CES1
CES1 (carboxylesterase 1, also known as HMSE, SES1, CEH and CES1A1) is the major liver carboxylesterase, a type-B carboxylesterase/lipase that hydrolyses esters in xenobiotics and in endogenous lipids. It contributes to drug clearance, prodrug activation and cholesterol ester metabolism. Browse Assay Genie's current range of CES1 research reagents below, or read on for the biology behind the target.
CES1 is involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. It hydrolyses aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Among its xenobiotic substrates, it hydrolyses the methyl ester group of cocaine to form benzoylecgonine, and it catalyses the transesterification of cocaine to cocaethylene. It also shows fatty acid ethyl ester synthase activity, converting oleic acid to ethyloleate. The NCBI Gene summary describes it as the major liver enzyme in drug clearance, acting on substrates such as cocaine and heroin.
The CES1 enzyme also acts on endogenous lipids. It converts monoacylglycerides to free fatty acids and glycerol, and hydrolyses 2-arachidonoylglycerol and prostaglandins. It hydrolyses cellular cholesteryl esters to free cholesterol and promotes reverse cholesterol transport at two points. It first allows free cholesterol efflux from macrophages to extracellular acceptors. It then releases free cholesterol from lipoprotein-delivered cholesteryl esters in the liver, for bile acid synthesis or direct secretion into bile. The protein is found in the endoplasmic reticulum lumen, the cytoplasm and lipid droplets. The carboxylesterase family may also play a role in the blood-brain barrier system.
The human CES1 gene belongs to the HGNC carboxylesterases group, and the protein belongs to the type-B carboxylesterase/lipase family. Its previous name was carboxylesterase 1 (monocyte/macrophage serine esterase 1), and earlier symbols include CES2 and HMSE1. Three transcript variants encode three isoforms. Mutations in the gene cause carboxylesterase 1 deficiency. The mouse ortholog is Ces1d and the rat ortholog is Ces1e. Related family members include CES2 and CES5A.
CES1 is the major liver enzyme in drug clearance, hydrolysing xenobiotics and activating ester and amide prodrugs.
It hydrolyses substrates such as cocaine and heroin, and catalyses cocaine transesterification to cocaethylene.
CES1 hydrolyses cholesteryl esters and monoacylglycerides, and supports reverse cholesterol transport from macrophages to the liver.
Mutations in the CES1 gene cause carboxylesterase 1 deficiency, making it relevant to studies of variation in esterase function.
CES1 hydrolyses aromatic and aliphatic esters. It detoxifies xenobiotics, activates ester and amide prodrugs, and acts on lipids including monoacylglycerides, 2-arachidonoylglycerol, prostaglandins and cholesteryl esters. In the liver it releases free cholesterol for bile acid synthesis or secretion into bile.
CES1 is also known as HMSE, HMSE1, SES1, CEH, CES1A1 and CES1A2, and earlier as CES2. Its former name was carboxylesterase 1 (monocyte/macrophage serine esterase 1). UniProt lists it as liver carboxylesterase 1. Three transcript variants encode three isoforms.
The mouse ortholog is Ces1d and the rat ortholog is Ces1e. Mutations in the human CES1 gene cause carboxylesterase 1 deficiency. Orthologs can differ in substrate handling, so check the datasheet of any product for its validated reactivity.
Other carboxylesterase family members with products at Assay Genie.
Gene and protein annotations from HGNC, NCBI Gene and UniProt P23141; product specifications from Assay Genie datasheets.