Advances in molecular biology over the past several years have permitted a much more detailed understanding of cellular dysfunction at the biochemical level in cancer cells. This has resulted in the identification of novel targets for therapeutic intervention, including proteins that regulate signal transduction, gene expression, and protein turnover. In many instances, small molecules are used to disrupt the function of these targets, often through competitive inhibition of ATP binding or the prevention of necessary protein-protein interactions. Future challenges lie in identifying appropriate targets for intervention and combining small molecule inhibitors with standard treatment modalities, such as radiation therapy and chemotherapy.