New technologies have greatly increased the scientist's ability to investigate complex molecular interactions that occur in cancer development and to identify genetic alterations and drug targets. However, these new capabilities have not accelerated drug development efforts; rather, they may be contributing to increased research and development costs because the large number of new drug targets discovered through genomics need to be investigated in great detail to characterize their putative functional involvement in the disease process. One solution to this bottleneck in functional analysis is the use of high-throughput technologies to produce efficient processes that can rapidly handle the large flood of information at every stage of disease. This review examines the use of new and emerging DNA, tissue, and live-cell transfection microarray technologies that can be used to discover, validate, and translate information resulting from the completion of the Human Genome Project.