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Literature summary for 3.1.1.1 extracted from

  • Wierdl, M.; Tsurkan, L.; Hyatt, J.L.; Edwards, C.C.; Hatfield, M.J.; Morton, C.L.; Houghton, P.J.; Danks, M.K.; Redinbo, M.R.; Potter, P.M.
    An improved human carboxylesterase for enzyme/prodrug therapy with CPT-11 (2008), Cancer Gene Ther., 15, 183-192.
    View publication on PubMed

Application

Application Comment Organism
medicine isolation of mutant enzyme hCE1m6, which is 70fold more efficient in cleavage of the antitumor prodrug irinotecan-7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin, i.e. CPT-11, than wild-type. Adenoviral-mediated delivery of mutant enzyme with human tumor cells results in up to 670fold reduction in the IC50 value for CPT-11 Homo sapiens
medicine isolation of mutant enzyme hCE1m6, which is 70fold more efficient in cleavage of the antitumor prodrug irinotecan-7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin, i.e. CPT-11, than wild-type. Adenoviral-mediated delivery of mutant enzyme with human tumor cells results in up to 670fold reduction in the IC50 value for CPT-11 Oryctolagus cuniculus

Protein Variants

Protein Variants Comment Organism
additional information isolation of mutant enzyme hCE1m6, which is 70fold more efficient in cleavage of the antitumor prodrug irinotecan-7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin, i.e. CPT-11, than wild-type Oryctolagus cuniculus
additional information isolation of mutant enzyme hCE1m6, which is 70fold more efficient in cleavage of the antitumor prodrug irinotecan-7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin, i.e. CPT-11, than wild-type. Comparison with rabbit enzyme Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0062
-
irinotecan ratio kcat/Km is 180 per min and mM Oryctolagus cuniculus
0.00625
-
irinotecan mutant hCE1m6, ratio kcat/Km is 19.8 per min and mM Homo sapiens
0.0828
-
irinotecan wild-type, ratio kcat/Km is 0.28 per min and mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P23141 isoform hCE1
-
Oryctolagus cuniculus P12337
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-
liver
-
Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
irinotecan + H2O antitumor prodrug, poor substrate Homo sapiens 7-ethyl-10-hydroxycampothecin + 1,4'-bipiperidine-1'-carboxylic acid
-
?
irinotecan + H2O antitumor prodrug, poor substrate Oryctolagus cuniculus 7-ethyl-10-hydroxycampothecin + 1,4'-bipiperidine-1'-carboxylic acid
-
?