G-Quadruplex Ligands as Stabilizer Targeting Telomerase Enzyme as Anti Cancer Agents

Abstract

The human telomere stabilization with G-Quadruplex DNA tends to induce apoptosis. The molecular target of telomere cascade with a rigid molecular may show efficacious to treat cancer. The study of intercalation to human telomeric DNA with proposed ligand can be evaluated by the help of biophysical studies and biological studies. G-Quadruplex is one of the key epigenetic episodes of eukaryotes and prokaryotes, generally found in the telomeric end region, immunoglobulin switch recombination and the lagging strand of the DNA. These chemotherapeutic advances are not enough to maintain a life expectancy of cancer affected patients. A number of G-Quadruplex ligands such as acridine, perylene, and anthraquinones have been synthesized reported and evaluated them for the inhibitor activity. Therefore, translational research can pave the novel prospect to treat cancer in a fundamental way. In that connection, basic research showed G-Quadruplex phenomenon of DNA, which is having a great impact in this chemotherapy.

PhenQE8, a Novel Ligand of the Human Telomeric Quadruplex

“…Taking into account these considerations, different types of molecules have been designed, synthesized and evaluated, which can be categorized in three main families: fused polyaromatic systems, macrocyclic compounds (either of natural or synthetic origin) and nonfused aromatic systems. Without being exhaustive [33,34], some examples of compounds studied as quadruplex ligands, and that have shown biological activity, include 2,6-diamidoanthraquinone, bisA, BRACO-19, PIPER, telomestatin, pyridostatin, TmPyP4, NMM, quarfloxacin, RHPS4, CX-5461, 360A, PhenDC3 and naphthalene diimides. Unfortunately, practical clinical applications remain elusive for most of these compounds, with some rare exceptions such as quarfloxacin and CX-5461.…”