Despite the incredible progress in mapping cancer genomes and annotating cancer gene function, a number of challenges (in technology, biology, chemistry, and financial incentive structure) currently impede the rapid translation of genome science into genome-inspired medicine. Industry tends to focus on well-trodden paths with more certain financial outcomes. In contrast, overcoming the major challenges of translating the cancer genome into therapeutics will require highly innovative approaches and the exploration of uncharted territory. Our overarching goal is to develop great answers and general solutions to these challenges, and to facilitate the development of therapeutics directed at biological targets identified through research into the genetics of cancer. Our efforts include both the development of transformative methods and the execution of specific drug discovery projects.