Reprograming cancer cells by a BODIPY G-quadruplex stabiliser

A cationic BODIPY-based G-quadruplex-selective stabiliser is developed and shown to decrease cancer cell migration-invasion up to 90%. The expression of critical genes (HIF1 alpha, VIM, CDH1) related to metastasis is modulated. The stabiliser reprograms hypoxia-adaptive metabolism and an 1.82-fold increase in O2 consumption, enabling back-to-normal switching of energy metabolism, is observed. Stabilisers with a strong G-quadruplex affinity (0.38 mu M Kd) significantly contribute to small molecule anti-cancer approaches. A BODIPY-based G-quadruplex-selective stabiliser is shown to silence regulator genes, reduce cell migration and invasion, and switch off the hypoxia-adaptive metabolism.