一种抗癌药物 - DNA 复合物的分子结构：柔红霉素加 d(CpGpTpApCpG)
Molecular structure of an anticancer drug-DNA complex: daunomycin plus d(CpGpTpApCpG).
作者信息
Quigley G J, Wang A H, Ughetto G, van der Marel G, van Boom J H, Rich A
出版信息
Proc Natl Acad Sci U S A. 1980 Dec;77(12):7204-8. doi: 10.1073/pnas.77.12.7204.
The structure of the crystalline daunomycin-d(CpGpTpApCpG) complex has been solved by x-ray diffraction analysis. The DNA forms a six-base-pair right-handed double helix with two daunomycin molecules intercalated in the d(CpG) sequences. The daunomycin aglycone chromophore is oriented at right angles to the long dimension of the DNA base pairs and the cyclohexene ring rests in the minor groove. Substituents on this ring have hydrogen bonding interactions to the base pairs above and below the intercalation site. These appear to be specific for anthracycline antibiotics. The amino sugar lies in the minor groove of the double helix without bonding to the DNA. The DNA double helix is distorted in a novel manner in accommodating the drug.
通过X射线衍射分析已解析出结晶态柔红霉素 - d（CpGpTpApCpG）复合物的结构。DNA形成一个六碱基对的右手双螺旋，有两个柔红霉素分子插入到d（CpG）序列中。柔红霉素糖苷配基发色团与DNA碱基对的长轴成直角取向，环己烯环位于小沟中。该环上的取代基与嵌入位点上方和下方的碱基对存在氢键相互作用。这些似乎是蒽环类抗生素所特有的。氨基糖位于双螺旋的小沟中，未与DNA结合。DNA双螺旋在容纳药物时以一种新颖的方式发生扭曲。
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