Structural biology and anticancer drug design

The discovery and development of a new drug are parts of a multistep process that starts with the detailed analysis of the disease to be investigated. The next step is the identification of the key biological molecules that are involved in the disease process whereby modulation of these molecules, usually proteins, will likely have a therapeutic effect. Using recombinant DNA technology, these molecules can be produced and functional assays developed to monitor the level of activity in the presence of potential inhibitors. The screening stage of the drug discovery process is a continually evolving field with new technologies being developed to improve the speed, accuracy, and sensitivity of detecting compounds that bind to the target protein (“hits”). Traditionally, functional assays have been used as the primary identifier of compound hits. Over the past decade, however, high-throughput protein crystallography has continued to evolve as a pivotal technique in early hit generation.