The cell-division cycle is a tightly controlled process that is regulated by the cyclin/CDK family of protein kinase complexes. Stringent control of this process is essential to ensure that DNA synthesis and subsequent mitotic division are accurately and coordinately executed. There is now strong evidence that CDKs, their regulators, and substrates are the targets of genetic alteration in many human cancers. As a result of this, the CDKs have been targeted for drug discovery and a number of small molecule inhibitors of CDKs have been identified.