Chemical modifications of histones, the proteins around which the genetic material is wrapped, provide an important regulatory layer for gene expression control. In this context, bromodomain proteins function as readers of specific chemical modifications on the histone tails. Given the direct connection between the regulation of gene expression and physiological and pathological processes, molecules interfering with readout of these modifications by the bromodomains have recently emerged as important chemical probes and clinical tools to fight cancer, inflammation and other diseases.
This project aims to provide a modular compound-generation and validation platform for rapid design, synthesis and characterization of potent and selective chemical inhibitors. Our collaboration interfaces in silico design and medicinal chemistry with functional genomics and in vivo models. The compounds resulting from our pipeline have great potential for the study of the chemical modifications that provide epigenetic modulation of transcriptional processes. Further, these small molecule modulators will be made available to the scientific community.
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