Chemistry Department, Wesleyan University, Middletown, CT 06459, USA.
Mutat Res. 2011 Nov 27;726(1):47-53. doi: 10.1016/j.mrgentox.2011.08.004. Epub 2011 Aug 27.
Tumor cell lines can replicate faster than normal cells and many also have defective DNA repair pathways. This has lead to the investigation of the inhibition of DNA repair proteins as a means of therapeutic intervention. An alternative approach is to hide or mask damaged DNA from the repair systems. We have developed a protocol to investigate the structures of the complexes of damaged DNA with drug like molecules. Nucleotide resolution structural information can be obtained using an improved hydroxyl radical cleavage protocol. The use of a dT(n) tail increases the length of the smallest fragments of interest and allows efficient co-precipitation of the fragments with poly(A). The use of a fluorescent label, on the 5' end of the dT(n) tail, in conjunction with modified cleavage reaction conditions, avoids the lifetime and other problems with (32)P labeling. The structures of duplex DNAs containing AC and CC mismatches in the presence and absence of minor groove binders have been investigated as have those of the fully complementary DNA. The results indicate that the structural perturbations of the mismatches are localized, are sequence dependent and that the presence of a mismatch can alter the binding of drug like molecules.
肿瘤细胞系比正常细胞复制得更快,许多肿瘤细胞系的 DNA 修复途径也存在缺陷。这促使人们研究抑制 DNA 修复蛋白作为治疗干预的一种手段。另一种方法是将受损的 DNA 隐藏或掩盖起来,使其免受修复系统的影响。我们已经开发了一种方案来研究受损 DNA 与类似药物分子的复合物的结构。使用改良的羟基自由基切割方案可以获得核苷酸分辨率的结构信息。使用 dT(n)尾巴可以增加感兴趣的最小片段的长度,并允许与 poly(A)有效地共沉淀片段。在 5' 端使用荧光标记,结合修饰的切割反应条件,可以避免 (32)P 标记的寿命和其他问题。已经研究了含有 AC 和 CC 错配的双链 DNA 的结构,以及完全互补的 DNA 的结构。结果表明,错配的结构扰动是局部的、序列依赖性的,并且错配的存在可以改变类似药物分子的结合。