V. P. Ma, Ka-Ho Leung, D. Chan, W. Lam, C. Leung, Dik‐Lung Ma
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引用次数: 0
Abstract
In this review, we summarize recent findings in the development of c-myc G-quadruplex ligands. Several features such as expanded aromatic rings, flexible molecules, dinuclear metal complexes, oligomers and G-quartet based ligands have been demonstrated to be advantageous for providing higher selectivity towards the c-myc G-quadruplex over duplex structures. High throughput screening methods including competition dialysis, G4 FID, FRET-based melting assay, direct ELISA and in silico virtual screening for analyzing the interaction between the ligands and the c-myc G-quadruplex are discussed. In particular, in silico virtual screening has been demonstrated to be a valuable means for the discovery of selective G-quadruplex ligands. Using this approach, ligands selective for the c-myc G-quadruplex have been successfully identified
本文综述了近年来c-myc - g四联体配体的研究进展。扩展芳环、柔性分子、双核金属配合物、低聚物和基于g -四重奏的配体等特征已被证明有利于对c-myc g -四重体提供比双相结构更高的选择性。讨论了用于分析配体与c-myc g -四联体相互作用的高通量筛选方法,包括竞争透析、G4 FID、基于fret的熔融法、直接ELISA和计算机虚拟筛选。特别是,在硅虚拟筛选已被证明是一个有价值的手段,发现选择性g -四重体配体。使用这种方法,已经成功地鉴定了c-myc g -四重体的选择性配体