G-quadruplexes are higher-order structures formed in guanine-rich sequences of nucleic acids. The quadruplex structure can occur naturally in G-rich sequences and have been identified in telomeres and gene promoter regions. Proteins and ligands can bind G-quadruplexes, stabilizing DNA and RNA, and inhibit or promote replication, transcription, and translation. As these structures are linked to such diverse functions, the development of small molecules to stabilize the G-quadruplex structure has garnered significant attention. The goal of our research is to synthesize and evaluate small molecules that stabilize the G-quadruplex structure. Through the derivatization of azobenzene and indigo based dyes, a small library of organic compounds was synthesized in 1-3 steps. These compounds, in addition to a small selection of RGG-motif peptides, were tested for G-quadruplex stabilizing abilities by measuring changes in melting point curves of DNA as measured by circular dichroism. Several of the drugs increased the melting temperature of the DNA, demonstrating that these core structures possess the ability to stabilize the telomeric G-quadruplex structure.<br/>

Evaluation of small molecules that bind and stabilize G-Quadruplex DNA

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.