G-Quadruplex-Specific Cell-Permeable Guanosine-Anthracene Conjugate Inhibits Telomere Elongation and Induces Apoptosis by Repressing the Gene.

We herein report a cell-membrane-permeable molecular probe , prepared by conjugating guanosine with anthracene, selectively interacts with G-quadruplex over other promoter and telomeric quadruplexes as well as duplex DNA. NMR spectroscopy suggests that interacts with terminal G-quartets as well as with the nearby G-rich tract (G13-G14-G15 and G8-G9-G10) of quadruplex. In vitro cellular studies indicate that represses expression by stabilizing its promoter G-quadruplex and alters -related cellular events. suppresses and gene expressions in a promoter-independent manner, inhibits elongation of telomere length, and activates apoptotic cascades in cancer cells.