MGP Database

MGP000528

UniProt Annotations

Entry Information
Gene Namecarboxylesterase 1
Protein EntryEST1_HUMAN
UniProt IDP23141
SpeciesHuman
Comments
Comment typeDescription
Alternative ProductsEvent=Alternative splicing; Named isoforms=3; Name=1; IsoId=P23141-1; Sequence=Displayed; Name=2; IsoId=P23141-2; Sequence=VSP_021026; Name=3; IsoId=P23141-3; Sequence=VSP_047158;
Biophysicochemical PropertiesKinetic parameters: KM=106.6 uM for p-nitrophenyl acetate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=775.7 uM for L-methylphenidate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=663.5 uM for D-methylphenidate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=116 uM for cocaine {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=43 mM for ethanol {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=0.8 mM for 4-methylumbelliferyl acetate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=6.3 mM for heroin {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; KM=8.3 mM for 6-monoacetylmorphine {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; Vmax=493.9 nmol/min/mg enzyme with p-nitrophenyl acetate as substrate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; Vmax=1701.1 pmol/min/mg enzyme with L-methylphenidate as substrate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; Vmax=177.2 pmol/min/mg enzyme with D-methylphenidate as substrate {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062}; pH dependence: Optimum pH is 6.5. {ECO:0000269|PubMed:18485328, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443, ECO:0000269|PubMed:9490062};
Catalytic Activity4-methylumbelliferyl acetate + H(2)O = 4- methylumbelliferone + acetate.
Catalytic ActivityA carboxylic ester + H(2)O = an alcohol + a carboxylate. {ECO:0000255|PROSITE-ProRule:PRU10039}.
Enzyme RegulationActivated by CHAPS. {ECO:0000269|PubMed:9490062}.
FunctionInvolved 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. {ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:9169443}.
PtmCleavage of the signal sequence can occur at 2 positions, either between Trp-17 and Gly-18 or between Gly-18 and His-19.
PtmContains sialic acid.
Sequence CautionSequence=AAA83932.1; Type=Frameshift; Positions=301, 312, 318, 383, 391; Evidence={ECO:0000305};
SimilarityBelongs to the type-B carboxylesterase/lipase family. {ECO:0000305}.
Subcellular LocationEndoplasmic reticulum lumen {ECO:0000269|PubMed:10562416}.
SubunitHomotrimer and homohexamer. Binds to beta-glucuronidase. {ECO:0000269|PubMed:12679808, ECO:0000269|PubMed:12725862, ECO:0000269|PubMed:7980644, ECO:0000269|PubMed:8597091}.
Tissue SpecificityExpressed predominantly in liver with lower levels in heart and lung. {ECO:0000269|PubMed:10562416}.
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