Venozhinskis M T, Nesterenko V F, Kanopkaĭte S I, Bur'ianov Ia I
Biokhimiia. 1985 May;50(5):749-54.
A correlation was found between the bacteriocide effect of 5-aza-C and the amount of cytosine DNA-methylases in E. coli cells. 5-Aza-C-DNA induced partial or complete inhibition of bacterial DNA-methylases with different site specificity; cytosine DNA-methylases were inhibited by the DNA more effectively than adenine DNA-methylase Eco dam. The inhibitory influence of 5-aza-C-DNA on cytosine DNA-methylases was due to the formation of stable inactive complexes between the enzyme and the non-methylating cytosine analog in the recognition sites. Cytosine DNA-methylase Eco RII formed a relatively firm bond with 5-aza-C-DNA, which could be disrupted by 1 M KCl; this disruption restores the DNA-methylase activity and the inhibiting capacity of 5-aza-C-DNA. Thus, the binding of cytosine DNA-methylase to 5-aza-C in DNA is noncovalent; the inhibition of the enzyme by 5-aza-C-DNA is reversible.
在大肠杆菌细胞中,发现5-氮杂胞苷(5-aza-C)的杀菌作用与胞嘧啶DNA甲基化酶的量之间存在相关性。5-氮杂胞苷-DNA(5-Aza-C-DNA)诱导对具有不同位点特异性的细菌DNA甲基化酶产生部分或完全抑制;胞嘧啶DNA甲基化酶比腺嘌呤DNA甲基化酶Eco dam更有效地被DNA抑制。5-氮杂胞苷-DNA对胞嘧啶DNA甲基化酶的抑制作用是由于在识别位点中酶与非甲基化胞嘧啶类似物之间形成了稳定的无活性复合物。胞嘧啶DNA甲基化酶Eco RII与5-氮杂胞苷-DNA形成相对牢固的结合,这种结合可被1 M KCl破坏;这种破坏恢复了DNA甲基化酶的活性以及5-氮杂胞苷-DNA的抑制能力。因此,胞嘧啶DNA甲基化酶与DNA中5-氮杂胞苷的结合是非共价的;5-氮杂胞苷-DNA对该酶的抑制是可逆的。