Tse Ting-Yuan, Chang Cheng-Chung, Lin Jing-Jer, Chang Ta-Chau
Institute of Atomic and Molecular Sciences, Academia Sinica, Taipei 10617, Taiwan, P.R. China.
Curr Top Med Chem. 2015;15(19):1964-70. doi: 10.2174/1568026615666150515150412.
Compelling evidence suggests that formation of guanine-quadruplex (G4) can protect the integrity of chromosome ends in eukaryotes, and regulate the activity of some gene promoters. In addition, G4 may be a novel therapeutic target. Thus, a number of ligands have been synthesized to stabilize G4. However, skepticism lingers over the existence of G4 in cells, as well as its biological function. The molecule 3,6-bis(1-methyl-4-vinylpyridium) carbazole diiodide (BMVC) can be used not only as a fluorescent probe to map endogenous and exogenous G4 in live cells, but also as therapeutic agent that arrests cancer growth by inhibiting telomerase activity and regulating gene expression. Thus, the fluorescence of a G4 anti-cancer agent is an invaluable tool to detect G4 in cells, investigate ligand-G4 interaction in live cells, examine the biological function of G4, and guide the development of new fluorescent anti-cancer agents.
有力证据表明，鸟嘌呤四链体（G4）的形成可保护真核生物染色体末端的完整性，并调节某些基因启动子的活性。此外，G4可能是一个新的治疗靶点。因此，人们已经合成了许多配体来稳定G4。然而，对于G4在细胞中的存在及其生物学功能仍存在怀疑。分子3,6-双（1-甲基-4-乙烯基吡啶）咔唑二碘化物（BMVC）不仅可以用作荧光探针来绘制活细胞内源性和外源性G4，还可以用作通过抑制端粒酶活性和调节基因表达来阻止癌症生长的治疗剂。因此，G4抗癌剂的荧光是检测细胞中G4、研究活细胞中配体与G4相互作用、检查G4生物学功能以及指导新型荧光抗癌剂开发的宝贵工具。
