Carboxylesterase 1 (CES1)

Carboxylesterase 1 (CES1) is a major human serine hydrolase enzyme belonging to the alpha/beta-hydrolase fold family. It is highly expressed in the liver, with additional distribution in the gastrointestinal tract, lung, and other tissues. CES1 catalyzes the hydrolysis of a wide variety of endogenous and exogenous esters, including drugs, prodrugs, environmental toxicants, and lipid molecules. It plays a critical role in phase I drug metabolism, activating certain prodrugs (such as oseltamivir and dabigatran), detoxifying xenobiotics, and regulating lipid and cholesterol homeostasis. CES1 activity shows substantial genetic and inter-individual variability, which can significantly influence therapeutic outcomes and toxicity of many drugs, especially those commonly prescribed or used as prodrugs. Carboxylesterase 1 is considered a clinically relevant therapeutic target, and its function or dysfunction is implicated in cancer, infections, chemical toxicity, and metabolic diseases.

Other names

CarboxylesteraseCarboxylesterase 1A1CES1A1hCE-1B-esteraseAli-esteraseCocaine esteraseProcaine esteraseCarboxylesterase BCAP-hydrolyzing enzymeCarboxyesteraseCarboxylester lipaseCarboxylate esteraseCarboxylic ester hydrolaseIsocarboxazid amidaseNaproxen esteraseNon-specific carboxylesteraseSerine esterase 1 (SES1)Monocyte esteraseCholesterol ester hydrolase (CEH)

Hydrolysis (inactivation or activation of drugs through catalytic cleavage of ester/amide/thioester/carbamate linkages) Prodrug activation (conversion of prodrug to active metabolite) Detoxification (catalysis of xenobiotic metabolism for excretion)