Small Molecule Transcriptional Modulators
Anna Mapp, University of Michigan

The human body is comprised of several hundred distinct cell types that all share a common genomic template. This diversity arises from regulated expression of individual genes. The first critical step in this process is transcription and is governed by a large number of transcription factors. Transcription involves the recruitment of protein complexes to gene promoters, and transcription factors achieve this recruitment by binding both DNA and coregulatory complexes. Small molecules that can alter transcription hold tremendous utility as chemical probes and therapeutics. To fully realize their potential, however, small molecule transcriptional modulators must be able to orchestrate protein recruitment at gene promoters just like their natural counterparts. Two classes of small molecule transcriptional regulators that have such properties will be described and their application in breast cancer and head and neck cancer will be discussed.

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