药物 - 核酸相互作用：嵌入位点的构象灵活性。
Drug-nucleic acid interactions: conformational flexibility at the intercalation site.
作者信息
Berman H M, Neidle S, Stodola R K
出版信息
Proc Natl Acad Sci U S A. 1978 Feb;75(2):828-32. doi: 10.1073/pnas.75.2.828.
Abstract
The conformational features of the intercalation site in polynucleotides were examined. We found that, for all the crystal structures of drug-dinucleoside complexes studied thus far, two torsion angles differ from those found in A RNA (phi and chi) and that alternate sugar puckering is not a prerequisite for intercalation. This intercalation geometry, which is the basis of helix axis displacement in a polymer, would necessitate conformational changes in the adjacent nucleotides. The base-turn angle is less sensitive to the conformation of the backbone than it is to small alterations in the base-pairing geometry. We postulate that this angle is dependent on the nature of the intercalating drug.
摘要
对多核苷酸中嵌入位点的构象特征进行了研究。我们发现，就目前所研究的药物 - 二核苷复合物的所有晶体结构而言，有两个扭转角与A RNA中的扭转角（φ和χ）不同，并且交替的糖折叠不是嵌入的先决条件。这种嵌入几何结构是聚合物中螺旋轴位移的基础，它将使相邻核苷酸发生构象变化。碱基转角对主链构象的敏感性低于对碱基配对几何结构微小变化的敏感性。我们推测这个角度取决于嵌入药物的性质。
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