Editorial [ “Spirit” of High Throughput Screening Guest Editors: Holger Wesche, Shou-Hua (Josh) Xiao and Steve Young ]

The last two decades have seen the rapid and extensive adoption of an increasingly diverse portfolio of automated high throughput technologies by the pharmaceutical and biotechnology industries. Such approaches are now established as a ubiquitous and integral component of modern drug discovery. From the inception of high throughput screening up until the early 90s', such techniques were predominantly applied to facilitate rapid high volume evaluation of low molecular weight chemical libraries. These early screening campaigns were performed primarily by the pharmaceutical industry with the goal of identifying small molecule modulators for novel drug targets. Today the preponderance of chemical drug leads are derived from high throughput screening, the success of which has resulted in over a hundred candidates in clinical trials or approved for marketing. At the beginning of the new millennium, sequencing of the human genome marked the beginning of what has popularly been termed the “genomic revolution”. High throughput technologies were enthusiastically adopted by biotechnology companies and applied to many aspects of modern biomedical research enabling systematic research endeavors on a scale not previously possible. Notable examples include expansive campaigns to sequence genomes or ESTs, automated gene expression profiling programs and protein/protein interaction mapping projects etc. This new target discovery paradigm generated many potential drug targets, which in turn needed to be screened against compound libraries to identify new drug candidates. In consequence, the demand for more, better, faster, more flexible and cost-effective technologies grew and was eagerly addressed by an ever growing field of equipment manufacturers and service companies. These new machines increasingly opened the world of high throughput research to ever more scientists across a broadening and increasingly diverse catalogue of disciplines. Consequently, high throughput approaches are no longer limited to industry, as they largely were in the early days; many academic institutions have established screening and technology centers. In addition, the application of high throughput techniques has expanded far beyond pharmaceutical and genomics laboratories and is revolutionizing all aspects of biology and drug discovery. Inevitably, new opportunities have brought new challenges. In particular, the enormous quantity of data now being routinely generated has driven the rapid development of new data capture, analysis and storage capabilities. This has been, and remains, critical in overcoming persistent limitations in the timely and effective utilization of the new data. This special issue of Combinatorial Chemistry & High Throughput Screening was conceived with the objective of bringing together leading scientists from diverse fields to give a broad overview of the impact of modern high throughput approaches on the whole process of drug discovery from target identification to lead identification and lead optimization.