Structure-Based Design of Potent Non-Peptide MDM2 Inhibitors

摘要

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-pep-tide small-molecule MDM2 inhibitors.The design of non-peptide small-molecule MDM2 inhibitors to block the p53-MDM2 interaction is being intensively pursued as a new strategy for anti-cancer drug design.