Advances toward the development of small molecule transcriptional activators

AEI 16

Jean-Paul Desaulniers, jdesauln@umich.edu, Amberlyn Wands, amwands@umich.edu, and Anna K. Mapp, amapp@umich.edu. Department of Chemistry, University of Michigan, 930 North University Ave, Ann Arbor, MI 48109
Transcription is the first committed step in gene expression, and is tightly regulated by the action of activators and repressors. Diseases are often characterized by aberrant gene expression profiles, and restoring these to their proper levels holds therapeutic promise. We have identified new small molecule scaffolds that activate transcription in mammalian cells. This new repertoire of small molecule activation domains will allow for the potential to target specific cell-types and activator-coactivator complexes. The results of a cellular small molecule screen in S. cerevisiae and human mammalian cells will be described.