Function first: a powerful approach to post-genomic drug discovery

In the post-genomic era, pharmaceutical researchers must evaluate vast numbers of protein sequences and formulate novel, intelligent strategies for identifying valid targets and discovering leads against them. The identification of small molecules that selectively target proteins or protein families will be aided by knowing the function and/or the structure of the target(s). By identifying protein function first, efficiencies are gained that allow subsequent focus of resources on particular protein families of interest. This article reviews current proteomic-scale approaches to identifying function as a way of accelerating lead discovery.