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Carboxylesterase (None)
- Target
- None
- Molecular classification
- Enzyme, Hydrolase, Serine hydrolase
01
Overview
Carboxylesterases are a family of serine-dependent hydrolase enzymes with broad substrate specificity. They catalyze the hydrolysis of carboxylic esters, amides, thioesters, and carbamates. These enzymes are widely distributed in mammalian tissues and play critical roles in both detoxification of xenobiotics and activation or deactivation of various drugs, including many prodrugs. Key isoforms include CES1 (primarily in the liver) and CES2 (primarily in the intestine). Genetic polymorphisms can significantly affect enzyme activity leading to inter-individual variability in drug response.
- Other names
- CESCarboxylic-ester hydrolaseCES1CES2
02
Mechanism of action
Hydrolyzes ester, amide, thioester, and carbamate bonds in drugs and xenobiotics, modifying their activity and clearance.
03
Biological functions
Hydrolysis of estersDrug metabolismXenobiotic detoxificationProdrug activationProdrug deactivationLipid metabolism (potential)Cholesterol esterification regulation (potential)
04
Disease associations
Organophosphate poisoningLeukemiaLymphoma
05
Safety considerations
Inter-individual variability due to genetic polymorphismsDrug-drug interactions (low risk, but possible)Inhibition by organophosphatesRepression by inflammatory cytokines
06
Interacting drugs
Methylphenidate
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