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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.
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.
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