- Length
- 567 aa
- Mass
- 62.5 kDa
- Annotated
- 2026-04-28
130 papers in source corpus
32 papers cited in narrative
32 extracted findings
Mechanistic narrative
Synthesis pass · prose summary of the discoveries below
Insufficient on-target evidence to synthesize a narrative — discovery timeline does not match the canonical CES1 protein.
Mechanism profile
Synthesis pass · controlled-vocabulary classification · explore literature graph →
No controlled-vocabulary terms were assigned to this entry.
Evidence
Reading pass · 32 per-paper findings extracted from the source corpus
| Year | Finding | Method | Journal | Conf | PMIDs |
|---|---|---|---|---|---|
| 1991 | CES1 (carboxylesterase 1) is expressed as a serine esterase in human alveolar macrophages and monocytes, where it is released into bronchoalveolar lavage fluid associated with surfactant; it is virtually identical to liver microsomal carboxylesterase, establishing CES1 as both a hepatic and macrophage enzyme with detoxification function. | Protein purification, [3H]DFP labeling, NH2-terminal sequencing, PCR cloning from macrophage cDNA library, Northern blot | The Journal of biological chemistry | High | 1918003 |
| 1993 | CES1 (hCE) encodes a 568-amino-acid serine hydrolase with an 18-aa signal peptide; baculovirus-expressed hCE hydrolyzes aromatic and aliphatic esters but not amides or fatty acyl-CoA esters; N-glycosylation is essential for maximal catalytic activity, as tunicamycin inhibition substantially reduces activity; two highly similar variants (hCE and hCEv) were identified as distinct gene family members. | cDNA cloning, baculovirus expression in Sf9 cells, enzymatic assays, tunicamycin inhibition, somatic cell hybrid chromosome mapping | Biochemistry | High | 8218228 |
| 1997 | Purified human liver CES1 (hCE-1) catalyzes hydrolysis of cocaine to benzoylecgonine, deacetylation of heroin to 6-acetylmorphine, and ethanol-dependent transesterification of cocaine to cocaethylene; binding is stereoselective for (R)-(-)-cocaine, and the methyl ester, benzoyl, and N-methyl groups of cocaine are critical for binding affinity. | Purified enzyme kinetic assays, competitive inhibition with 4-methylumbelliferyl acetate, stereoisomer comparison | Drug metabolism and disposition | High | 9311626 |
| 2000 | CES1 expressed in human macrophages functions as a cholesteryl ester hydrolase (CEH); overexpression in COS cells yielded >20-fold increased CEH activity; overexpression in CHO-K1 cells impaired LDL receptor mRNA upregulation under cholesterol-deficient conditions, placing CES1 in the intracellular cholesteryl ester metabolism pathway. | RT-PCR, cDNA cloning, transient transfection in COS-1/COS-7/CHO-K1 cells, enzymatic activity assay, Northern blot | Physiological genomics | High | 11015575 |
| 2003 | Crystal structures of human CES1 (hCE1) in complex with the cocaine analog homatropine and heroin analog naloxone reveal that the active site contains both a specific and a promiscuous compartment enabling metabolism of structurally distinct chemicals; a separate surface ligand-binding site regulates the trimer-hexamer equilibrium and allows each monomer to bind two narcotic molecules simultaneously. | X-ray crystallography of hCE1 glycoprotein complexes | Nature structural biology | High | 12679808 |
| 2003 | Crystal structure of hCE1 with tacrine (2.4 Å) shows tacrine binds in multiple orientations within the catalytic gorge, in contrast to acetylcholinesterase; this promiscuity is structurally explained by the larger, flexible active-site architecture of hCE1; tacrine derivatives were identified as low-micromolar CES1 inhibitors. | X-ray crystallography, inhibitor screening assays | Chemistry & biology | High | 12725862 |
| 2004 | CES1A1 (along with CES2 and CES3) hydrolyzes irinotecan and its oxidative metabolites NPC and APC to the active metabolite SN-38; the relative catalytic efficiency for CPT-11 hydrolysis is CES2 > CES1A1 >> CES3. | Purified recombinant enzyme kinetic assays | Drug metabolism and disposition | High | 15100172 |
| 2006 | Crystal structures of hCE1 with CoA, palmitate, cholate, and taurocholate reveal three ligand-binding sites (active site plus two additional sites), all exhibiting non-specific binding; this multisite promiscuity structurally explains CES1's ability to perform cholesterol ester hydrolysis, fatty acyl-CoA hydrolysis, acyl-CoA:cholesterol acyltransfer, and fatty acyl ethyl ester synthesis depending on cellular context. | X-ray crystallography of four hCE1 complexes with endogenous substrates/analogs | Journal of molecular biology | High | 16962139 |
| 2008 | Two CES1 coding mutations, p.Gly143Glu (exon 4) and p.Asp260fs (exon 6 frameshift/premature stop), cause complete loss of hydrolytic activity toward methylphenidate; p.Gly143Glu retains only 21.4% catalytic efficiency (Vmax/Km) and p.Asp260fs retains 0.6% relative to wild-type using p-nitrophenyl acetate; minor allele frequency of p.Gly143Glu is 3.7%/4.3%/2.0%/0% in white/black/Hispanic/Asian populations. | DNA sequencing, in vitro functional expression, kinetic assays with methylphenidate and p-nitrophenyl acetate | American journal of human genetics | High | 18485328 |
| 2008 | Human CES1 (HCE1) is expressed predominantly in liver and shows age-dependent ontogeny: fetal liver has lowest expression (~10-fold lower than adult), child liver is intermediate; CES1 selectively hydrolyzes oseltamivir over CES2, and adult microsomes are ~4× more active than child and ~10× more active than fetal microsomes; large inter-individual variability (up to 100-fold in protein) exists within the same age group. | RT-qPCR, Western immunoblotting across 104 liver samples (fetal, child, adult), hydrolytic activity assays | Biochemical pharmacology | High | 18983829 |
| 2009 | Mouse esterase-x/Ces1 (Es-x/Ces1), stably expressed in McArdle-RH7777 hepatocytes, reduces triacylglycerol (TG) accumulation by redirecting exogenous fatty acids toward beta-oxidation rather than TG synthesis, as evidenced by increased acid-soluble metabolites; this TG-lowering effect persisted with esterase inhibitor E600, indicating the mechanism is primarily reduction of fatty acid partitioning into TG rather than increased TG turnover; Es-x expression did not alter VLDL-TG or apolipoprotein B secretion. | Stable transfection of McArdle-RH7777 cells, TG quantification, acid-soluble metabolite measurement, E600 inhibitor experiment, glycerol supplementation | Biochimica et biophysica acta | High | 19651238 |
| 2012 | CES1 is the primary enzyme responsible for hydrolytic inactivation of clopidogrel and its intermediate 2-oxo-clopidogrel in human liver S9 fractions; inhibition of CES1 by bis(4-nitrophenyl) phosphate significantly increased concentrations of clopidogrel active metabolite; CES1 variants G143E and D260fs have completely impaired catalytic activity toward clopidogrel and 2-oxo-clopidogrel, whereas variants G18V, S82L, and A269S show no significant effect. | Human liver S9 fraction incubations, CES1 inhibitor experiments, transfected cell line S9 fractions, LC-MS/MS metabolite quantification | The Journal of pharmacology and experimental therapeutics | High | 23275066 |
| 2013 | The CES1 G143E variant carriers show significantly increased clopidogrel active metabolite levels and better clopidogrel response (reduced ADP-stimulated platelet aggregation) compared with non-carriers, confirming that CES1-mediated hydrolysis constitutes the primary inactivation route of clopidogrel in vivo. | Clinical pharmacogenomics study (PAPI study, n=566 + 350 CHD patients), active metabolite measurement, platelet aggregation assay | Pharmacogenetics and genomics | High | 23111421 |
| 2013 | Recombinant human CES1 efficiently hydrolyzes enalapril, ramipril, and trandolapril (but not CES2), establishing CES1 as the primary activating enzyme for these ACE inhibitor prodrugs; enalapril shows substrate inhibition kinetics while ramipril and trandolapril follow Michaelis-Menten kinetics; isradipine and tacrolimus are identified as novel CES1 inhibitors. | Recombinant enzyme assays, Michaelis-Menten/substrate inhibition kinetic modeling, inhibitor screening with human liver microsomes | Drug metabolism and disposition | High | 24141856 |
| 2015 | CES1 selectively activates ACE inhibitor prodrugs enalapril, ramipril, perindopril, moexipril, and fosinopril in human liver (not intestine or kidney); the G143E variant is a loss-of-function variant reducing enalapril activation to ~one-third of wild-type in human liver samples carrying the 143G/E genotype; neither CES1/CES1VAR nor CES1P1/CES1P1VAR genotypes/diplotypes affected hepatic CES1 expression or activity in normal liver samples. | Human liver/intestine/kidney S9 fraction incubations, CES1 inhibitor (BNPP), recombinant transfected cell lines, 102 normal human liver samples | The pharmacogenomics journal | High | 26076923 |
| 2015 | Fluoxetine decreases CES1 expression and hydrolytic activity in HepG2 cells by decreasing pregnane X receptor (PXR) expression and increasing DEC1; PXR overexpression attenuated and PXR knockdown abolished CES1 decreases; DEC1 knockdown increased PXR and restored CES1, establishing a FLX→DEC1↑/PXR↓→CES1↓ transcriptional regulatory axis. | HepG2 cell transfection (overexpression and siRNA knockdown), RT-PCR, Western blot, enzymatic activity assay | Xenobiotica | High | 26340669 |
| 2016 | Sacubitril is selectively activated (hydrolyzed) by CES1 in human liver S9 fractions but not by CES2 or in intestine/kidney/plasma; the G143E variant is a loss-of-function variant for sacubitril activation; human livers with G143E genotype show significantly impaired sacubitril activation. | Incubation with human tissue S9 fractions, CES1-selective inhibitor BNPP, recombinant CES1 and CES2, transfected cell lines, human liver samples with G143E genotyping | Drug metabolism and disposition | High | 26817948 |
| 2016 | The CES1VAR genomic translocation (replacing 5'UTR, exon 1, and part of intron 1 with CES1P1 pseudogene sequence, minor allele frequency 17%) reduces CES1 mRNA by ~2.6-fold and allelic mRNA by ~1.35-fold; however, CES1VAR did not detectably alter CES1 protein expression or metabolizing activity toward enalapril, clopidogrel, or methylphenidate in liver. | Sanger and Ion Torrent sequencing, allelic mRNA analysis (SNaPshot), quantitative targeted proteomics, luciferase reporter assays in HepG2 | Pharmacogenetics and genomics | High | 26871237 |
| 2016 | CES1 and CES2 protein abundance in human liver microsomes increases approximately 5-fold and 3-fold from neonates to adults, respectively; oseltamivir carboxylase activity correlates with CES1 protein abundance across pediatric and adult liver microsomes, validating the ontogeny function for PBPK modeling. | LC-MS/MS proteomics with purified protein standards as calibrators and heavy-labeled peptide internal standards in 171 liver samples | Drug metabolism and disposition | High | 27895113 |
| 2018 | The CES1 G143E variant (p.Gly143Glu) reduces lipolytic activity to ~20% of wild-type; humanized mice expressing CES1G143E on a Ces1-null background fed a high-fat diet show reduced liver and plasma triacylglycerol levels; the hypolipidemic mechanism involves decreased VLDL secretion, decreased hepatic lipogenic gene expression, and increased fatty acid oxidation (elevated plasma ketone bodies and hepatic mitochondrial electron transport chain protein abundance). | Humanized mouse model (liver-specific CES1WT, CES1G143E, CES1S221A expression on Ces1-/- background), high-fat diet feeding, TG/cholesterol measurements, lipogenic gene expression, ketone body assay, mitochondrial protein quantification | Biochimica et biophysica acta. Molecular and cell biology of lipids | High | 29631096 |
| 2017 | Global inactivation of Ces1/Ces1g in Ldlr-/- mice protects against atherosclerosis by inhibiting intestinal cholesterol and fat absorption (including reduced Niemann-Pick C1-like 1 expression), increasing macrophage cholesterol efflux (via ABCA1 and ABCG1 induction), promoting M2 macrophage polarization, and inducing hepatic cholesterol 7α-hydroxylase and sterol 12α-hydroxylase; paradoxically, hepatic-specific Ces1/Ces1g knockdown in Apoe-/- mice exacerbated atherogenesis. | Ces1g-/- Ldlr-/- double knockout mice, Western diet feeding, atherosclerotic lesion quantification, intestinal cholesterol absorption assay, macrophage cholesterol efflux assay, gene expression analysis | Scientific reports | High | 29259301 |
| 2019 | Vitamin E reverses NAFLD-associated lipid accumulation in fructose-treated mice via upregulation of Nrf2 and CES1; the Nrf2 inhibitor ML385 abolished the protective effects of vitamin E on lipid metabolism, establishing a Nrf2→CES1 signaling axis in hepatic lipid homeostasis. | NAFLD mouse model (fructose feeding), vitamin E treatment, Nrf2 inhibitor (ML385), histopathology, lipid assays, in vitro L02 cell experiments | Digestive diseases and sciences | Medium | 31076985 |
| 2019 | CES1 is the most abundant drug-metabolizing enzyme in human liver (~1% of entire liver proteome), responsible for 80-95% of total hepatic hydrolytic activity; alcohol is identified as a potent CES1 inhibitor that can alter therapeutic outcomes of CES1 substrate medications. | Proteomic quantification studies (reviewed), inhibitor characterization studies (reviewed) | Drug metabolism and disposition | Medium | 31871135 |
| 2020 | CES1 in human monocytic THP-1 cells hydrolyzes prostaglandin D2-glyceryl ester (PGD2-G), accounting for ~50% of its hydrolytic metabolism; CES1 knockdown or pharmacological inhibition (CPO, WWL113, WWL229) stabilizes PGD2-G, augmenting its anti-inflammatory effects (reduced IL-6, TNFα) upon LPS stimulation; PGD2-G (and/or downstream metabolites) activates PPARγ, altering alternative macrophage activation; inhibitor potency rank order: CPO > WWL113 > WWL229. | THP-1 cell CES1 knockdown (siRNA), CES1 inhibitor dose-response, LC-MS/MS metabolite quantification, cytokine ELISA, PPARγ activation assay | ACS omega | High | 33225149 |
| 2021 | Melatonin treatment restores CES1 expression in prostate cancer cells via epigenetic modification; restored CES1 expression reduces lipid droplet accumulation, induces ER stress-mediated apoptosis, and reduces intratumoral androgen synthesis; Ces1-knockout mice show increased PCa tumor growth, confirming CES1's tumor-suppressive role via lipid metabolism regulation. | Animal CRPC models, PCa cell lines, Ces1-/- mouse model, lipid droplet quantification, apoptosis assays, androgen synthesis measurement, epigenetic assays | Clinical and translational medicine | Medium | 34185414 |
| 2021 | CES1 G143E heterozygous carriers show 30.9% lower enalaprilat Cmax and 27.5% lower enalaprilat AUC0-∞ at steady state compared to non-carriers; carriers also showed no statistically significant blood pressure reduction vs ~12.4% reduction in non-carriers, directly linking CES1 loss-of-function to impaired prodrug activation and pharmacodynamic effect in vivo. | Prospective multi-dose PK/PD clinical study, LC-MS/MS quantification, blood pressure monitoring | British journal of clinical pharmacology | High | 33963573 |
| 2022 | TMAO (trimethylamine N-oxide) increases Ces1 protein expression and activity in mouse liver and HepG2 cells via a NOX-dependent ROS/Nrf2/CES1 pathway, leading to increased clopidogrel hydrolysis (inactivation) and impaired platelet response; co-administration of TMAO-synthesis inhibitor (3,3-dimethyl-1-butanol), antioxidant (N-acetyl-L-cysteine), or Nrf2 inhibitor (ML385) reversed these effects. | Mouse dietary TMAO/choline feeding, pharmacological pathway dissection (FMO inhibitor, antioxidant, Nrf2 inhibitor), HepG2 cell treatment, Ces1 protein/activity measurement, clopidogrel metabolite LC-MS/MS, platelet aggregation assay | Journal of thrombosis and haemostasis | High | 36695375 |
| 2023 | CES1 inhibition (pharmacological or siRNA) in hepatocellular carcinoma cells alters lipid profiles by reducing polyunsaturated fatty acids (PUFAs), which activates PPARα/γ; loss of PPARα/γ activation downregulates the target gene SCD (involved in chemoresistance); the CES1-PPARα/γ-SCD axis sensitizes HCC cells to cisplatin, and co-administration of cisplatin with CES1 inhibition slows xenograft tumor growth. | Pharmacological CES1 inhibition, siRNA knockdown, lipidomic analysis, PPARα/γ pathway analysis, SCD expression measurement, cisplatin sensitivity assays, xenograft mouse model | JCI insight | High | 36472914 |
| 2023 | G9a (Ehmt2-encoded histone methyltransferase) suppresses transcription of Ces1 in renal tubules; G9a and farnesoid X receptor (FXR) competitively bind to the same promoter regions of Ces1; tubular-specific G9a knockout (Ehmt2Ksp) or G9a inhibition derepresses Ces1, reducing lipid accumulation and alleviating AKI; pharmacological Ces1 inhibition reverses the AKI-protective effect of Ehmt2Ksp mice, establishing a G9a/FXR-Ces1 axis controlling renal lipid homeostasis. | Renal tubular-specific G9a knockout mice, pharmacological G9a inhibition, Ces1 pharmacological inhibition, chromatin binding assays (G9a vs FXR competition at Ces1 promoter), lipid staining, AKI model (I/R and cisplatin), atorvastatin and FXR agonist treatment | EMBO reports | High | 37042626 |
| 2024 | Nicotine activates CHRNA5 in head and neck squamous cell carcinoma cells, which physically interacts with CES1 (confirmed by co-immunoprecipitation and molecular docking); CHRNA5 activation via the MEK/ERK pathway upregulates CES1 expression; CHRNA5 knockdown reduces CES1 mRNA and protein levels, an effect reversed by nicotine exposure. | Co-immunoprecipitation, molecular docking, immunofluorescence, CHRNA5 knockdown/overexpression, Western blot for p-MEK/MEK, p-ERK/ERK and CES1, nude mouse tumor formation assay | Cell death & disease | Medium | 39472448 |
| 2018 | CES1 in human lungs is present predominantly in the microsomal fraction with 30-50-fold higher Vmax for pNPA (CES1 marker substrate) compared to FD (CES2 marker); CES1 and CES2 show 2.5-5-fold and 8-15-fold inter-individual variation in lung hydrolytic activity, respectively, demonstrating CES1 as the dominant esterase in human lung tissue. | Cytosol and microsomal fractionation of 20 human lung samples, kinetic assays (Vmax, Km), selective inhibitor studies (loperamide for CES2, BNPP, PMSF) | Biochemical pharmacology | High | 29407485 |
| 2018 | MiR-155 overexpression in THP-1 macrophages upregulates CES1 (CEH) mRNA and protein in a dose- and time-dependent manner; miR-155-mediated CEH induction reduces intracellular cholesteryl ester accumulation and foam cell formation; siRNA knockdown of CEH reverses miR-155's anti-foam cell effect; Tim-3 overexpression attenuates miR-155-mediated CEH induction, placing Tim-3 upstream of the miR-155/CES1 axis. | miR-155 mimic transfection, siCEH knockdown, Tim-3 overexpression in THP-1 macrophages, cholesterol efflux assay, lipid accumulation quantification, RT-PCR and Western blot | Biomedicine & pharmacotherapy | Medium | 29803178 |
Source papers
Stage 0 corpus · 130 papers · ranked by NIH iCite citations
| Year | Title | Journal | Citations | PMID |
|---|---|---|---|---|
| 2002 | Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. | Proceedings of the National Academy of Sciences of the United States of America | 1479 | 12477932 |
| 2020 | A reference map of the human binary protein interactome. | Nature | 849 | 32296183 |
| 2005 | Microarray analysis identifies a death-from-cancer signature predicting therapy failure in patients with multiple types of cancer. | The Journal of clinical investigation | 760 | 15931389 |
| 2021 | Dual proteome-scale networks reveal cell-specific remodeling of the human interactome. | Cell | 705 | 33961781 |
| 2011 | Phylogenetic-based propagation of functional annotations within the Gene Ontology consortium. | Briefings in bioinformatics | 656 | 21873635 |
| 2004 | The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). | Genome research | 438 | 15489334 |
| 2005 | Diversification of transcriptional modulation: large-scale identification and characterization of putative alternative promoters of human genes. | Genome research | 409 | 16344560 |
| 2001 | A regulatory cascade of three homeobox genes, ceh-10, ttx-3 and ceh-23, controls cell fate specification of a defined interneuron class in C. elegans. | Development (Cambridge, England) | 248 | 11493519 |
| 2002 | Current progress on esterases: from molecular structure to function. | Drug metabolism and disposition: the biological fate of chemicals | 241 | 11950776 |
| 2013 | Genetic determinants of dabigatran plasma levels and their relation to bleeding. | Circulation | 209 | 23467860 |
| 2003 | Irinotecan pathway genotype analysis to predict pharmacokinetics. | Clinical cancer research : an official journal of the American Association for Cancer Research | 209 | 12960109 |
| 2011 | Next-generation sequencing to generate interactome datasets. | Nature methods | 200 | 21516116 |
| 2008 | Two CES1 gene mutations lead to dysfunctional carboxylesterase 1 activity in man: clinical significance and molecular basis. | American journal of human genetics | 188 | 18485328 |
| 2007 | Carboxylesterase in the liver and small intestine of experimental animals and human. | Life sciences | 170 | 17764701 |
| 2012 | Carboxylesterase 1 as a determinant of clopidogrel metabolism and activation. | The Journal of pharmacology and experimental therapeutics | 166 | 23275066 |
| 2003 | Structural basis of heroin and cocaine metabolism by a promiscuous human drug-processing enzyme. | Nature structural biology | 166 | 12679808 |
| 2010 | Recommended nomenclature for five mammalian carboxylesterase gene families: human, mouse, and rat genes and proteins. | Mammalian genome : official journal of the International Mammalian Genome Society | 146 | 20931200 |
| 1996 | Transcriptional regulator of programmed cell death encoded by Caenorhabditis elegans gene ces-2. | Nature | 141 | 8700229 |
| 2003 | Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. | Chemistry & biology | 136 | 12725862 |
| 2013 | The functional G143E variant of carboxylesterase 1 is associated with increased clopidogrel active metabolite levels and greater clopidogrel response. | Pharmacogenetics and genomics | 135 | 23111421 |
| 1991 | A serine esterase released by human alveolar macrophages is closely related to liver microsomal carboxylesterases. | The Journal of biological chemistry | 128 | 1918003 |
| 2008 | Human carboxylesterases HCE1 and HCE2: ontogenic expression, inter-individual variability and differential hydrolysis of oseltamivir, aspirin, deltamethrin and permethrin. | Biochemical pharmacology | 126 | 18983829 |
| 2006 | Multisite promiscuity in the processing of endogenous substrates by human carboxylesterase 1. | Journal of molecular biology | 117 | 16962139 |
| 2021 | Paralog knockout profiling identifies DUSP4 and DUSP6 as a digenic dependence in MAPK pathway-driven cancers. | Nature genetics | 116 | 34857952 |
| 2004 | Hydrolysis of irinotecan and its oxidative metabolites, 7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin and 7-ethyl-10-[4-(1-piperidino)-1-amino]-carbonyloxycamptothecin, by human carboxylesterases CES1A1, CES2, and a newly expressed carboxylesterase isoenzyme, CES3. | Drug metabolism and disposition: the biological fate of chemicals | 105 | 15100172 |
| 1999 | The C. elegans cell death specification gene ces-1 encodes a snail family zinc finger protein. | Molecular cell | 102 | 10518212 |
| 2009 | Human carboxylesterases: an update on CES1, CES2 and CES3. | Protein and peptide letters | 100 | 19508181 |
| 2003 | The Snail-like CES-1 protein of C. elegans can block the expression of the BH3-only cell-death activator gene egl-1 by antagonizing the function of bHLH proteins. | Development (Cambridge, England) | 99 | 12874127 |
| 2000 | Cholesteryl ester hydrolase in human monocyte/macrophage: cloning, sequencing, and expression of full-length cDNA. | Physiological genomics | 99 | 11015575 |
| 2004 | Pharmacogenomic assessment of carboxylesterases 1 and 2. | Genomics | 95 | 15475243 |
| 1993 | Glycosylation-dependent activity of baculovirus-expressed human liver carboxylesterases: cDNA cloning and characterization of two highly similar enzyme forms. | Biochemistry | 95 | 8218228 |
| 2019 | Carboxylesterase 1 and Precision Pharmacotherapy: Pharmacogenetics and Nongenetic Regulators. | Drug metabolism and disposition: the biological fate of chemicals | 92 | 31871135 |
| 2013 | In vitro drug metabolism by human carboxylesterase 1: focus on angiotensin-converting enzyme inhibitors. | Drug metabolism and disposition: the biological fate of chemicals | 91 | 24141856 |
| 2009 | Human plasma carboxylesterase 1, a novel serologic biomarker candidate for hepatocellular carcinoma. | Proteomics | 89 | 19658107 |
| 1997 | Human liver carboxylesterase hCE-1: binding specificity for cocaine, heroin, and their metabolites and analogs. | Drug metabolism and disposition: the biological fate of chemicals | 86 | 9311626 |
| 2016 | Age-Dependent Absolute Abundance of Hepatic Carboxylesterases (CES1 and CES2) by LC-MS/MS Proteomics: Application to PBPK Modeling of Oseltamivir In Vivo Pharmacokinetics in Infants. | Drug metabolism and disposition: the biological fate of chemicals | 85 | 27895113 |
| 2014 | The pharmacogenetics of carboxylesterases: CES1 and CES2 genetic variants and their clinical effect. | Drug metabolism and drug interactions | 84 | 24988246 |
| 2003 | Human carboxylesterase 1: from drug metabolism to drug discovery. | Biochemical Society transactions | 82 | 12773168 |
| 1997 | The POU gene ceh-18 promotes gonadal sheath cell differentiation and function required for meiotic maturation and ovulation in Caenorhabditis elegans. | Developmental biology | 79 | 9405097 |
| 2004 | Proteins associated with type II bone morphogenetic protein receptor (BMPR-II) and identified by two-dimensional gel electrophoresis and mass spectrometry. | Proteomics | 77 | 15188402 |
| 1994 | Targeted mutations in the Caenorhabditis elegans POU homeo box gene ceh-18 cause defects in oocyte cell cycle arrest, gonad migration, and epidermal differentiation. | Genes & development | 75 | 7958868 |
| 2000 | Overlapping roles of two Hox genes and the exd ortholog ceh-20 in diversification of the C. elegans postembryonic mesoderm. | Development (Cambridge, England) | 72 | 11060243 |
| 2000 | The LIM homeobox gene ceh-14 confers thermosensory function to the AFD neurons in Caenorhabditis elegans. | Neuron | 70 | 10774727 |
| 2007 | The C. elegans protein CEH-30 protects male-specific neurons from apoptosis independently of the Bcl-2 homolog CED-9. | Genes & development | 69 | 18056428 |
| 2006 | Wnt signaling and CEH-22/tinman/Nkx2.5 specify a stem cell niche in C. elegans. | Current biology : CB | 69 | 16461282 |
| 2011 | The homeobox protein CEH-23 mediates prolonged longevity in response to impaired mitochondrial electron transport chain in C. elegans. | PLoS biology | 68 | 21713031 |
| 2002 | Roles of the Homothorax/Meis/Prep homolog UNC-62 and the Exd/Pbx homologs CEH-20 and CEH-40 in C. elegans embryogenesis. | Development (Cambridge, England) | 65 | 12399316 |
| 1995 | The C. elegans neuronally expressed homeobox gene ceh-10 is closely related to genes expressed in the vertebrate eye. | Development (Cambridge, England) | 63 | 7789259 |
| 2007 | Control of sex-specific apoptosis in C. elegans by the BarH homeodomain protein CEH-30 and the transcriptional repressor UNC-37/Groucho. | Genes & development | 62 | 18056429 |
| 1999 | Anterior organization of the Caenorhabditis elegans embryo by the labial-like Hox gene ceh-13. | Development (Cambridge, England) | 62 | 10068646 |
| 2016 | Sacubitril Is Selectively Activated by Carboxylesterase 1 (CES1) in the Liver and the Activation Is Affected by CES1 Genetic Variation. | Drug metabolism and disposition: the biological fate of chemicals | 59 | 26817948 |
| 2005 | Distinct molecular alterations in complex endometrial hyperplasia (CEH) with and without immature squamous metaplasia (squamous morules). | The American journal of surgical pathology | 59 | 16160475 |
| 2000 | The homeodomain protein CePHOX2/CEH-17 controls antero-posterior axonal growth in C. elegans. | Development (Cambridge, England) | 59 | 10887091 |
| 2009 | Regulation of carboxylesterase 1 (CES1) in human adipose tissue. | Biochemical and biophysical research communications | 56 | 19332024 |
| 2015 | CES1 genetic variation affects the activation of angiotensin-converting enzyme inhibitors. | The pharmacogenomics journal | 53 | 26076923 |
| 2006 | Direct regulation of egl-1 and of programmed cell death by the Hox protein MAB-5 and by CEH-20, a C. elegans homolog of Pbx1. | Development (Cambridge, England) | 53 | 16421192 |
| 2002 | Conserved regulation of the Caenorhabditis elegans labial/Hox1 gene ceh-13. | Developmental biology | 53 | 11820809 |
| 2007 | UNC-4 represses CEH-12/HB9 to specify synaptic inputs to VA motor neurons in C. elegans. | Genes & development | 49 | 17289921 |
| 2019 | Synthesis of clathrate cerium superhydride CeH9 at 80-100 GPa with atomic hydrogen sublattice. | Nature communications | 48 | 31575861 |
| 2016 | Age-Dependent Human Hepatic Carboxylesterase 1 (CES1) and Carboxylesterase 2 (CES2) Postnatal Ontogeny. | Drug metabolism and disposition: the biological fate of chemicals | 48 | 26825642 |
| 2010 | A dysregulation in CES1, APOE and other lipid metabolism-related genes is associated to cardiovascular risk factors linked to obesity. | Obesity facts | 48 | 20975297 |
| 2005 | ceh-16/engrailed patterns the embryonic epidermis of Caenorhabditis elegans. | Development (Cambridge, England) | 48 | 15659483 |
| 2005 | Functional characterization of three naturally occurring single nucleotide polymorphisms in the CES2 gene encoding carboxylesterase 2 (HCE-2). | Drug metabolism and disposition: the biological fate of chemicals | 45 | 16033949 |
| 2001 | Regulation of ectodermal and excretory function by the C. elegans POU homeobox gene ceh-6. | Development (Cambridge, England) | 45 | 11171402 |
| 2019 | CEH-60/PBX and UNC-62/MEIS Coordinate a Metabolic Switch that Supports Reproduction in C. elegans. | Developmental cell | 42 | 30956009 |
| 2018 | The impact of ABCB1 (rs1045642 and rs4148738) and CES1 (rs2244613) gene polymorphisms on dabigatran equilibrium peak concentration in patients after total knee arthroplasty. | Pharmacogenomics and personalized medicine | 42 | 30100750 |
| 2009 | The NK-2 class homeodomain factor CEH-51 and the T-box factor TBX-35 have overlapping function in C. elegans mesoderm development. | Development (Cambridge, England) | 42 | 19605496 |
| 2021 | Melatonin inhibits lipid accumulation to repress prostate cancer progression by mediating the epigenetic modification of CES1. | Clinical and translational medicine | 41 | 34185414 |
| 2017 | The impact of CES1 genotypes on the pharmacokinetics of methylphenidate in healthy Danish subjects. | British journal of clinical pharmacology | 38 | 28087982 |
| 2004 | The C. elegans ceh-36 gene encodes a putative homemodomain transcription factor involved in chemosensory functions of ASE and AWC neurons. | Journal of molecular biology | 38 | 15095973 |
| 2001 | The Caenorhabditis elegans Six/sine oculis class homeobox gene ceh-32 is required for head morphogenesis. | Developmental biology | 38 | 11476572 |
| 1997 | The expression of the C. elegans labial-like Hox gene ceh-13 during early embryogenesis relies on cell fate and on anteroposterior cell polarity. | Development (Cambridge, England) | 38 | 9334268 |
| 2010 | The HMX/NKX homeodomain protein MLS-2 specifies the identity of the AWC sensory neuron type via regulation of the ceh-36 Otx gene in C. elegans. | Development (Cambridge, England) | 37 | 20150279 |
| 2010 | Depot-specific expression of lipolytic genes in human adipose tissues--association among CES1 expression, triglyceride lipase activity and adiposity. | Journal of atherosclerosis and thrombosis | 35 | 21081832 |
| 2009 | Es-x/Ces1 prevents triacylglycerol accumulation in McArdle-RH7777 hepatocytes. | Biochimica et biophysica acta | 35 | 19651238 |
| 2023 | Interfering with lipid metabolism through targeting CES1 sensitizes hepatocellular carcinoma for chemotherapy. | JCI insight | 33 | 36472914 |
| 2018 | Presence and inter-individual variability of carboxylesterases (CES1 and CES2) in human lung. | Biochemical pharmacology | 33 | 29407485 |
| 2019 | Vitamin E Ameliorates Lipid Metabolism in Mice with Nonalcoholic Fatty Liver Disease via Nrf2/CES1 Signaling Pathway. | Digestive diseases and sciences | 32 | 31076985 |
| 2023 | Loss of renal tubular G9a benefits acute kidney injury by lowering focal lipid accumulation via CES1. | EMBO reports | 30 | 37042626 |
| 2015 | CYP2C19 and CES1 polymorphisms and efficacy of clopidogrel and aspirin dual antiplatelet therapy in patients with symptomatic intracranial atherosclerotic disease. | Journal of neurosurgery | 29 | 26587656 |
| 2013 | Methylphenidate side effect profile is influenced by genetic variation in the attention-deficit/hyperactivity disorder-associated CES1 gene. | Journal of child and adolescent psychopharmacology | 29 | 24350812 |
| 2007 | Haplotypes and a novel defective allele of CES2 found in a Japanese population. | Drug metabolism and disposition: the biological fate of chemicals | 29 | 17640957 |
| 2003 | The Caenorhabditis elegans ems class homeobox gene ceh-2 is required for M3 pharynx motoneuron function. | Development (Cambridge, England) | 29 | 12810585 |
| 2018 | Genetic variation in human carboxylesterase CES1 confers resistance to hepatic steatosis. | Biochimica et biophysica acta. Molecular and cell biology of lipids | 28 | 29631096 |
| 2015 | The Bicoid class homeodomain factors ceh-36/OTX and unc-30/PITX cooperate in C. elegans embryonic progenitor cells to regulate robust development. | PLoS genetics | 28 | 25738873 |
| 2022 | The enteric nervous system of the C. elegans pharynx is specified by the Sine oculis-like homeobox gene ceh-34. | eLife | 27 | 35324425 |
| 2018 | Effect of Genetic Variation of NAT2 on Isoniazid and SLCO1B1 and CES2 on Rifampin Pharmacokinetics in Ghanaian Children with Tuberculosis. | Antimicrobial agents and chemotherapy | 27 | 29263072 |
| 2009 | The C. elegans engrailed homolog ceh-16 regulates the self-renewal expansion division of stem cell-like seam cells. | Developmental biology | 24 | 19607822 |
| 2020 | Natural Products as Modulators of CES1 Activity. | Drug metabolism and disposition: the biological fate of chemicals | 23 | 32591414 |
| 2017 | Transcription factors CEP-1/p53 and CEH-23 collaborate with AAK-2/AMPK to modulate longevity in Caenorhabditis elegans. | Aging cell | 23 | 28560849 |
| 2005 | Altered expression of TFF-1 and CES-2 in Barrett's Esophagus and associated adenocarcinomas. | Neoplasia (New York, N.Y.) | 23 | 15967118 |
| 2019 | Influence of CYP450 Enzymes, CES1, PON1, ABCB1, and P2RY12 Polymorphisms on Clopidogrel Response in Patients Subjected to a Percutaneous Neurointervention. | Clinical therapeutics | 22 | 31128980 |
| 2017 | Global inactivation of carboxylesterase 1 (Ces1/Ces1g) protects against atherosclerosis in Ldlr -/- mice. | Scientific reports | 22 | 29259301 |
| 2014 | CES2, ABCG2, TS and Topo-I primary and synchronous metastasis expression and clinical outcome in metastatic colorectal cancer patients treated with first-line FOLFIRI regimen. | International journal of molecular sciences | 22 | 25198900 |
| 2007 | Transcriptional regulation of AQP-8, a Caenorhabditis elegans aquaporin exclusively expressed in the excretory system, by the POU homeobox transcription factor CEH-6. | The Journal of biological chemistry | 22 | 17660295 |
| 2018 | MiR-155 inhibits transformation of macrophages into foam cells via regulating CEH expression. | Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie | 21 | 29803178 |
| 2022 | The COVID-19 Oral Drug Molnupiravir Is a CES2 Substrate: Potential Drug-Drug Interactions and Impact of CES2 Genetic Polymorphism In Vitro. | Drug metabolism and disposition: the biological fate of chemicals | 20 | 35790245 |
| 2015 | Individualization of treatments with drugs metabolized by CES1: combining genetics and metabolomics. | Pharmacogenomics | 20 | 25896426 |
| 2013 | Relationship between CES2 genetic variations and rifampicin metabolism. | The Journal of antimicrobial chemotherapy | 20 | 23471941 |
| 2010 | Carboxylesterase 1 (Ces1): from monocyte marker to major player. | Journal of clinical pathology | 20 | 21177752 |
| 2024 | Nicotine-induced CHRNA5 activation modulates CES1 expression, impacting head and neck squamous cell carcinoma recurrence and metastasis via MEK/ERK pathway. | Cell death & disease | 19 | 39472448 |
| 2020 | Effect of Sex, Use of Pantoprazole and Polymorphisms in SLC22A1, ABCB1, CES1, CYP3A5 and CYP2D6 on the Pharmacokinetics and Safety of Dabigatran. | Advances in therapy | 19 | 32564268 |
| 2016 | Regulatory effects of genomic translocations at the human carboxylesterase-1 (CES1) gene locus. | Pharmacogenetics and genomics | 19 | 26871237 |
| 2010 | The C. elegans Hox gene ceh-13 regulates cell migration and fusion in a non-colinear way. Implications for the early evolution of Hox clusters. | BMC developmental biology | 19 | 20667114 |
| 2009 | Two Hox cofactors, the Meis/Hth homolog UNC-62 and the Pbx/Exd homolog CEH-20, function together during C. elegans postembryonic mesodermal development. | Developmental biology | 19 | 19643105 |
| 2009 | Relations between strain and gender dependencies of irinotecan toxicity and UGT1A1, CES2 and TOP1 expressions in mice. | Toxicology letters | 19 | 19931604 |
| 2023 | The homeodomain transcription factor CEH-37 regulates PMK-1/p38 MAPK pathway to protect against intestinal infection via the phosphatase VHP-1. | Cellular and molecular life sciences : CMLS | 18 | 37796333 |
| 2013 | The LIM homeobox gene ceh-14 is required for phasmid function and neurite outgrowth. | Developmental biology | 18 | 23608457 |
| 2020 | Effect of CES1 and ABCB1 genotypes on the pharmacokinetics and clinical outcomes of dabigatran etexilate in patients with atrial fibrillation and chronic kidney disease. | Drug metabolism and personalized therapy | 17 | 32134727 |
| 2020 | Inactivation of CES1 Blocks Prostaglandin D2 Glyceryl Ester Catabolism in Monocytes/Macrophages and Enhances Its Anti-inflammatory Effects, Whereas the Pro-inflammatory Effects of Prostaglandin E2 Glyceryl Ester Are Attenuated. | ACS omega | 17 | 33225149 |
| 2019 | The impact of human CES1 genetic variation on enzyme activity assessed by ritalinic acid/methylphenidate ratios. | Basic & clinical pharmacology & toxicology | 17 | 30801959 |
| 2017 | The Pharmacokinetics of Enalapril in Relation to CES1 Genotype in Healthy Danish Volunteers. | Basic & clinical pharmacology & toxicology | 17 | 28639420 |
| 2013 | Coordination of cell proliferation and cell fate determination by CES-1 snail. | PLoS genetics | 17 | 24204299 |
| 2003 | Twelve novel single nucleotide polymorphisms in the CES2 gene encoding human carboxylesterase 2 (hCE-2). | Drug metabolism and pharmacokinetics | 17 | 15618752 |
| 2001 | The Caenorhabditis elegans distal-less ortholog ceh-43 is required for development of the anterior hypodermis. | Developmental dynamics : an official publication of the American Association of Anatomists | 17 | 11747075 |
| 1998 | Effects of deletion mutations in the yeast Ces1 protein on cell growth and morphology and on high copy suppression of mutations in mRNA capping enzyme and translation initiation factor 4A. | Nucleic acids research | 17 | 9443973 |
| 2022 | Choline and trimethylamine N-oxide impair metabolic activation of and platelet response to clopidogrel through activation of the NOX/ROS/Nrf2/CES1 pathway. | Journal of thrombosis and haemostasis : JTH | 16 | 36695375 |
| 2021 | Enhancer RNA lnc-CES1-1 inhibits decidual cell migration by interacting with RNA-binding protein FUS and activating PPARγ in URPL. | Molecular therapy. Nucleic acids | 16 | 33738142 |
| 2015 | Fluoxetine reduces CES1, CES2, and CYP3A4 expression through decreasing PXR and increasing DEC1 in HepG2 cells. | Xenobiotica; the fate of foreign compounds in biological systems | 16 | 26340669 |
| 2013 | Clinical implications of CES2 RNA expression in neuroblastoma. | Journal of pediatric surgery | 16 | 23480903 |
| 2009 | Exploring the diabetogenicity of the HLA-B18-DR3 CEH: independent association with T1D genetic risk close to HLA-DOA. | Genes and immunity | 16 | 19458622 |
| 2004 | An early pharyngeal muscle enhancer from the Caenorhabditis elegans ceh-22 gene is targeted by the Forkhead factor PHA-4. | Developmental biology | 16 | 14738885 |
| 2003 | Sequence-specific binding to telomeric DNA by CEH-37, a homeodomain protein in the nematode Caenorhabditis elegans. | The Journal of biological chemistry | 16 | 12711598 |
| 2021 | CES2 sustains HNF4α expression to promote pancreatic adenocarcinoma progression through an epoxide hydrolase-dependent regulatory loop. | Molecular metabolism | 15 | 34971802 |
| 2020 | PIG-1 MELK-dependent phosphorylation of nonmuscle myosin II promotes apoptosis through CES-1 Snail partitioning. | PLoS genetics | 15 | 32946434 |
| 2019 | CEH-60/PBX regulates vitellogenesis and cuticle permeability through intestinal interaction with UNC-62/MEIS in Caenorhabditis elegans. | PLoS biology | 15 | 31675356 |
| 2017 | Single-nucleotide polymorphisms in the genes of CES2, CDA and enzymatic activity of CDA for prediction of the efficacy of capecitabine-containing chemotherapy in patients with metastatic breast cancer. | Pharmacological research | 15 | 28827188 |
| 2020 | Genetic Analysis Reveals a Significant Contribution of CES1 to Prostate Cancer Progression in Taiwanese Men. | Cancers | 14 | 32466188 |
| 2001 | Multiple enhancers contribute to expression of the NK-2 homeobox gene ceh-22 in C. elegans pharyngeal muscle. | Genesis (New York, N.Y. : 2000) | 14 | 11783006 |
| 2021 | Effect of CES1 genetic variation on enalapril steady-state pharmacokinetics and pharmacodynamics in healthy subjects. | British journal of clinical pharmacology | 13 | 33963573 |