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Carboxylesterase 3 (liver carboxylesterase 31 homolog, CES3)
Function:
- role in the detoxification of xenobiotics & in the activation of ester & amide prodrugs
- low catalytic efficiency for hydrolysis of CPT-11 (7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin), a prodrug for camptothecin used in cancer therapeutics
carboxylic ester + H2O an alcohol + carboxylate
Kinetic parameters:
- KM=137 uM for CPT-11
- KM=460 uM for 7-ethyl-10-[4-(1-piperidino)-1-amino]-carbonyloxycamptothecin
Structure:
- belongs to the type-B carboxylesterase/lipase family
- N-glycosylated
Compartment: endoplasmic reticulum lumen (putative)
Expression: expressed in liver, colon & small intestine
General
carboxylase (carboxylic ester hydrolase)
glycoprotein
Properties
SIZE: entity length = 571 aa
MW = 62 kD
MOTIF: signal sequence {1-26}
cysteine residue {C97}
MODIFICATION: cysteine residue {C124}
N-glycosylation site {N105}
cysteine residue {C124}
MODIFICATION: cysteine residue {C97}
serine residue {S229}
cysteine residue {C281}
MODIFICATION: cysteine residue {C292}
active site
cysteine residue {C292}
MODIFICATION: cysteine residue {C281}
glutamate residue {E347}
histidine residue {H460}
ER retention {568-571}
Database Correlations
OMIM 605279
UniProt Q6UWW8
Pfam PF00135
ENZYME 3.1.1.1
References
UniProt :accession Q6UWW8