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Literature summary for 3.1.1.1 extracted from

  • Sanghani, S.P.; Quinney, S.K.; Fredenburg, T.B.; Davis, W.I.; Murry, D.J.; Bosron, W.F.
    Hydrolysis of irinotecan and its oxidative metabolites, 7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin and 7-ethyl-10-[4-(1-piperidino)-1-amino]-carbonyloxycamptothecin, by human carboxylesterases CES1A1, CES2, and a newly expressed carboxylesterase isoenzyme, CES3 (2004), Drug Metab. Dispos., 32, 505-511.
    View publication on PubMed

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.001
-
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES2 Homo sapiens
0.0032
-
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES2 Homo sapiens
0.039
-
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES1A1 Homo sapiens
0.08
-
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES1A1 Homo sapiens
0.137
-
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C Homo sapiens
0.27
-
7-ethyl-10-(4-N-(5-aminopentanoic acid)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES2 Homo sapiens
0.46
-
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin pH 7.0, 37°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
60000
-
x * 60000, SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoform CES3, expression in baculoviral system
-
Homo sapiens
-
isoforms CES1A1, CES2
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
5.8
-
pH 7.0, 37°C Homo sapiens
6.6
-
pH 7.0, 37°C, isoform CES1A1 Homo sapiens
120
-
pH 7.0, 37°C, isoform CES2 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin + H2O i.e. NPC Homo sapiens 7-ethyl-10-hydroxycampothecin + 4-aminopiperidine-1-carboxylic acid
-
?
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin + H2O i.e. irinotecan, CPT-11 Homo sapiens 7-ethyl-10-hydroxycampothecin + 1,4'-bipiperidine-1'-carboxylic acid
-
?
7-ethyl-10-(4-N-(5-aminopentanoic acid)-1-piperidino)carbonyloxycampothecin + H2O i.e. APC Homo sapiens 7-ethyl-10-hydroxycampothecin + 4-((4-carboxybutyl)amino)piperidine-1-carboxylic acid
-
?

Subunits

Subunits Comment Organism
? x * 60000, SDS-PAGE Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.000003
-
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES1A1 Homo sapiens
0.000015
-
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C Homo sapiens
0.00008
-
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES1A1 Homo sapiens
0.00027
-
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES2 Homo sapiens
0.00041
-
7-ethyl-10-(4-N-(5-aminopentanoic acid)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES2 Homo sapiens
0.004
-
7-ethyl-10-(4-(1-piperidino)-1-amino)carbonyloxycampothecin pH 7.0, 37°C Homo sapiens
0.017
-
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycampothecin pH 7.0, 37°C, isoform CES2 Homo sapiens