Recombinant Human Liver carboxylesterase 1 (CES1)

1. Study utilized humanized mouse model expressing WT (control), G143E and catalytically dead S221A variants of human CES1 in the liver in the absence of endogenous expression of the mouse orthologous gene shows that compared to wild-type CES1, expression of the CES1G143E confers resistance to development of high-fat diet induced hepatic steatosis and leads to improved metabolic profile. PMID: 29631096
2. Which selectively amplified CES1A1 and, if present, also CES1A2. PMID: 29457755
3. These results are consistent with a model in which abrogation of CES1 function attenuates the CYP27A1-LXRalpha-ABCA1 signaling axis by depleting endogenous ligands for the nuclear receptors PPARgamma, RAR, and/or RXR that regulate cholesterol homeostasis. PMID: 29321244
4. Anordrin is predominantly catalyzed by CES1 and CES2 to generate the main active metabolite, anordiol. PMID: 28532270
5. genetic association and pharmacogenomic studies in population in Finland: Data suggest that 2 SNPs in CES1 (rs12443580, rs8192935) are associated with variations in expression of CES1 (in whole blood samples but not in liver); these CES1 SNPs do not affect pharmacokinetics or pharmacodynamics of clopidogrel, an inhibitor of platelet aggregation. A missense mutation in CES1 (rs71647871) impairs hydrolysis of clopidogrel. PMID: 28990360
6. The frequencies of SNVs with a potential functional impact were below 0.02 suggesting limited pharmacogenetic potential for CES1 genotyping. PMID: 28786738
7. none of the selected variations of CES1 had a clinically relevant impact on the metabolism of enalapril PMID: 28639420
8. Study revealed that several nsSNPs significantly impaired CES1 activity on the metabolism of the CES1 substrates enalapril, clopidogrel, and sacubitril. PMID: 28838926
9. Suggest a primary metabolic role for CES1 in the capacity of skin/keratinocytes to mediated biotransformation of penta-ethyl ester prodrug of DTPA. PMID: 27130352
10. These data suggest that infants younger than 3 weeks of age would exhibit significantly lower CES1- and CES2-dependent metabolic clearance compared with older individuals. PMID: 26825642
11. The intestinal transport of oseltamivir, a hCE1 substrate, could be evaluated in subclone #78 cell monolayers. PMID: 27638507
12. An association was identified with a genetic variation in CES1 and early-onset capecitabine-related toxicity. PMID: 28139840
13. Reduced CES1 expression/activity could promote development of METH-PAH. PMID: 28473326
14. These data suggest that CES1 genetic variants and gender are important contributing factors to variability in dabigatran etexilate activation in humans. PMID: 27614009
15. some functional CES1 genetic variants (for example, G143E) may impair ACE inhibitor activation, and consequently affect therapeutic outcomes of ACEI prodrugs. PMID: 26076923
16. HNF4alpha regulated CES1 expression by directly binding to the proximal promoter of CES1. PMID: 27075303
17. We conclude that the -816A>C variant is not associated with interindividual variability in CES1 expression and activity or therapeutic response to ACEI prodrugs PMID: 26915813
18. Our study identified CYP2C19*3 and CES1 rs8192950 as genetic polymorphisms related to recurrent ischemic events in patients with extracranial or intracranial occlusive disease, demonstrating the important roles of CYP2C19 and CES1 in patients treated with clopidogrel PMID: 27450232
19. Data suggest oseltamivir activation is associated with an SNP in CES1 (rs71647871, G143E); in liver from donors with genotype 143G/E activation is 40% of that from donors with genotype 143G/G. Hepatic CES1 expression in females is 17.3% higher than in males; oseltamivir activation rate in females is 27.8% higher than in males. (Liver tissues used were obtained from tissue banks located in the United States.) PMID: 27228223
20. Study confirms previous reports of the CES1P1-CES1 translocation generating the CES1VAR allele with 11 SNPs in the 5'UTR, exon 1, and intron 1 derived from the CES1P1 sequence with decreased CES1 mRNA expression in the human liver by approximately 30% but normal protein expression. PMID: 26871237
21. Study found that CYP2C19*2, *3, and *8 were associated with lower odds of the primary and secondary endpoints in the symptomatic intracranial atherosclerotic medical group compared with wild-type homozygotes; due to the low incidence of CES1 genetic variation, our study was unable to demonstrate any association between CES1 variations and the primary and secondary endpoints PMID: 26587656
22. decreases of CES and CYP3A4 expression and enzymatic activities induced by Fluoxetine are through decreasing PXR and increasing DEC1 in HepG2 cells PMID: 26340669
23. The structure and activity of glycosylated and aglycosylated human CES1 has been determined. PMID: 26657071
24. CES1 c.428G>A single nucleotide variation increases clopidogrel active metabolite concentrations and antiplatelet effects by reducing clopidogrel hydrolysis to inactive metabolites PMID: 25704243
25. CEH is an important regulator in enhancing cholesterol elimination. PMID: 24563511
26. study found an association between two CES1 SNP markers and the occurrence of sadness as a side effect of short-acting methylphenidate PMID: 24350812
27. 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. PMID: 24212379
28. The conversion of 2-oxo-ticlopidine to M1 was further confirmed with recombinant paraoxonase 1 (PON1) and CES1. PMID: 24170778
29. CES1 plays a role in the metabolism of several drugs. PMID: 24141856
30. An influence of carboxylesterase 1 -75 T>G polymorphism on the worsening of appetite reduction with MPH treatment in youths with ADHD. PMID: 22688218
31. 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 PMID: 23936796
32. carboxylesterase I controls RhoA methylation PMID: 23658012
33. Carboxylesterase 1 gene duplication and mRNA expression in adipose tissue are linked to obesity and metabolic function. PMID: 23468884
34. The CES1 SNP rs8192950 AC genotype and rs1968753 GG genotype might be the candidates for risk prediction of antituberculosis drug-induced hepatotoxicity. PMID: 22943824
35. Deficient CES1 catalytic activity resulting from CES1 inhibition. PMID: 23275066
36. Genetic variation in CES1 may be an important determinant of the efficacy of clopidogrel. PMID: 23111421
37. 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. PMID: 22700792
38. 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. PMID: 22588607
39. 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. PMID: 22237548
40. 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 PMID: 22525521
41. High mRNA levels of CES1 is associated with adiposity and lipolysis, thereby contributing to the development of obesity-associated phenotypes. PMID: 21081832
42. 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. PMID: 20975297
43. Report CES1 mediated hydrolysis of heroin, cocaine and CPT-11. PMID: 20649590
44. 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. PMID: 20530478
45. 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. PMID: 19932971
46. A comparison of the substrate specificity of CES1 versus CES2 reveals broad but distinct substrate preferences. PMID: 19508181
47. 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. PMID: 19733552
48. crystal structure bound to analogs of cocaine and heroin PMID: 12679808
49. A serine esterase involved in both drug metabolism and activation. PMID: 12773168
50. Findings indicate that F417 but not L418, L420, or C390 participates in substrate hydrolysis by triacylglycerol hydrolase. PMID: 16282638

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HGNC: 1863

OMIM: 114835

KEGG: hsa:1066

STRING: 9606.ENSP00000353720

UniGene: Hs.558865