5-(.alpha.-Bromoacetyl)-2'-deoxyuridine 5'-phosphate: an affinity label for thymidylate synthetase

Abstract

5-(alpha-Bromoacetyl)-2'-deoxyuridine 5'-phosphate (1) is an active-site-directed irreversible inhibitor of thymidylate synthetase from Lactobacillus casei. Analysis of the rate of inactivation of the enzyme in the presence of substrate confirmed the intermediate formation of a reversible enzyme-inhibitor complex.

5-Substituted N4-Hydroxy-2‘-deoxycytidines and Their 5‘-Monophosphates: Synthesis, Conformation, Interaction with Tumor Thymidylate Synthase, and in Vitro Antitumor Activity

“…The slopes of the semilog plots of percent (%) remaining activity vs preincubation time, expressing apparent inactivation rate constants ( k app ) and corresponding inhibitor concentrations [ I ], were then replotted as double-reciprocal plots, according to the relationship: 41 where k 2 is the inactivation rate constant. The values of k 2 and K i were determined from the plot intercept and slope, respectively. , …”

“…The values of k2 and Ki were determined from the plot intercept and slope, respectively. 38,42 Statistically Evaluated Results. These are presented as means ( SEM or means ( percent difference between the mean and each of the two results, followed by the number of experiments (N) in parentheses.…”

Phosphorylation of thymidylate synthase affects slow-binding inhibition by 5-fluoro-dUMP and N4-hydroxy-dCMP

“…32 The slopes of the semi-log plots of percent remaining activity vs. preincubation time, expressing apparent inactivation rate constants (k app ) and corresponding inhibitor concentrations ([I]), were then replotted as double-reciprocal plots, and the values of k 2 and K i were determined from the plot intercept and slope, respectively. 44 …”

Synthesis and spectroscopic studies of charge transfer complexes between chloranilic acid and some heterocyclic amines in ethanol

“…Pyrimidines, thiazoles, pyrazoles and triazines are very important heterocyclic compounds. They considered to be important not only because they are on integral part of genetic materials viz., DNA and RNA as nucleotides and nucleosides also they have important numerous biodynamic properties and biological activities such as bactericides, fungicides, vermicides and medicines [13][14][15][16][17][18][19]. Charge transfer complexes of organic species are intensively studied because of their special type of interaction, which is accompanied by transfer of an electron from the donor to the acceptor [20,21].…”