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DNA 中的连接点:治疗干预的未充分探索靶点。

Junctions in DNA: underexplored targets for therapeutic intervention.

机构信息

School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, United Kingdom.

School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, United Kingdom.

出版信息

Bioorg Med Chem. 2022 Sep 1;69:116897. doi: 10.1016/j.bmc.2022.116897. Epub 2022 Jun 24.

Abstract

DNA has been a key target for cancer therapy, with a range of compounds able to bind and either impair its processing or induce damage. Targeting DNA with small molecules in a truly sequence specific way, to impair gene specific processes, remains out of reach. The ability of DNA to assume different structures from the classical double helix allows access to more specific ligand binding modes and, potentially, to new avenues of treatment. In this review, we illustrate the small molecules that have been reported to bind to three- and four-way junctions.

摘要

DNA 一直是癌症治疗的一个关键靶点,有一系列的化合物能够与 DNA 结合,从而损害其加工过程或诱导其损伤。以真正的序列特异性方式用小分子靶向 DNA 以损害特定基因的过程,仍然遥不可及。DNA 从经典的双螺旋结构转变为不同结构的能力,为获得更特异的配体结合模式,并可能开辟新的治疗途径提供了可能。在这篇综述中,我们举例说明了已报道的与三链和四链结结合的小分子。

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