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Literature summary for 3.5.4.5 extracted from

  • Sigmond, J.; Honeywell, R.J.; Postma, T.J.; Dirven, C.M.; de Lange, S.M.; van der Born, K.; Laan, A.C.; Baayen, J.C.; Van Groeningen, C.J.; Bergman, A.M.; Giaccone, G.; Peters, G.J.
    Gemcitabine uptake in glioblastoma multiforme: potential as a radiosensitizer (2009), Ann. Oncol., 20, 182-187.
    View publication on PubMed

Application

Application Comment Organism
medicine studies on radiosensitization of glioblastoma multiforme (GBM), deoxynucleoside analogue gemcitabine (dFdC) considered for combination therapy with radiation in glioblastomas Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0092
-
2',2'-difluorodeoxycytidine i.e. gemcitabine, variation of plasma gemcitabine between 0.9 and 9.2 microM Homo sapiens
0.0726
-
2',2'-difluorodeoxyuridine i.e. dFdU, variation of plasma ranges between 24.9 and 72.6 microM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
deoxycytidine + H2O Homo sapiens
-
deoxyuridine + NH3
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
glioblastoma multiforme (GBM) patients
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma glioblastoma multiforme (GBM) patients Homo sapiens
-
glioblastoma multiforme cell glioblastoma multiforme (GBM) patients Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
variation between 1.51 to 5.50 nmol/h/mg protein, about 100-fold lower than that in liver Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2',2'-difluorodeoxycytidine + H2O deamination of the deoxynucleoside analogue gemcitabine (dFdC) to difluorodeoxyuridine (dFdU), difluorodeoxyuridine used as radiosensitizer in gene therapy Homo sapiens 2',2'-difluorodeoxyuridine + NH3
-
?
deoxycytidine + H2O
-
Homo sapiens deoxyuridine + NH3
-
?

Synonyms

Synonyms Comment Organism
dCDA
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens