Small Molecule Modulators of Transcription

Abstract

Signal transduction cascades ultimately trigger transcriptional programs that are executed by transcription factors interacting with coactivator or corepressor proteins in large multi‐protein complexes. Despite the difficulties associated with discovering and verifying potent antagonists (or agonists) of protein–protein interaction events, several small molecules have been identified within the last few years that modulate transcription by directly interacting with transcriptional proteins. Some of these small molecules display surprising selectivity and some even show efficacy in vivo. This review summarizes the current status in this developing field to illustrate the emerging opportunities in the chemical biology of transcription.