360A iodide

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.