Protein–Protein Interaction Inhibitors

The study of cellular mechanisms of cancer growth and survival has revealed a complex web of signalling pathways that produce the ‘hallmarks of cancer’. A number of critical cellular signalling nodes have been characterised from which many new drug targets have been proposed. A number of these nodes are regulated by protein–protein interactions, and so present attractive, if challenging, targets for drug discovery. Drug discovery efforts towards three PPI families have resulted in clinically investigated drugs: i.e. Bcl-2 family inhibitors, MDM2-p53 inhibitors and IAP inhibitors. The discovery and optimisation of these drug classes are detailed in this chapter.