Drs A.M. Burgoyne, T.G. Kutateladze, D.L. Durden and colleagues have described now a new synthetic small molecule inhibitor with triple action against the targets CDK4/6, PI3K and BET. The molecule shows potent inhibitory activity against the three targets and demonstrate increased specific cytotoxicity in cancer cells compared with the correspondent most promising single inhibitors (Palbociclib, BKM120 and JQ1 respectively) or a combination of those. Among the cancer cells tested, we show great action on neuroblastoma cancer cells. This triple inhibitor has the potential of disrupting cancer cell signaling with high specificity and efectivity, overcoming some of the problems associated with combination therapy and offering a promising strategy against drug resistant tumors.
Cancer Cell Biology Laboratory 