Selective Chemotherapeutics That Specifically Target Tumor Cells

Description

This technology is a series of synthesized cyanines that display high binding affinity to quadruplex DNA with high selectivity over duplex sequences. Cyanines are a class of small molecules that could be developed as potential G-quadruplex targeting agents. These cyanines have been designed to achieve highly selective binding to DNA G-quadruplexes with weaker binding to DNA duplexes. Data have shown that elevated quadruplex binding and specificity are highly sensitive to the polymethine chain length, heterocyclic structure, and intrinsic charge of the compound.

Chemotherapy is a treatment that kills cancer cells in patients. Due to the lack of specificity of chemotherapeutic drugs, the treatment kills any rapidly dividing cells including normal cells. Therefore, there is an urgent need to develop new selective chemotherapeutics that specifically target tumor cells. G-Quadruplex DNA has been recognized as a highly promising target for the development of new selective chemotherapeutics. G-quadruplex (G4) DNA is a type of four-stranded structure formed by a continuous guanine-rich DNA sequence. Quadruplex-forming sequences are present in oncogene promoter regions and within telomerase, and thus, developing compounds that strongly selectively bind quadruplex sequences could lead to potent chemotherapeutics.