Bernier J L, Henichart J P, Catteau J P
Biochem J. 1981 Dec 1;199(3):479-84. doi: 10.1042/bj1990479.
A lysyl-lysine bifunctional derivative of 9-aminoacridine has been synthesized and its DNA-binding capacity established by electron-paramagnetic-resonance study. For this purpose the binding parameters of a spin-labelled aminoacridine probe were estimated and the affinities of the lysylacridinyl-lysyldiamino-octane dimer and of 9-amino-acridine could be evaluated by competitive assays. The competition study provided quantitative results concerning the dissociation constant (KD) of the dimer. The obtained value was closely similar to the KD of 9-aminoacridine determined by the same method and to the KD previously reported for the anti-tumour and antibiotic bifunctional intercalator quinomycins.
已合成了9-氨基吖啶的赖氨酰-赖氨酸双功能衍生物，并通过电子顺磁共振研究确定了其与DNA的结合能力。为此，估算了自旋标记的氨基吖啶探针的结合参数，并通过竞争性分析评估了赖氨酰吖啶基-赖氨酰二氨基辛烷二聚体和9-氨基吖啶的亲和力。竞争研究提供了有关二聚体解离常数（KD）的定量结果。所得值与用相同方法测定的9-氨基吖啶的KD以及先前报道的抗肿瘤和抗生素双功能嵌入剂醌霉素的KD非常相似。
