Aptamer-based Targeted Delivery of a G-quadruplex Ligand in Cervical Cancer Cells.

ABSTRACT: AS1411 is a G-rich DNA oligonucleotide that functions as an aptamer of the protein nucleolin, found at high levels on the surface of cancer cells but not on the surface of normal cells. Herein, we have studied AS1411 as a supramolecular carrier for the delivery of an acridine-based G-quadruplex ligand, C₈, to HeLa cancer cells. Two AS1411 derivatives, LNA-AS1411 and U-AS1411, were also tested, in an attempt to compare AS1411 pharmacological properties. The results showed that AS1411-C₈ complexation was made with great binding strength and that it lowered the ligand's cytotoxicity towards non-malignant cells. This effect was suggested to be due to a decreased internalization of the complexed versus free C₈ as shown by flow cytometry. The AS1411 derivatives,

SUBMITTER: Carvalho J 

PROVIDER: S-EPMC6538641 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature