Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate
نویسندگان
چکیده
منابع مشابه
Yeast cytosine deaminase improves radiosensitization and bystander effect by 5-fluorocytosine of human colorectal cancer xenografts.
The efficacy of cancer gene therapy using bacterial cytosine deaminase (bCD)/5-fluorocytosine (5-FC) enzyme/prodrug strategy is limited by the inefficiency of cytosine deaminase (CD)-catalyzed conversion of 5-FC into 5-fluorouracil (5-FU). We have shown previously that yeast CD (yCD) is more efficient at the conversion of 5-FC than bCD. In the current study, we hypothesized that the increased p...
متن کاملDNA (Cytosine-C5) methyltransferase inhibition by oligodeoxyribonucleotides containing 2-(1H)-pyrimidinone (zebularine aglycon) at the enzymatic target site.
Aberrant cytosine methylation in promoter regions leads to gene silencing associated with cancer progression. A number of DNA methyltransferase inhibitors are known to reactivate silenced genes; including 5-azacytidine and 2-(1H)-pyrimidinone riboside (zebularine). Zebularine is a more stable, less cytotoxic inhibitor compared to 5-azacytidine. To determine the mechanistic basis for this differ...
متن کاملProduct release is rate-limiting in the activation of the prodrug 5-fluorocytosine by yeast cytosine deaminase.
Yeast cytosine deaminase (yCD), a zinc metalloenzyme, catalyzes the hydrolytic deamination of cytosine to uracil. The enzyme is of great biomedical interest because it also catalyzes the deamination of the prodrug 5-fluorocytosine (5FC) to form the anticancer drug 5-fluorouracil (5FU). yCD/5FC is one of the most widely used enzyme/prodrug combinations for gene-directed enzyme prodrug therapy fo...
متن کامل5-Bromo-2-hydroxybenzonitrile
The title compound, C(7)H(4)BrNO, crystallizes with two mol-ecules in the asymmetric unit. The two molecules exhibit nearly linear C-C N nitrile bond angles of 179.1 (4) and 177.1 (4)°. In the crystal, the mol-ecules are linked into a one-dimensional hydrogen-bonded chain by inter-actions between the phenol H atom and the nitrile N atom [N⋯O = 2.805 (4) and 2.810 (4) Å].
متن کامل5-(5-Bromo-2-methoxyphenyl)-2-fluoropyridine
In the title compound, C(12)H(9)BrFNO, the dihedral angle between the aromatic rings is 51.39 (5)°; the C atom of the meth-oxy group is close to being coplanar with its attached ring (r.m.s. deviation = 0.0172 Å] and is oriented away from the pyridine ring. In the crystal, mol-ecules inter-act by van der Waals forces.
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ژورنال
عنوان ژورنال: European Journal of Biochemistry
سال: 1986
ISSN: 0014-2956,1432-1033
DOI: 10.1111/j.1432-1033.1986.tb09581.x