具有抗肿瘤活性的DNA小沟区结合剂的研究新进展

随着近年来基因工程基础研究的迅速发展以及小分子配体与DNA相互作用的机制研究的逐步深入,DNA已成为抗肿瘤药物研究的一个重要的药理学作用靶点,DNA小沟区结合剂成为抗肿瘤药物研究的重要方向。目前已开发了大量结构新颖、靶点单一、高效低毒的有效药物,多种已处于临床研究阶段。该文对近5年来DNA小沟区结合剂的研究新进展进行简要综述。

Advances on DNA minor groove binding agents as potential antitumor drugs

With the development and application of genetic engineering, DNA has become an important pharmacological target of many antitumor drugs. Based on the understanding of the mechanism of interaction between small molecular ligands and DNA, a lot of novel DNA minor groove binding agents as potential antitumor drugs have been designed and synthesized. Because of their interesting novel structure, single-target and higher-activity with lower-toxicity, some of them are used currently in clinical or in advanced clinical trials. Recent development with minor groove binders are discussed.