Carboxylesterase 2 (CES2)

Carboxylesterase 2 (CES2) is a member of the carboxylesterase family and belongs to the multigene family. Carboxylesterase 2 is responsible for the hydrolysis of ester- and amide-bond-containing drugs such as cocaine and beroin. It also serves to hydrolyze long-chain fatty acid esters and thioesters. It is speculated that carboxylesterases may play a role in lipid metabolism and the blood-brain barrier system and together with isform 1, are a serine esterase involved in both drug metabolism and activation. Human carboxylesterase 2 is commonly expressed in tumor tissues and irinotecan, a topoisomerase I inhibitor commonly used in the treatment of many solid tumors.

Carboxylesterase 2 (CES2) Related Areas

Enzyme>>Lipid Metabolism Enzymes>>CES2/Carboxylesterase 2

Cardiovascular>>Lipid Metabolism>>Lipid Metabolism Enzymes>>CES2/Carboxylesterase 2

Carboxylesterase 2 (CES2) Alternative Names

CES2, Carboxylesterase 2, CE-2, CES2A1, PCE-2, iCE [Homo sapiens]

Ces2, Carboxylesterase 2, ces2A3 [Mus musculus]

Summaries for Carboxylesterase 2 (CES2)

Entrez Gene summary for CES2:

This CES2 gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or transesterification of various xenobiotics, such as cocaine and heroin, and endogenous substrates with ester, thioester, or amide bonds. They may participate in fatty acyl and cholesterol ester metabolism, and may play a role in the blood-brain barrier system. The protein encoded by this CES2 gene is the major intestinal enzyme and functions in intestine drug clearance. Alternatively spliced transcript variants have been found for this gene.[provided by RefSeq, Oct 2010]

OMIM - description for Carboxylesterase 2:

Carboxylesterases (CESs; EC 3.1.1.1) hydrolyze ester groups of drugs and toxins. CES2 specifically catalyzes the hydrolysis of the benzoyl group of cocaine and the acetyl groups of 4-methylumbelliferyl acetate, heroin, and 6-monoacetylmorphine. CES2 differs from another liver carboxylesterase, CES1 (114835), in drug ester substrate specificity. See 114835 for additional background information on carboxylesterases.

Wikipedia summary for Carboxylesterase 2:

Carboxylesterase 2 is an enzyme that in humans is encoded by the CES2 gene. It is a member of the alpha/beta fold hydrolase family.
Carboxylesterase 2 is a member of a large multigene family. The enzymes encoded by these genes are responsible for the hydrolysis of ester- and amide-bond-containing drugs such as cocaine and heroin. They also hydrolyze long-chain fatty acid esters and thioesters. The specific function of this enzyme has not yet been determined; however, it is speculated that carboxylesterases may play a role in lipid metabolism and/or the blood–brain barrier system. Two alternatively spliced transcript variants encoding distinct isoforms have been found for this gene.[

Human Carboxylesterase 2 (CES2) Protein General Information

 

• Protein names: Carboxylesterase 2, Short name=CE-2
• Sequence length
• Catalytic activity: Cocaine + H2O = ecgonine methyl ester + benzoate.
  A carboxylic ester + H2O = an alcohol + a carboxylate.
  4-methylumbelliferyl acetate + H2O = 4-methylumbelliferone + acetate.
• Sequence similarities: Carboxylesterase 2 belongs to the type-B carboxylesterase/lipase family.
• Post-translational modification: Glycosylated.
• Subunit structure: Monomer.
• Subcellular location: Endoplasmic reticulum lumen
• Biophysicochemical properties: Kinetic parameters:
  KM=0.39 mM for cocaine
  KM=0.15 mM for 4-methylumbelliferyl acetate
  KM=6.8 mM for heroin
  KM=0.13 mM for 6-monoacetylmorphine
• Tissue specificity: Carboxylesterase 2 is preferentially expressed in intestine with moderate expression in liver. Within the intestine, highest expression is found in small intestine with lower expression in colon and rectum.
• Sequence caution: The sequence AAH32095.1 differs from that shown. Reason: Erroneous initiation. Translation N-terminally shortened.
  The sequence AAW29943.1 differs from that shown. Reason: Erroneous initiation. Translation N-terminally shortened.
  The sequence CAD28531.1 differs from that shown. Reason: Erroneous initiation. Translation N-terminally shortened.
  The sequence CAD98009.1 differs from that shown. Reason: Erroneous initiation. Translation N-terminally shortened.

General information above from UniProt

Function for Carboxylesterase 2 (CES2) Protein

UniProtKB:

Carboxylesterase 2 is involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Carboxylesterase 2 shows high catalytic efficiency for hydrolysis of cocaine, 4-methylumbelliferyl acetate, heroin and 6-monoacetylmorphine.

Genatlas:

• Carboxylesterase 2 may be playing a role in lipid metabolism and/or the blood-brain barrier system