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Literature summary for 3.1.1.1 extracted from

  • Hatfield, M.J.; Tsurkan, L.; Garrett, M.; Shaver, T.M.; Hyatt, J.L.; Edwards, C.C.; Hicks, L.D.; Potter, P.M.
    Organ-specific carboxylesterase profiling identifies the small intestine and kidney as major contributors of activation of the anticancer prodrug CPT-11 (2011), Biochem. Pharmacol., 81, 24-31.
    View publication on PubMedView publication on EuropePMC
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Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
duodenum low expression Homo sapiens
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ileum low expression Homo sapiens
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jejunum low expression Homo sapiens
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kidney low expression Homo sapiens
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liver high expression Homo sapiens
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lung low expression Homo sapiens
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small intestine high expression Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CPT-11 + H2O CPT-11 is also named irinotecan, i.e. 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. Human intestine carboxylesterase demonstrates the most efficient kinetic parameters for CPT-11 hydrolysis to the active metabolite SN-38 Homo sapiens SN-38 + 1,4'-bipiperidine-1'-carboxylic acid + CO2
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Synonyms

Synonyms Comment Organism
CE1 hepatic carboxylesterase Homo sapiens
CES1 hepatic carboxylesterase Homo sapiens
hiCE intestinal carboxylaesterase Homo sapiens

General Information

General Information Comment Organism
physiological function hepatic carboxylesterase CE1 plays a significant role in CPT-11 hydrolysis even though it is up to 100fold less efficient at drug activation than intestinal carboxylesterase. The drug activation in the intestine and kidney are likely major contributors to SN-38 production in vivo Homo sapiens