured quantitative traits of 752 healthy Japanese subjects.
19332024 2009 Regulation of carboxylesterase 1 (CES1) in human adipose tissue.
19225040 2009 Different inhibitory effects in rat and human carboxylesterases.
19185566 2009 Role of carboxylesterase 1 and impact of natural genetic variants on the hydrolysis of trandolapril.
18983829 2009 Human carboxylesterases HCE1 and HCE2: ontogenic expression, inter-individual variability and differential hydrolysis of oseltamivir, aspirin, deltamethrin and permethrin.
18794728 2008 Structure and characterization of human carboxylesterase 1A1, 1A2, and 1A3 genes.
18599737 2008 Hepatic overexpression of cholesteryl ester hydrolase enhances cholesterol elimination and in vivo reverse cholesterol transport.
18485328 2008 Two CES1 gene mutations lead to dysfunctional carboxylesterase 1 activity in man: clinical significance and molecular basis.
18328811 2008 Functional polymorphisms in carboxylesterase1A2 (CES1A2) gene involves specific protein 1 (Sp1) binding sites.
18305377 2008 Structural organization and characterization of the regulatory element of the human carboxylesterase (CES1A1 and CES1A2) genes.
17764701 2007 Carboxylesterase in the liver and small intestine of experimental animals and human.
17537833 2007 Interleukin-6 alters the cellular responsiveness to clopidogrel, irinotecan, and oseltamivir by suppressing the expression of carboxylesterases HCE1 and HCE2.
17264798 2007 Human carboxylesterase 1A2 expressed from carboxylesterase 1A1 and 1A2 genes is a potent predictor of CPT-11 cytotoxicity in vitro.
16971496 2007 Stable overexpression of human macrophage cholesteryl ester hydrolase results in enhanced free cholesterol efflux from human THP1 macrophages.
16962139 2006 Multisite promiscuity in the processing of endogenous substrates by human carboxylesterase 1.
16712791 2006 Identification of intrahepatic cholangiocarcinoma related genes by comparison with normal liver tissues using expressed sequence tags.
16419644 2005 A single nucleotide polymorphism in the carboxylesterase gene is associated with the responsiveness to imidapril medication and the promoter activity.
16344560 2006 Diversification of transcriptional modulation: large-scale identification and characterization of putative alternative promoters of human genes.
16282638 2006 Mutation of F417 but not of L418 or L420 in the lipid binding domain decreases the activity of triacylglycerol hydrolase.
15931389 2005 Microarray analysis identifies a death-from-cancer signature predicting therapy failure in patients with multiple types of cancer.
15616553 2004 The sequence and analysis of duplication-rich human chromosome 16.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15475733 2004 Determination and analysis of single nucleotide polymorphisms and haplotype structure of the human carboxylesterase 2 gene.
15475243 2004 Pharmacogenomic assessment of carboxylesterases 1 and 2.
15188402 2004 Proteins associated with type II bone morphogenetic protein receptor (BMPR-II) and identified by two-dimensional gel electrophoresis and mass spectrometry.
14702039 2004 Complete sequencing and characterization of 21,243 full-length human cDNAs.
12960109 2003 Irinotecan pathway genotype analysis to predict pharmacokinetics.
12773168 2003 Human carboxylesterase 1: from drug metabolism to drug discovery.
12725862 2003 Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition.
12721789 2003 Catalog of 680 variations among eight cytochrome p450 ( CYP) genes, nine esterase genes, and two other genes in the Japanese population.
12679808 2003 Structural basis of heroin and cocaine metabolism by a promiscuous human drug-processing enzyme.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12022871 2002 Structure-function analysis of human triacylglycerol hydrolase by site-directed mutagenesis: identification of the catalytic triad and a glycosylation site.
11950776 2002 Current progress on esterases: from molecular structure to function.
11812220 2002 Heterologous expression, purification, and characterization of human triacylglycerol hydrolase.
11409902 2001 Cloning of the human cholesteryl ester hydrolase promoter: identification of functional peroxisomal proliferator-activated receptor responsive elements.
11015575 2000 Cholesteryl ester hydrolase in human monocyte/macrophage: cloning, sequencing, and expression of full-length cDNA.
10562416 1999 Human egasyn binds beta-glucuronidase but neither the esterase active site of egasyn nor the C terminus of beta-glucuronidase is involved in their interaction.
10518925 1999 cDNA cloning, characterization and stable expression of novel human brain carboxylesterase.
10452915 1999 Human carboxylesterases in term placentae: enzymatic characterization, molecular cloning and evidence for the existence of multiple forms.
9490062 1998 Purification and characterization of retinyl ester hydrolase as a member of the non-specific carboxylesterase supergene family.
9169443 1997 Purification and cloning of a broad substrate specificity human liver carboxylesterase that catalyzes the hydrolysis of cocaine and heroin.
9003459 1997 Structural organization and characterization of the promoter region of a human carboxylesterase gene.
8597091 1995 Molecular aspects of carboxylesterase isoforms in comparison with other esterases.
8406473 1993 Molecular cloning and characterization of a human carboxylesterase gene.
8218228 1993 Glycosylation-dependent activity of baculovirus-expressed human liver carboxylesterases: cDNA cloning and characterization of two highly similar enzyme forms.
8049197 1994 Purification, cloning, and expression of a human enzyme with acyl coenzyme A: cholesterol acyltransferase activity, which is identical to liver carboxylesterase.
7980644 1994 Purification and characterization of a human liver cocaine carboxylesterase that catalyzes the production of benzoylecgonine and the formation of cocaethylene from alcohol and cocaine.
2612723 1989 Purification and characterization of two human liver carboxylesterases.
2070086 1991 cDNA cloning and characterization of human monocyte/macrophage serine esterase-1.
1997784 1991 Cloning and sequencing of a human liver carboxylesterase isoenzyme.
1918003 1991 A serine esterase released by human alveolar macrophages is closely related to liver microsomal carboxylesterases.
1748313 1991 Cloning and analysis of a cDNA encoding a human liver carboxylesterase.