Epigenetic mechanisms work in concert to control transcriptional activity by altering the chromatin landscape of cells. Until recently, enzymatic modulators of writer and eraser classes have been the main focus of therapeutic development. Operating at the interface of translating histone marks, reader domains that recognize the histone code written in acetyl and methyl marks have now emerged as viable targets for therapeutic development. In particular, the BET bromodomain family of readers has gained significant attention for the treatment of human cancers, with several inhibitors developed and clinical-stage programs now underway. Adding to the collection of the already robust targets in reader, writer and eraser classes, strategies are now emerging to regulate gene activity by targeting components of remodelers such as the mammalian SWI/SNF chromatin remodeling complex – which displays functional mutations in several human cancers. In total, chromatin-associated proteins and readers represent significant opportunities for therapeutic intervention far beyond previously imagined.
Cambridge Healthtech Institute’s Second Annual Targeting Epigenetic Readers and Chromatin Remodelers meeting will unite academic and industry researchers for the development of chemical probes, and clinical-stage inhibitors to further our understanding of the therapeutic opportunities associated with targeting reader domains and chromatin remodelers.
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