Target intelligence / Profile preview

Carboxylesterase 5A (CES5A)

Target
CES5A
Molecular classification
Enzyme, Serine hydrolase, Carboxylesterase family, α/β hydrolase fold protein
01

Overview

Carboxylesterase 5A (CES5A) is an enzyme from the carboxylesterase superfamily that catalyzes the hydrolysis or transesterification of a wide variety of esters, including drugs, xenobiotics, and endogenous lipid substrates[1][3]. CES5A is encoded by the CES5A gene on human chromosome 16 and is structurally similar to other carboxylesterases but is distinguished by its secretion into body fluids such as urine and male reproductive fluids, and by several isoforms resulting from alternative splicing[1][3]. Its physiological roles include detoxification of foreign compounds, regulation of pheromonal activity (notably in some non-human mammals), lipid metabolism, and possibly neuroprotection from xenobiotics[1]. Unlike more widely studied family members CES1 and CES2, CES5A’s detailed substrate specificity and involvement in clinically significant drug metabolism are still being investigated.

Other names
Carboxylesterase 5ACES5ACES7cauxinFLJ31547CES4C1CES5carboxylesterase-like urinary excreted protein homologepididymis luminal protein 126HEL126
02

Mechanism of action

Catalyzes hydrolysis and transesterification of carboxylesters, thioesters, and aromatic amides Detoxifies and metabolizes some xenobiotics (including certain narcotics and clinical drugs) May activate or inactivate prodrugs as part of drug metabolism pathways

03

Biological functions

Xenobiotic metabolism (hydrolysis and transesterification of drugs and endogenous esters)Lipid metabolism, including cholesterol and fatty acid metabolismDrug detoxification and biotransformationPotential regulation of male reproductive fluid compositionRegulation of urinary pheromone levels (especially in some mammals)Protection of neural tissue from drugs and xenobiotics
04

Disease associations

Drug detoxification/Drug metabolism (potential pharmacokinetics impact)Other (biomarker in specific tissues/fluids; links to reproductive or neurological effects are under investigation)
05

Safety considerations

Limited data on safety concerns specific to CES5A inhibition or modulationPotential risk of altered drug metabolism or detoxification if CES5A activity is inhibited, but clinical relevance uncertain due to redundancy and tissue specificity in carboxylesterase family
06

Interacting drugs

No specific drugs uniquely targeting CES5A are currently well established in humans; carboxylesterase inhibitors or substrates may have off-target effects, but CES5A’s specific substrate profile and key clinical drug interactions remain underexplored compared to CES1 or CES2
07

Biomarkers

Elevated in urine (notably, as cauxin in cats) and in some reproductive fluids (potential as tissue/fluid-specific biomarker)Use as biomarker in humans remains poorly defined

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