CES1 trimer.CES2 hydrolyse COCN to BEG

Stable Identifier
R-HSA-5693691
Type
Reaction [transition]
Species
Homo sapiens
Compartment
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Cocaine (COCN) is an addictive, psychoactive alkaloid that is primarily inactivated by hydrolysis to benzoylecgonine (BEG), the major urinary metabolite of the drug. Human liver carboxylesterases 1 and 2 (CES1 and 2), located in the ER lumen, are involved in the detoxification of xenobiotics and can hydrolyse COCN to BEG (Brzezinski et al. 1994, Pindel et al. 1997). CES1 is functional as a homotrimer or homohexamer (Bencharit et al. 2003) whereas CES2 is monomeric.

Literature References
PubMed ID Title Journal Year
12725862 Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition

Bencharit, S, Morton, CL, Hyatt, JL, Kuhn, P, Danks, MK, Potter, PM, Redinbo, MR

Chem. Biol. 2003
9169443 Purification and cloning of a broad substrate specificity human liver carboxylesterase that catalyzes the hydrolysis of cocaine and heroin

Pindel, EV, Kedishvili, NY, Abraham, TL, Brzezinski, MR, Zhang, J, Dean, RA, Bosron, WF

J. Biol. Chem. 1997
7980644 Purification and characterization of a human liver cocaine carboxylesterase that catalyzes the production of benzoylecgonine and the formation of cocaethylene from alcohol and cocaine

Brzezinski, MR, Abraham, TL, Stone, CL, Dean, RA, Bosron, WF

Biochem. Pharmacol. 1994
Participants
Participant Of
Catalyst Activity
Catalyst Activity
Title
carboxylic ester hydrolase activity of CES1 trimer, CES2 [endoplasmic reticulum lumen]
Physical Entity
Activity
Orthologous Events
Authored
Reviewed
Created