Target intelligence / Profile preview

Liver carboxylesterase 1 (CES1)

Target
CES1
Molecular classification
Enzyme, Carboxylesterase, Serine esterase, Alpha/beta fold hydrolase
01

Overview

Liver carboxylesterase 1 (CES1) is a major human enzyme that belongs to the carboxylesterase family and the alpha/beta fold hydrolase family. It is primarily expressed in the liver and monocytes/macrophages and localized to the endoplasmic reticulum lumen. CES1 catalyzes the hydrolysis of ester and amide bonds in xenobiotics, drugs, and endogenous substrates, playing a crucial role in drug metabolism, detoxification, and lipid processing. Genetic variants can affect drug response, and its inhibition can impair immune function. It is involved in both activating prodrugs and deactivating active drugs.

Other names
hCE-1CES1A1CEHREHTGHEgasynCocaine carboxylesterase
02

Mechanism of action

Hydrolyzes ester and amide bonds in various substrates, including drugs, xenobiotics, and endogenous compounds, leading to activation or deactivation of drugs, detoxification, and modulation of lipid metabolism.

03

Biological functions

Hydrolysis of ester and amide bondsDrug metabolismXenobiotic metabolismLipid processingDetoxificationReverse cholesterol transport
04

Disease associations

Non-Hodgkin lymphomaB-cell lymphocytic leukemiaOrganophosphate poisoning
05

Safety considerations

Genetic variants/polymorphisms altering drug pharmacokinetics/pharmacodynamicsInhibition by organophosphates impairs monocyte tumor-killing activity
06

Interacting drugs

Oseltamivir

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