Binding characterization of anthraquinone derivatives by stabilizing G-quadruplex DNA leads to an anticancerous activity.

ABSTRACT: G-quadruplex is a non-canonical secondary structure identified in the telomeric region and the promoter of many oncogenes. Anthraquinone derivatives, a well-known inducer of telomere disruption in malignant cells and activate the apoptotic pathway. We used biophysical and biochemical studies to confirm the interaction of synthesized anthraquinone derivatives with the human telomeric G-quadruplex sequence. The binding affinity of N-2DEA and N-1DEA are K _b = 4.8 × 10⁶ M^-1 and K _b = 7.6 × 10⁵ M^-1, respectively, leading to hypochroism, fluorescence quenching with minor redshift and ellipticity variations indicating ligand binding in the external groove. We found that sodium ions induced stabilization more rather th

SUBMITTER: Dey A 

PROVIDER: S-EPMC9720492 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature