Fox K R, Kentebe E
Department of Physiology and Pharmacology, University of Southampton, Bassett Crescent East, U.K.
Biochem J. 1990 Jul 1;269(1):217-21. doi: 10.1042/bj2690217.
The interaction of echinomycin with a kinetoplast DNA fragment which contains phased runs of adenine residues has been examined by various footprinting techniques. DNAase I footprinting confirms that all drug-binding sites contain the dinucleotide CpG. However, not all such sequences are protected. Three sites, each of which is located between two adenine tracks in the sequence GCGA, are not protected from DNAase I attack. Enhanced cleavage by DNAase I, DNAase II and micrococcal nuclease is observed in regions surrounding drug-binding sites. The results suggest that echinomycin alters the conformation of the AT tracks, making them more like an average DNA structure. Echinomycin renders adenine residues in the sequence CGA hyper-reactive to diethyl pyrocarbonate.
通过各种足迹技术研究了棘霉素与含有腺嘌呤残基相间排列的动质体DNA片段的相互作用。DNA酶I足迹法证实所有药物结合位点都含有二核苷酸CpG。然而,并非所有此类序列都受到保护。在序列GCGA中,位于两条腺嘌呤序列之间的三个位点不受DNA酶I攻击的保护。在药物结合位点周围区域观察到DNA酶I、DNA酶II和微球菌核酸酶的切割增强。结果表明,棘霉素改变了AT序列的构象,使其更类似于平均DNA结构。棘霉素使序列CGA中的腺嘌呤残基对焦碳酸二乙酯具有高反应性。