360A iodide is a G-quadruplex stabilizer and also an effective inhibitor of telomerase activity (IC₅₀=300nM)[1-2]. 360A iodide can interfere with the cell cycle and induce cancer cell death[3-4].
In vitro, treatment of human glioma cell lines T98G, CB193, and U118-MG with 360A iodide (5μM) for 7-14 days. 360A iodide significantly reduced cell viability and induced cell cycle arrest and apoptosis[5]. Treatment of ATM-deficient (ATMKD) and ATM-normal human HeLa cells with 360A iodide (5μM) for 12 hours. 360A iodide significantly induced telomere instability, including sister telomere fusion, telomere loss, and telomere doublet formation[6].
References:
[1] Granotier C, Pennarun G, Riou L, et al. Preferential binding of a G-quadruplex ligand to human chromosome ends. Nucleic Acids Res. 2005 Jul 28;33(13):4182-90.
[2] Hwang IP, Mailliet P, Hossard V, et al. Investigating the Effect of Mono- and Dimeric 360A G-Quadruplex Ligands on Telomere Stability by Single Telomere Length Analysis (STELA). Molecules. 2019 Feb 6;24(3):577.
[3] Revikumar A, Kashyap V, Palollathil A, et al. Multiple G-quadruplex binding ligand induced transcriptomic map of cancer cell lines. J Cell Commun Signal. 2022 Mar;16(1):129-135.
[4] Gauthier LR, Granotier C, Hoffschir F, et al. Rad51 and DNA-PKcs are involved in the generation of specific telomere aberrations induced by the quadruplex ligand 360A that impair mitotic cell progression and lead to cell death. Cell Mol Life Sci. 2012 Feb;69(4):629-40.
[5] Pennarun G, Granotier C, Gauthier LR, et al. Apoptosis related to telomere instability and cell cycle alterations in human glioma cells treated by new highly selective G-quadruplex ligands. Oncogene. 2005 Apr 21;24(18):2917-28.
[6] Pennarun G, Granotier C, Hoffschir F, et al. Role of ATM in the telomere response to the G-quadruplex ligand 360A. Nucleic Acids Res. 2008 Mar;36(5):1741-54.
360A iodide是一种G-四联体（G-quadruplex）的稳定剂，360A iodide还是有效的端粒酶（telomerase；IC50=300nM）的活性抑制剂[1-2]。360A iodide可干预细胞周期，诱导癌细胞死亡[3-4]。
在体外，360A iodide (5μM)处理人脑胶质瘤细胞系T98G、CB193和U118-MG 7-14天。360A iodide显著降低细胞活力并诱导细胞周期阻滞和凋亡[5]。360A iodide（5μM）处理ATM缺陷型（ATMKD）和ATM正常的人HeLa细胞12小时。360A iodide显著诱导端粒不稳定性，包括姐妹端粒融合、端粒缺失和端粒双联体形成[6]。