Krishnan B S, Moore M E, Lavoie C P, Long B H, Dalterio R A, Wong H S, Rosenberg I E
Bristol-Myers Squibb Company, Wallingford, CT 06492, USA.
J Biomol Struct Dyn. 1994 Dec;12(3):625-36. doi: 10.1080/07391102.1994.10508763.
The DNA binding of BMS 181176, an antitumor antibiotic derivative of rebeccamycin was characterized by DNA unwinding assays, as well as by fluorescence emission and polarization spectroscopic techniques. Unwinding and rewinding of supercoiled DNA was interpreted in terms of intercalation of BMS 181176 into DNA. BMS 181176 shows an enhanced fluorescence emission upon binding to the AT sequence and no enhancement upon binding to the GC sequence. BMS 181176 appears to be a weaker binder to poly(dAdT).poly(dAdT) compared to doxorubicin and ethidium bromide. When bound to DNA, the rotational motion of BMS 181176 is substantially decreased as evident from the increase in fluorescence polarization. BMS 181176 exhibits a range of binding strengths depending on the DNA. This is demonstrated by the Acridine Orange displacement assay using fluorescence polarization.
通过DNA解旋分析以及荧光发射和偏振光谱技术对丽蝇霉素抗肿瘤抗生素衍生物BMS 181176的DNA结合特性进行了表征。超螺旋DNA的解旋和复旋是根据BMS 181176插入DNA来解释的。BMS 181176与AT序列结合时荧光发射增强，与GC序列结合时则无增强。与多柔比星和溴化乙锭相比，BMS 181176与聚（dAdT）.聚（dAdT）的结合力似乎较弱。从荧光偏振增加可以明显看出，当BMS 181176与DNA结合时，其旋转运动大幅降低。BMS 181176根据DNA表现出一系列结合强度。这通过使用荧光偏振的吖啶橙置换试验得到了证明。
