CES1 trimer.CES2 hydrolyse COCN to BEG

Stable Identifier
Reaction [transition]
Homo sapiens
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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
9169443 Purification and cloning of a broad substrate specificity human liver carboxylesterase that catalyzes the hydrolysis of cocaine and heroin

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

J. Biol. Chem. 1997
12725862 Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition

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

Chem. Biol. 2003
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

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

Biochem. Pharmacol. 1994
Catalyst Activity

carboxylic ester hydrolase activity of CES1 trimer, CES2 [endoplasmic reticulum lumen]

Orthologous Events
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