Developing Novel G-Quadruplex Ligands: from Interaction with Nucleic Acids to Interfering with Nucleic Acid–Protein Interaction

• Main Authors: Zhi-Yin Sun, Xiao-Na Wang, Sui-Qi Cheng, Xiao-Xuan Su, Tian-Miao Ou
• Format: Article
• Language: English
• Published: MDPI AG 2019-01-01
• Series: Molecules
• Subjects: G-quadruplex; G-quadruplex ligand; G-quadruplex-related proteins; helicase; anti-tumor
• Online Access: https://www.mdpi.com/1420-3049/24/3/396

G-quadruplex is a special secondary structure of nucleic acids in guanine-rich sequences of genome. G-quadruplexes have been proved to be involved in the regulation of replication, DNA damage repair, and transcription and translation of oncogenes or other cancer-related genes. Therefore, targeting G-quadruplexes has become a novel promising anti-tumor strategy. Different kinds of small molecules targeting the G-quadruplexes have been designed, synthesized, and identified as potential anti-tumor agents, including molecules directly bind to the G-quadruplex and molecules interfering with the binding between the G-quadruplex structures and related binding proteins. This review will explore the feasibility of G-quadruplex ligands acting as anti-tumor drugs, from basis to application. Meanwhile, since helicase is the most well-defined G-quadruplex-related protein, the most extensive research on the relationship between helicase and G-quadruplexes, and its meaning in drug design, is emphasized.