Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate

Yeast cytosine deaminase (EC 3.5.4.1) is inhibited by 5‐bromo‐2‐pyrimidinone. In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these thr...

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Veröffentlicht in:European journal of biochemistry 1986, Vol.156 (2), p.297-300
Hauptverfasser: Kornblatt, M.J, Tee, O.S
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Tee, O.S
description Yeast cytosine deaminase (EC 3.5.4.1) is inhibited by 5‐bromo‐2‐pyrimidinone. In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these three forms to the observed inhibition. The anion makes little or no contribution. Both the parent and the covalent hydrate inhibit the enzyme, with the Ki for the hydrate being 0.2–0.02 times that of the parent. In the presence of stoichiometric concentrations of the enzyme, the equilibrium between parent and hydrate is displaced towards the hydrate; however, the hydration is not catalyzed by cytosine deaminase.
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In aqueous solution at neutral pH three forms of this compound (the anion, the parent, and the covalent hydrate) are in equilibrium. Experiments were undertaken in order to determine the relative contributions of these three forms to the observed inhibition. The anion makes little or no contribution. Both the parent and the covalent hydrate inhibit the enzyme, with the Ki for the hydrate being 0.2–0.02 times that of the parent. In the presence of stoichiometric concentrations of the enzyme, the equilibrium between parent and hydrate is displaced towards the hydrate; however, the hydration is not catalyzed by cytosine deaminase.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>3516692</pmid><doi>10.1111/j.1432-1033.1986.tb09581.x</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record>
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subjects 5-bromo-2-pyrimidinone
Applied sciences
bakers yeast
cytosine
Cytosine Deaminase
enzyme activity
Exact sciences and technology
Hydrogen-Ion Concentration
inhibition
Kinetics
Nucleoside Deaminases - antagonists & inhibitors
Other techniques and industries
Pyrimidinones - pharmacology
Saccharomyces cerevisiae
Saccharomyces cerevisiae - enzymology
title Inhibition of yeast cytosine deaminase by 5-bromo-2-pyrimidinone and its covalent hydrate
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