Recombinant Human Liver Carboxylesterase 1 (CES1) Protein (His)

Name: Recombinant Human Liver Carboxylesterase 1 (CES1) Protein (His)
Brand: Beta LifeScience
SKU: BLC-07104P
Availability: InStock

Greater than 85% as determined by SDS-PAGE.

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Product Overview

Description	Recombinant Human Liver Carboxylesterase 1 (CES1) Protein (His) is produced by our Baculovirus expression system. This is a full length protein.
Purity	Greater than 85% as determined by SDS-PAGE.
Uniprotkb	P23141
Target Symbol	CES1
Species	Homo sapiens (Human)
Expression System	Baculovirus
Tag	C-6His
Target Protein Sequence	GHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAKKAVEKPPQTEHIEL
Expression Range	18-567aa
Protein Length	Full Length of Mature Protein
Mol. Weight	66.3 kDa
Research Area	Cardiovascular
Form	Liquid or Lyophilized powder
Buffer	Liquid form: default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. Lyophilized powder form: the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution	Briefly centrifuged the vial prior to opening to bring the contents to the bottom. Reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. It is recommended to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. The default final concentration of glycerol is 50%.
Storage	1. Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4°C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20°C/-80°C. Protein in lyophilized powder form is stable for up to 12 months at -20°C/-80°C.
Notes	Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Target Details

Target Function	Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine. Catalyzes the transesterification of cocaine to form cocaethylene. Displays fatty acid ethyl ester synthase activity, catalyzing the ethyl esterification of oleic acid to ethyloleate. Converts monoacylglycerides to free fatty acids and glycerol. Hydrolyzes of 2-arachidonoylglycerol and prostaglandins. Hydrolyzes cellular cholesteryl esters to free cholesterols and promotes reverse cholesterol transport (RCT) by facilitating both the initial and final steps in the process. First of all, allows free cholesterol efflux from macrophages to extracellular cholesterol acceptors and secondly, releases free cholesterol from lipoprotein-delivered cholesteryl esters in the liver for bile acid synthesis or direct secretion into the bile.
Subcellular Location	Endoplasmic reticulum lumen. Cytoplasm. Lipid droplet.
Protein Families	Type-B carboxylesterase/lipase family
Database References	HGNC: 1863 OMIM: 114835 KEGG: hsa:1066 STRING: 9606.ENSP00000353720 UniGene: Hs.558865
Tissue Specificity	Expressed predominantly in liver with lower levels in heart and lung. Expressed in macrophages.

Gene Functions References

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
Which selectively amplified CES1A1 and, if present, also CES1A2. PMID: 29457755
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
Anordrin is predominantly catalyzed by CES1 and CES2 to generate the main active metabolite, anordiol. PMID: 28532270
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
The frequencies of SNVs with a potential functional impact were below 0.02 suggesting limited pharmacogenetic potential for CES1 genotyping. PMID: 28786738
none of the selected variations of CES1 had a clinically relevant impact on the metabolism of enalapril PMID: 28639420
Study revealed that several nsSNPs significantly impaired CES1 activity on the metabolism of the CES1 substrates enalapril, clopidogrel, and sacubitril. PMID: 28838926
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
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
The intestinal transport of oseltamivir, a hCE1 substrate, could be evaluated in subclone #78 cell monolayers. PMID: 27638507
An association was identified with a genetic variation in CES1 and early-onset capecitabine-related toxicity. PMID: 28139840
Reduced CES1 expression/activity could promote development of METH-PAH. PMID: 28473326
These data suggest that CES1 genetic variants and gender are important contributing factors to variability in dabigatran etexilate activation in humans. PMID: 27614009
some functional CES1 genetic variants (for example, G143E) may impair ACE inhibitor activation, and consequently affect therapeutic outcomes of ACEI prodrugs. PMID: 26076923
HNF4alpha regulated CES1 expression by directly binding to the proximal promoter of CES1. PMID: 27075303
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
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
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
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
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
decreases of CES and CYP3A4 expression and enzymatic activities induced by Fluoxetine are through decreasing PXR and increasing DEC1 in HepG2 cells PMID: 26340669
The structure and activity of glycosylated and aglycosylated human CES1 has been determined. PMID: 26657071
CES1 c.428G>A single nucleotide variation increases clopidogrel active metabolite concentrations and antiplatelet effects by reducing clopidogrel hydrolysis to inactive metabolites PMID: 25704243
CEH is an important regulator in enhancing cholesterol elimination. PMID: 24563511
study found an association between two CES1 SNP markers and the occurrence of sadness as a side effect of short-acting methylphenidate PMID: 24350812
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
The conversion of 2-oxo-ticlopidine to M1 was further confirmed with recombinant paraoxonase 1 (PON1) and CES1. PMID: 24170778
CES1 plays a role in the metabolism of several drugs. PMID: 24141856
An influence of carboxylesterase 1 -75 T>G polymorphism on the worsening of appetite reduction with MPH treatment in youths with ADHD. PMID: 22688218
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
carboxylesterase I controls RhoA methylation PMID: 23658012
Carboxylesterase 1 gene duplication and mRNA expression in adipose tissue are linked to obesity and metabolic function. PMID: 23468884
The CES1 SNP rs8192950 AC genotype and rs1968753 GG genotype might be the candidates for risk prediction of antituberculosis drug-induced hepatotoxicity. PMID: 22943824
Deficient CES1 catalytic activity resulting from CES1 inhibition. PMID: 23275066
Genetic variation in CES1 may be an important determinant of the efficacy of clopidogrel. PMID: 23111421
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
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
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
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
High mRNA levels of CES1 is associated with adiposity and lipolysis, thereby contributing to the development of obesity-associated phenotypes. PMID: 21081832
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
Report CES1 mediated hydrolysis of heroin, cocaine and CPT-11. PMID: 20649590
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
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
A comparison of the substrate specificity of CES1 versus CES2 reveals broad but distinct substrate preferences. PMID: 19508181
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
crystal structure bound to analogs of cocaine and heroin PMID: 12679808
A serine esterase involved in both drug metabolism and activation. PMID: 12773168
Findings indicate that F417 but not L418, L420, or C390 participates in substrate hydrolysis by triacylglycerol hydrolase. PMID: 16282638

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Proteins are sensitive to heat, and freeze-drying can preserve the activity of the majority of proteins. It improves protein stability, extends storage time, and reduces shipping costs. However, freeze-drying can also lead to the loss of the active portion of the protein and cause aggregation and denaturation issues. Nonetheless, these adverse effects can be minimized by incorporating protective agents such as stabilizers, additives, and excipients, and by carefully controlling various lyophilization conditions.

Commonly used protectant include saccharides, polyols, polymers, surfactants, some proteins and amino acids etc. We usually add 8% (mass ratio by volume) of trehalose and mannitol as lyoprotectant. Trehalose can significantly prevent the alter of the protein secondary structure, the extension and aggregation of proteins during freeze-drying process; mannitol is also a universal applied protectant and fillers, which can reduce the aggregation of certain proteins after lyophilization.

Our protein products do not contain carrier protein or other additives (such as bovine serum albumin (BSA), human serum albumin (HSA) and sucrose, etc., and when lyophilized with the solution with the lowest salt content, they often cannot form A white grid structure, but a small amount of protein is deposited in the tube during the freeze-drying process, forming a thin or invisible transparent protein layer.

Reminder: Before opening the tube cap, we recommend that you quickly centrifuge for 20-30 seconds in a small centrifuge, so that the protein attached to the tube cap or the tube wall can be aggregated at the bottom of the tube. Our quality control procedures ensure that each tube contains the correct amount of protein, and although sometimes you can't see the protein powder, the amount of protein in the tube is still very precise.

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