Guanine-rich DNA sequences have the propensity to adopt four-stranded tetrahelical G-quadruplex (G4) structures that are overrepresented in gene promoters. The structural polymorphism and physicochemical properties of these non-Watson–Crick G4 structures make them important targets for drug development. The guanine-rich nuclease hypersensitivity element III₁ present in the upstream of P1 promoter of c-MYC oncogene has the ability to form an intramolecular parallel G4 structure. The G4 structure that forms transiently in the c-MYC promoter functions as a transcriptional repressor element. The c-MYC oncogene is overexpressed in a wide variety of cancers and plays a key role in cancer progression. Till now, a large number of compounds that are capable of interacting and stabilizing thec-MYC G4 have been reported. In this review, we summarize various c-MYC G4 specific molecules and discuss their effects on c-MYC gene expression in vitro and in vivo.

中文翻译：

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小分子靶向c-MYC G-四链体抗癌治疗的最新进展

富含鸟嘌呤的DNA序列倾向于采用基因启动子中过度表达的四链四螺旋G-四链体（G4）结构。这些非Watson-Crick G4结构的结构多态性和理化特性使其成为药物开发的重要目标。存在于c-MYC癌基因P1启动子上游的富含鸟嘌呤的核酸酶超敏元件III ₁具有形成分子内平行G4结构的能力。在c-MYC启动子中短暂形成的G4结构充当转录阻遏元件。在C-MYC癌基因在多种癌症中均过表达，并且在癌症进展中起关键作用。迄今为止，已经报道了许多能够相互作用和稳定c-MYC G4的化合物。在这次审查中，我们总结各种c-Myc的G4特定的分子并讨论他们对效果的c-MYC基因的表达在体外和体内。