title: Simple and fast screening of G-quadruplex ligands with electrochemical detection system.
abstract: Small molecules that may facilitate and stabilize the formation of G-quadruplexes can be used for cancer treatments, because the G-quadruplex structure can inhibit the activity of telomerase, an enzyme over-expressed in many cancer cells. Therefore, there is considerable interest in developing a simple and high-performance method for screening small molecules binding to G-quadruplex. Here, we have designed a simple electrochemical approach to screen such ligands based on the fact that the formation and stabilization of G-quadruplex by ligand may inhibit electron transfer of redox species to electrode surface. As a proof-of-concept study, two types of classical G-quadruplex ligands, TMPyP4 and BRACO-19, are studied in this work, which demonstrates that this method is fast and robust and it may be applied to screen G-quadruplex ligands for anticancer drugs testing and design in the future.
authors: State Key Laboratory of Pharmaceutical Biotechnology and Collaborative Innovation Center of Chemistry for Life Sciences, Department of Biochemistry, Nanjing University, Nanjing 210093, PR China.
authors: Qiongxuan
authors: Q
authors: Fan
authors: State Key Laboratory of Pharmaceutical Biotechnology and Collaborative Innovation Center of Chemistry for Life Sciences, Department of Biochemistry, Nanjing University, Nanjing 210093, PR China.
authors: Chao
authors: C
authors: Li
authors: State Key Laboratory of Pharmaceutical Biotechnology and Collaborative Innovation Center of Chemistry for Life Sciences, Department of Biochemistry, Nanjing University, Nanjing 210093, PR China.
authors: Yaqin
authors: Y
authors: Tao
authors: Laboratory of Biosensing Technology, School of Life Sciences, Shanghai University, Shanghai 200444, PR China.
authors: Xiaoxia
authors: X
authors: Mao
authors: State Key Laboratory of Pharmaceutical Biotechnology and Collaborative Innovation Center of Chemistry for Life Sciences, Department of Biochemistry, Nanjing University, Nanjing 210093, PR China; Laboratory of Biosensing Technology, School of Life Sciences, Shanghai University, Shanghai 200444, PR China. Electronic address: genxili@nju.edu.cn.
authors: Genxi
authors: G
authors: Li
mesh_terms: D000166:Acridines / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry*; D055664:Electrochemical Techniques; D054856:G-Quadruplexes; D006427:Hemin / Q000737:chemistry; D006861:Hydrogen Peroxide / Q000737:chemistry; D008024:Ligands; D011166:Porphyrins / Q000737:chemistry*
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D008024:Ligands; D011166:Porphyrins; C021096:tetra(4-N-methylpyridyl)porphine; D006427:Hemin; D006861:Hydrogen Peroxide; C454064:BRACO-19
keywords: Drug screening; Electrochemical method; G-quadruplex; Ligand