title: Inhibition of DNA polymerases by tripeptide derivative protease inhibitors.
abstract: Benzyloxycarbonyl(Z)-Leu-Leu-Leu-al and dansyl(Dns)-Leu-Leu-Leu-CH2Cl, well known as protease inhibitors, effectively inhibit the activities of DNA polymerases alpha, beta and gamma from rat liver and pol I from Escherichia coli, but the ability of these inhibitors to inhibit terminal deoxynucleotidyl transferase (TdT) is weak. The mode of inhibition by these tripeptide analogues is non-competitive with dNTP. The Ki values for Z-Leu-Leu-Leu-al and Dns-Leu-Leu-Leu-CH2Cl are 6.25 x 10(-5) M and 6.56 x 10(-5) M, respectively.
authors.affiliation: Department of Molecular Biology, Tokyo Metropolitan Institute of Gerontology, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Taguchi
authors.forename: A
authors.initials: A
authors.lastname: Matsukage
authors.forename: H
authors.initials: H
authors.lastname: Ito
authors.forename: Y
authors.initials: Y
authors.lastname: Saito
authors.forename: S
authors.initials: S
authors.lastname: Kawashima
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D004253:DNA Nucleotidylexotransferase / Q000037:antagonists & inhibitors; D004256:DNA Polymerase I / Q000037:antagonists & inhibitors; D004257:DNA Polymerase II / Q000037:antagonists & inhibitors; D004258:DNA Polymerase III / Q000037:antagonists & inhibitors; D004792:Enzyme Precursors / Q000097:blood* / Q000302:isolation & purification / Q000378:metabolism; D004926:Escherichia coli / Q000201:enzymology; D047908:Intracellular Signaling Peptides and Proteins; D007700:Kinetics; D008099:Liver / Q000201:enzymology; D008969:Molecular Sequence Data; D019384:Nucleic Acid Synthesis Inhibitors; D009842:Oligopeptides / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D011505:Protein-Tyrosine Kinases / Q000097:blood* / Q000302:isolation & purification / Q000378:metabolism; D051381:Rats; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D000072377:Syk Kinase
chemical_list: D004792:Enzyme Precursors; D047908:Intracellular Signaling Peptides and Proteins; D019384:Nucleic Acid Synthesis Inhibitors; D009842:Oligopeptides; D011480:Protease Inhibitors; D011994:Recombinant Proteins; D011505:Protein-Tyrosine Kinases; D000072377:Syk Kinase; C000606898:Syk protein, rat; D004253:DNA Nucleotidylexotransferase; D004256:DNA Polymerase I; D004257:DNA Polymerase II; D004258:DNA Polymerase III