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Literature summary for 3.5.4.1 extracted from

  • Chaszczewska-Markowska, M.; Stebelska, K.; Sikorski, A.; Madej, J.; Opolski, A.; Ugorski, M.
    Liposomal formulation of 5-fluorocytosine in suicide gene therapy with cytosine deaminase - for colorectal cancer (2008), Cancer Lett., 262, 164-172.
    View publication on PubMed

Application

Application Comment Organism
pharmacology applicability of gene-directed enzyme prodrug therapy (GDEPT), prodrug encapsulation in liposomes, liposomal 5-fluorocytosine (5-FC) achieves high local concentration for suicide therapy Escherichia coli

Cloned(Commentary)

Cloned (Comment) Organism
enzyme expression in murine colorectal cancer cell line MC38 Escherichia coli
plasmid pBCMGSNeo/CD/CMV containing cytosine deaminase of Escherichia coli used for transfection of MC-38 cells Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cytosine + H2O Escherichia coli
-
uracil + NH3
-
?

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Escherichia coli P25524
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
incubation of transfected cells increasing concentrations of free or liposomal 5-fluorocytosine (5-FC) for 72 h, effectivness gene-directed enzyme prodrug therapy (GDEPT) tested in mice transplantated with MC-38 tumor cells, survival times of mice bearing tumors, local concentration and toxicity of liposomal prodrug in different organs, enhancement of antitumor effects by liposomal form of 5-fluorocytosine (5-FC) Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-fluorocytosine + H2O activation of the prodrug to the cytotoxic drug in cancer therapy by recombinant enzyme, the cytosine deaminase gene acts as suicide gene leading to increased 5-fluorouracil-mediated murine colorectal cancer cell killing, liposomal formulation of substrate 5-fluorocytosine using dipalmitoylphopshatidylcholine and cholesterol in a 1:1 ratio, overview Escherichia coli 5-fluorouracil + NH3
-
?
5-fluorocytosine + H2O gene-directed enzyme prodrug therapy (GDEPT) with free and liposomal 5-fluorocytosine (5-FC), antitumor effects of liposomal 5-fluorocytosine (5-FC) increased if compared to free prodrug Escherichia coli 5-fluorouracil + NH3
-
?
cytosine + H2O
-
Escherichia coli uracil + NH3
-
?

Synonyms

Synonyms Comment Organism
CD
-
Escherichia coli