Dual Targeting Topoisomerase/G-Quadruplex Agents in Cancer Therapy-An Overview.

ABSTRACT: Topoisomerase (Topo) inhibitors have long been known as clinically effective drugs, while G-quadruplex (G4)-targeting compounds are emerging as a promising new strategy to target tumor cells and could support personalized treatment approaches in the near future. G-quadruplex (G4) is a secondary four-stranded DNA helical structure constituted of guanine-rich nucleic acids, and its stabilization impairs telomere replication, triggering the activation of several protein factors at telomere levels, including Topos. Thus, the pharmacological intervention through the simultaneous G4 stabilization and Topos inhibition offers a new opportunity to achieve greater antiproliferative activity and circumvent cellular insensitivity and resistance. In this line, dual ligands targeting both Topos and G4 e

SUBMITTER: Salerno S 

PROVIDER: S-EPMC9687504 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature