Selective Up-Regulation of Tumor Suppressor Gene Retinoblastoma by Bisacridine Derivative Through Gene Promoter Quadruplex Structures for Cancer Treatment.

ABSTRACT: The retinoblastoma (RB) gene is an important tumor suppressor gene with a higher mutation frequency than other tumor suppressor genes. The mutation or inactivation of RB has been found in various cancers. The discovery of small molecules to promote RB expression is an effective anti-cancer strategy. Special DNA secondary structures with G-quadruplex and i-motif on the RB promoter could act as "molecular switches" for gene transcriptional regulation and are potentially important targets for the development of new anti-cancer drugs. After extensive screening, we found that the bisacridine derivative A06 had selective binding and destabilization for both the G-quadruplex and i-motif on the RB promoter, which significantly up-regulated RB gene transcription and translation, resul

SUBMITTER: Lin X 

PROVIDER: S-EPMC11855212 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature