Breakthroughs in our understanding of the Ubiquitin system are increasingly being routed towards clinical applications. Targeting Ubiquitin for Drug Discovery and Development conference has assembled leaders from industrial and academic research to discuss the state of the art and prospects for the future. With the FDA approval and commercialization of Velcade, scientists are now beginning to see the potential of this ever expanding science. New therapeutic targets are being explored and implications for new compounds, line-extensions and combination therapies are on the horizon.