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- W2070381172 abstract "Ligand techniques, as employed in radio-immunossay and radioreceptor assay, offer a sensitive and precise method for characterizing the interaction of enzymes and tight-binding inhibitors. Tetrahydrouridine (H4U) inhibition of human liver cytidine deaminase (EC 3.5.4.5) has been examined by direct measurement of enzyme-inhibitor (EI) binding and release. With partially purified enzyme from human liver, the EI complex was found to have a dissociation constant (KD) of 4.5 × 10−8M at 37°, in close agreement with estimates based on inhibition of enzyme activity by H4U. The presence of steady state conditions during competitive binding analysis was confirmed by direct measurement of the rate constants for EI binding at 25° and 37° (Kon 1.7 × 104 and 5.6 x ×04M−1sec−1 respectively). The rate constant for EI release at 37° was also determined experimentally (Koff = 4.0 × 10−3sec−1), and was in close agreement with the Koff value calculated from the experimentally determined KD and Kon values (KD = Koff/Kon). Scatchard analysis of H4U-enzyme binding, both in the presence and in the absence of 10−3M cytidine, showed no variation in total enzyme concentration (ET) but a decrease in apparent inhibitor affinity for enzyme, suggesting that cytidine and H4U compete for the same binding sites on cytidine deaminase, and confirming the competitive inhibition suggested by Lineweaver-Burk analysis. The turnover number for cytidine deaminase based on per H4U binding sites was 3.9 × 103 min−1. Thermodynamic constants for cytidine deaminase-tetrahydrouridine binding were derived from data on the temperature dependence of binding and included an enthalpy change (ΔH) = −12.7 kcal/mole, entropy change (ΔS) = −8.68 cal/deg/mole and Gibbs free energy change (ΔG) = −9.96 kcal/mole at 37.1°. This study indicates that ligand techniques can be applied to the difficult problem of characterizing the interaction of enzymes and tight-binding inhibitors." @default.
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- W2070381172 date "1978-01-01" @default.
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- W2070381172 title "Analysis of cytidine deaminase and tetrahydrouridine interaction by use of ligand techniques" @default.
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- W2070381172 doi "https://doi.org/10.1016/0006-2952(78)90256-3" @default.
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