Garbesi A, Bonazzi S, Zanella S, Capobianco M L, Giannini G, Arcamone F
I.Co.CEA-CNR, Via P.Gobetti 101, 40129 Bologna, Italy.
Nucleic Acids Res. 1997 Jun 1;25(11):2121-8. doi: 10.1093/nar/25.11.2121.
Conjugation of an anthracycline to a triplex-forming oligonucleotide (TFO) allows delivery of this drug to a specific DNA site, preserving the intercalation geometry of this class of anticancer agents. Conjugate 11, in which the TFO is linked via a hexamethylene bridge to the O-4 on the D ring of the anthraquinone moiety, affords the most stable triple helix, through intercalation of the planar chromophore between DNA bases and binding of both the TFO and the amino sugar to the major and the minor groove respectively.
将蒽环类药物与三链形成寡核苷酸(TFO)偶联,可将该药物递送至特定的DNA位点,保持这类抗癌药物的嵌入几何结构。偶联物11中,TFO通过六亚甲基桥连接到蒽醌部分D环上的O-4位,通过平面发色团嵌入DNA碱基之间以及TFO和氨基糖分别与大沟和小沟结合,提供了最稳定的三链螺旋结构。