School of Chemical Sciences, Indian Association for the Cultivation of Science, Jadavpur, Kolkata 700032, India.
School of Applied & Interdisciplinary Sciences, Indian Association for the Cultivation of Science, Kolkata 700032, India.
J Med Chem. 2021 Jan 14;64(1):42-70. doi: 10.1021/acs.jmedchem.0c01145. Epub 2020 Dec 23.
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 III present in the upstream of P1 promoter of oncogene has the ability to form an intramolecular parallel G4 structure. The G4 structure that forms transiently in the promoter functions as a transcriptional repressor element. The 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 the G4 have been reported. In this review, we summarize various G4 specific molecules and discuss their effects on gene expression and .
富含鸟嘌呤的 DNA 序列有倾向形成四链体的 tet-rahelical G-四链体 (G4) 结构，这些结构在基因启动子中过度表达。这些非 Watson-Crick G4 结构的结构多态性和物理化学性质使它们成为药物开发的重要目标。致癌基因 P1 启动子上游的富含鸟嘌呤的核酸酶超敏元件 III 能够形成分子内平行 G4 结构。在 启动子中形成的瞬时 G4 结构作为转录阻遏元件发挥作用。致癌基因在多种癌症中过度表达，在癌症进展中发挥关键作用。到目前为止，已经报道了大量能够与 G4 相互作用并稳定 G4 的化合物。在这篇综述中，我们总结了各种 G4 特异性分子，并讨论了它们对 基因表达和 的影响。
