Chemical approaches to transcriptional regulation.

Given the correlation between many human diseases and mis-regulated transcription, there is a growing need for molecules that can inhibit or mimic key interactions between transcriptional activators and their binding partners. Because transcriptional activators typically participate in many different protein-protein binding events, the identification of small molecules or peptides that specifically target individual interactions represents a significant challenge. In spite of this, several small molecules that preferentially inhibit particular complexes of transcriptional activators or mimic the function of activators have recently been reported. These molecules serve as excellent mechanistic tools for studying transcription and, further, have outstanding therapeutic potential.