CES2

CES2

Target · Carboxylesterase

CES2 Carboxylesterase 2 · Cocaine esterase

CES2 (carboxylesterase 2, also known as cocaine esterase, CE-2, iCE or CES2A1) is an endoplasmic reticulum enzyme of the type-B carboxylesterase/lipase family. It hydrolyses xenobiotics, ester and amide prodrugs and endogenous lipids, and is the major intestinal carboxylesterase. Browse Assay Genie's current range of CES2 research reagents below, or read on for the biology behind the target.

Endoplasmic reticulum lumenXenobiotic and prodrug hydrolysisMajor intestinal enzyme
559 aa
Protein length
~62 kDa
Molecular weight
16q22.1
Gene locus
EC 3.1.1.84
Enzyme class
Target information

What is CES2 (carboxylesterase 2)?

CES2 is involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. It shows high catalytic efficiency for the hydrolysis of cocaine, 4-methylumbelliferyl acetate, heroin and 6-monoacetylmorphine, and it also hydrolyses aspirin and substrates with a large alcohol group and a small acyl group. Among endogenous substrates, it acts on lipids such as triacylglycerol, converts monoacylglycerides to free fatty acids and glycerol, and hydrolyses 2-arachidonoylglycerol and prostaglandins.

The CES2 gene encodes a member of the large carboxylesterase family, whose members hydrolyse or transesterify xenobiotics and endogenous substrates containing ester, thioester or amide bonds. The protein is a type-B carboxylesterase/lipase family member and sits in the lumen of the endoplasmic reticulum. The family may participate in fatty acyl and cholesterol ester metabolism and may play a role in the blood-brain barrier system. Alternatively spliced transcript variants have been described for this gene. HGNC places it in the carboxylesterases gene group, and the mouse and rat orthologues are both named Ces2c.

NCBI describes the CES2 protein as the major intestinal enzyme, functioning in intestinal drug clearance. This makes it a frequent subject in pharmacology and drug metabolism, particularly where prodrug activation is concerned. The gene was previously named carboxylesterase 2 (intestine, liver), and the enzyme is also listed as cocaine esterase, reflecting one of its best-characterised substrates. Related family members include CES1 and CES5A.

Drug metabolism research

CES2 hydrolyses ester and amide prodrugs, so it is central to studying how such compounds are activated and cleared.

Intestinal drug clearance

As the major intestinal carboxylesterase, CES2 functions in intestine drug clearance and is relevant to first-pass processing of orally administered compounds.

Xenobiotic detoxification

CES2 hydrolyses substrates including cocaine, heroin, 6-monoacetylmorphine and aspirin, making it useful for detoxification studies.

Lipid metabolism studies

CES2 acts on triacylglycerol, monoacylglycerides, 2-arachidonoylglycerol and prostaglandins, linking it to fatty acyl and lipid processing.

Background

CES2 frequently asked questions

What does CES2 do?

CES2 is a carboxylesterase that hydrolyses ester, thioester and amide bonds. It detoxifies xenobiotics such as cocaine and heroin, activates ester and amide prodrugs, and acts on endogenous lipids including triacylglycerol, 2-arachidonoylglycerol and prostaglandins. It is the major intestinal enzyme of its family.

What other names does CES2 go by?

CES2 is the HGNC symbol for carboxylesterase 2. UniProt lists the protein as cocaine esterase, and aliases include CE-2, iCE and CES2A1. An earlier gene name was carboxylesterase 2 (intestine, liver). Alternatively spliced transcript variants have been reported for the gene.

Does CES2 have orthologues in other species?

Yes. The data list Ces2c as the mouse and rat orthologue of human CES2. The protein belongs to the type-B carboxylesterase/lipase family and the wider carboxylesterase gene group; check the datasheet of any product for its validated reactivity.

Explore

Related targets

Other carboxylesterase family members involved in xenobiotic and lipid ester hydrolysis.

Gene and protein annotations from HGNC, NCBI Gene and UniProt O00748; product specifications from Assay Genie datasheets.

CES2 Product listing