Pub. Date : 1997 Jun
PMID : 9241661
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Identification of the polymorphically expressed CYP2C19 and the wild-type CYP2C9-ILE359 allele as low-Km catalysts of cyclophosphamide and ifosfamide activation. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 2 | With cyclophosphamide as substrate, CYP2C19 had the lowest apparent Km, followed by CYP2C9, CYP2C18 and CYP2C8, whereas in the case of ifosfamide, the rank order was: Km CYP2C19 < CYP2C18 < CYP2C9 < CYP2C8. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 3 | With cyclophosphamide as substrate, CYP2C19 had the lowest apparent Km, followed by CYP2C9, CYP2C18 and CYP2C8, whereas in the case of ifosfamide, the rank order was: Km CYP2C19 < CYP2C18 < CYP2C9 < CYP2C8. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 4 | In the case of CYP2C9, a Ile359 to Leu mutation associated with poor metabolism of the hypoglycemic drug tolbutamide decreased catalytic efficiency toward cyclophosphamide by increasing the apparent Km, whereas the same mutation reduced the efficiency of this P450 toward ifosfamide by decreasing the Vmax. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 5 | Substitution of CYP2C9-Gly417 by Asp resulted in a two-fold lower catalytic efficiency for cyclophosphamide metabolism but a three-fold higher efficiency for ifosfamide metabolism. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 6 | Thus (a) wild type CYP2C19 and CYP2C9 are relatively low Km catalysts of cyclophosphamide and ifosfamide activation, and (b) all four human CYP2C enzymes activate these two anticancer prodrugs with varying efficiencies and with striking differences among naturally occurring allelic variants in the case of CYP2C9 and CYP2C18. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 7 | Thus (a) wild type CYP2C19 and CYP2C9 are relatively low Km catalysts of cyclophosphamide and ifosfamide activation, and (b) all four human CYP2C enzymes activate these two anticancer prodrugs with varying efficiencies and with striking differences among naturally occurring allelic variants in the case of CYP2C9 and CYP2C18. | Cyclophosphamide | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |