Carboxylesterase enzyme (CES (for main isoforms: CES1, CES2))

Endogenous brain esterase enzymes refer to a variety of serine hydrolase enzymes within brain tissue that catalyze the hydrolysis of ester bonds in endogenous substrates (such as neurotransmitters) and xenobiotics (such as ester-containing drugs and prodrugs)[2][5][6]. Key members of this group include carboxylesterases (such as CES1 and CES2), cholinesterases (such as acetylcholinesterase and butyrylcholinesterase), and others like paraoxonases and certain lipid esterases[2][5][6][7]. These enzymes play critical roles in neurotransmitter regulation (acetylcholinesterase terminates synaptic transmission by hydrolyzing acetylcholine[3]), drug metabolism (activation and deactivation of prodrugs and detoxification of toxins), and lipid signaling (metabolism of endocannabinoids by enzymes like monoacylglycerol lipase and ABHD6/ABHD12[4]). Their activities are highly relevant to therapeutic drug design, neurodegenerative and metabolic disease, and toxicity. The term "endogenous brain esterase enzymes" is not a single specific target but instead a heterogeneous group, and thus is not a canonical molecular target but rather an umbrella functional description, which makes it scientifically imprecise and impractical as a therapeutic target entity[2][4][5].

Other names

EsteraseCarboxylesteraseAcetylcholinesteraseButyrylcholinesteraseParaoxonaseCholinesterase

Enzyme inhibition (irreversible and reversible), Substrate hydrolysis (prodrug activation or deactivation), Modulation of neurotransmitter levels