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 | 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 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P23141 | isoform hCE1 | - |
Oryctolagus cuniculus | P12337 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
liver | - |
Oryctolagus cuniculus | - |
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 | - |
? |