Advances in molecular methods have massively facilitated the discovery of potential molecular targets for gene-specific therapy. Accelerated lead discovery has at the same time generated a massive demand for thorough validation of such putative targets. Very often human tissue analysis is needed for this purpose. However, the need to analyse large numbers of well-characterized human tissues constitutes a major bottleneck in drug discovery and development. Traditional tissue analysis in a slide-by-slide manner is slow, expensive and difficult to standardize. In addition, precious specimens, such as tissue samples from clinical studies, are usually exhausted after a few analyses. The tissue microarray technology overcomes these shortcomings as it allows the simultaneous analysis of up to 1,000 minute tissue samples in a single experiment. This article will review how high-throughput tissue microarray analyses can dramatically facilitate translational research at several different levels.