Gosset Molecular Classification
Enzyme, Hydrolase, Serine hydrolase
Other Names
CES, Carboxylic-ester hydrolase, CES1, CES2
Disease Roles
Carboxylesterase 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.
Mechanism of Action
Hydrolyzes ester, amide, thioester, and carbamate bonds in drugs and xenobiotics, modifying their activity and clearance.
Biological Functions
Hydrolysis of esters
Drug metabolism
Xenobiotic detoxification
Prodrug activation
Prodrug deactivation
Lipid metabolism (potential)
Cholesterol esterification regulation (potential)
Disease Associations
Organophosphate poisoning
Leukemia
Lymphoma
Safety Considerations
- Inter-individual variability due to genetic polymorphisms
- Drug-drug interactions (low risk, but possible)
- Inhibition by organophosphates
- Repression by inflammatory cytokines
Interacting Drugs
Methylphenidate