Hudecz F, Kajtár J, Szekerke M
Nucleic Acids Res. 1981 Dec 21;9(24):6959-73. doi: 10.1093/nar/9.24.6959.
The interaction of AMSA with nucleic acids was studied by several techniques. Melting temperature and CD studies equally suggest that AMSA-binding is interfering with the secondary structure of DNA. An overlap by two mechanism of binding seems to exist. Based on the CD measurements at low drug concentration intercalation is the most likely way of binding. At higher drug concentration stacking interaction predominates leading to cooperativity and formation of oriented sheets of aromatic ring-systems as reflected in the optical activity induced in the metachromatic band of the achiral drug. No base-pair specificity could be confirmed; however, a high affinity of AMSA to poly(A) chains was demonstrated. The CD measurements did not indicate any significant interaction with RNA. The selectivity of the AMSA-DNA interaction can be regarded as an important argument in favour of the role of this interaction in the anti-tumour effect of the drug.
通过多种技术研究了AMSA与核酸的相互作用。解链温度和圆二色性研究均表明,AMSA结合会干扰DNA的二级结构。似乎存在两种结合机制的重叠。根据低药物浓度下的圆二色性测量结果,插入是最可能的结合方式。在较高药物浓度下,堆积相互作用占主导,导致协同作用并形成芳香环系统的定向片层,这在手性药物的异染带中诱导的光学活性中得到体现。未证实有碱基对特异性;然而,已证明AMSA对聚(A)链具有高亲和力。圆二色性测量未表明与RNA有任何显著相互作用。AMSA与DNA相互作用的选择性可被视为支持这种相互作用在该药物抗肿瘤作用中发挥作用的重要论据。