Target intelligence / Profile preview

Carboxylesterase 4A (CES4A)

Target
CES4A
Molecular classification
Enzyme, Carboxylesterase family, α/β hydrolase fold superfamily
01

Overview

Carboxylesterase 4A (CES4A) is an enzyme that belongs to the mammalian carboxylesterase superfamily responsible for hydrolyzing and transesterifying a wide array of compounds, including pharmaceuticals (such as cocaine and heroin), dietary and environmental xenobiotics, and endogenous lipids (such as cholesterol esters and fatty acyl esters). CES4A is expressed as a secreted enzyme and may have functions in the blood-brain barrier and cerebrospinal fluid, contributing to detoxification and protection in neural and other tissues. Its exact role in human metabolism is still emerging compared to related family members (CES1, CES2), but it is presumed to be relevant to drug activation, clearance, and metabolic homeostasis. Multiple transcript variants and isoforms have been identified, although not all have been fully characterized. Research into substrate specificity, biological relevance, and regulation is ongoing, particularly regarding its impact on drug metabolism and possible disease associations. If more structured details on substrate, interacting drugs, or biomarkers are needed, additional targeted proteomic or pharmacogenomic sources may be required.

Other names
CES6CES8carboxylesterase 6
02

Mechanism of action

Hydrolysis of prodrugs to active forms. Detoxification by transforming active agents to inactive or less toxic metabolites. Transesterification (changing ester groups) of drugs and endogenous molecules.

03

Biological functions

Hydrolysis of esters, thioesters, and amidesDetoxification of drugs and xenobioticsMetabolism of fatty acyl and cholesterol estersPotential role in blood-brain barrier and cerebrospinal fluid function
04

Disease associations

Cancer (reported DNA methylation changes and transcriptional impact)Involvement in Cauda Equina Syndrome and Schwartz-Jampel Syndrome type 1 (GeneCards disease association)Other (possible roles in metabolic and neurological conditions)
05

Safety considerations

Possible impact on drug efficacy and toxicity due to metabolism variabilityPolymorphisms and expression level differences may influence individual drug response and adverse effectsUnclear contribution to specific safety concerns related to CES4A itself (requires more research)
06

Interacting drugs

cocaine

2 more in the full profile.

07

Biomarkers

None established in these sources; carboxylesterases can be potential pharmacogenetic or efficacy biomarkers in drug metabolism research

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