Structure-Based Design of Potent Non-Peptide MDM2 Inhibitors.

This article presents a structure-based design of potent non-peptide MDM2 oncoprotein inhibitors. It is believed that the p53 tumor suppressor plays a central role in controlling cell cycle progression and apoptosis, and is an attractive cancer therapeutic target because its tumor suppressor activity can be stimulated to eradicate tumor cells. A new approach to stimulation of the activity of p53 is through blocking its interaction with the MDM2 oncoprotein, an endogenous cellular inhibitor of p53, using non-peptide small-molecule MDM2 inhibitors.