Phillips D R, DiMarco A, Zunino F
Eur J Biochem. 1978 Apr 17;85(2):487-92. doi: 10.1111/j.1432-1033.1978.tb12264.x.
The ability of daunomycin to bind to various DNA polymers has been sutided by thermal denaturation, spectrophotometric analysis and inhibition of the polymerisation reactions catalysed by Escherichia coli DNA polymerase I and rat liver DNA polymerase alpha. The quantitative binding measurements revealed that the antibiotic binds tightly to all synthetic polydeoxynucleotides studied. The results demonstrated that daunomycin can bind with equal affinity to dG . dC or dA . dT basepaired sequences. However, the number of binding sites per nucleotide for poly(dA) . poly(dT) is significantly lower than that found for poly(dA-dT) . poly(dA-dT), thus indicating an appreciable preference of the drug for the alternating copolymer. The inactivation of the template properties of the synthetic DNA polymers in the DNA polymerase system is consistent with their daunomycin binding ability. However, a lack of correlation was observed between the drug binding ability of different DNA polymers and the binding-induced stabilisation of the double helix to heat denaturation.
通过热变性、分光光度分析以及对大肠杆菌DNA聚合酶I和大鼠肝脏DNA聚合酶α催化的聚合反应的抑制作用,对柔红霉素与各种DNA聚合物的结合能力进行了研究。定量结合测量结果表明,该抗生素与所有研究的合成聚脱氧核苷酸紧密结合。结果表明,柔红霉素能以相同的亲和力与dG·dC或dA·dT碱基配对序列结合。然而,聚(dA)·聚(dT)每核苷酸的结合位点数明显低于聚(dA-dT)·聚(dA-dT),这表明该药物对交替共聚物有明显的偏好。合成DNA聚合物在DNA聚合酶系统中的模板特性失活与其柔红霉素结合能力一致。然而,观察到不同DNA聚合物的药物结合能力与结合诱导的双螺旋对热变性的稳定性之间缺乏相关性。