Functional genomics is expected to bring about significant advances in the discovery and development of new anticancer agents. Genomics-based drug target discovery will revolutionize how cancer is detected and classified, resulting in more finely tailored therapies. The explosion of information generated by large-scale functional genomics technologies has led to an exponential increase in the number of potential genes and proteins available for pharmaceutical and diagnostic research development. In tapping this potential, the primary challenge is to develop a strategy to integrate and extract meaning from the human genomic sequence information generated since the start of the Human Genome Project, relying on pragmatic strategies to sort and triage this information. Using a suite of integrated, high-throughput genomics technologies developed at CuraGen, we have devised streamlined approaches to identify new gene sequences rapidly, link them to specific diseases using reverse biology and finally validate them as effectors of disease progression. Application of these technologies has enabled us to identify 24 antibody drug targets for further evaluation and possible development as anticancer agents. We will discuss the role of some of the targets in cancer progression.