CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal.
University of Bordeaux, ARNA Laboratory, INSERM, U1212, CNRS UMR 5320, IECB, F-33600 Pessac, France; Institute of Biophysics of the Czech Academy of Sciences, Královopolská 135, Brno, 612 65, Czech Republic.
Trends Mol Med. 2020 Sep;26(9):848-861. doi: 10.1016/j.molmed.2020.05.002. Epub 2020 May 25.
The clinical applicability of G-quadruplexes (G4s) as anticancer drugs is currently being evaluated. Several G4 ligands and aptamers are undergoing clinical trials following the notable examples of quarfloxin and AS1411, respectively. In this review, we summarize the latest achievements and breakthroughs in the use of G4 nucleic acids as both therapeutic tools ('friends', as healing anticancer drugs) and targets ('foes', within the harmful cancer cell), particularly using aptamers and quadruplex-targeted ligands, respectively. We explore the recent research on synthetic G4 ligands toward the discovery of anticancer therapeutics and their mechanism of action. Additionally, we highlight recent advances in chemical and structural biology that enable the design of specific G4 aptamers to be used as novel anticancer agents.
目前正在评估 G-四链体 (G4s) 作为抗癌药物的临床适用性。在 quarfloxin 和 AS1411 这两个著名的例子之后，有几种 G4 配体和适体正在进行临床试验。在这篇综述中，我们总结了使用 G4 核酸作为治疗工具（“朋友”，作为治疗癌症的药物）和靶标（“敌人”，在有害的癌细胞内）的最新进展和突破，分别使用适体和四链体靶向配体。我们探讨了合成 G4 配体在发现抗癌治疗药物及其作用机制方面的最新研究。此外，我们还强调了化学和结构生物学方面的最新进展，这些进展使设计特定的 G4 适体作为新型抗癌药物成为可能。
