Synthesis and binding properties of conjugates between oligodeoxynucleotides and daunorubicin derivatives
Synthesis and binding properties of conjugates between oligodeoxynucleotides and daunorubicin derivatives
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DOI：
10.1093/nar/25.11.2121
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发表时间：
1997-06-01
影响因子：
14.9
通讯作者：
Arcamone, F
中科院分区：
文献类型：
--
作者：
Garbesi, A;Bonazzi, S;Arcamone, F
将蒽环类药物与形成三聚体的寡核苷酸 (TFO) 结合，可以将该药物递送至特定的 DNA 位点，从而保留此类抗癌药物的嵌入几何形状。缀合物 11 中的 TFO 通过六亚甲基桥与蒽醌部分 D 环上的 O-4 连接，通过在 DNA 碱基之间插入平面发色团以及 TFO 和氨基糖分别与大沟和小沟结合，提供最稳定的三螺旋。
Conjugation of an anthracycline to a tripler-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.