Epigenetics

Covalent modifications to DNA or histone proteins with various chemical groups can determine whether genes are turned on or off and can thus influence the production of proteins in a cell. This genetic control without altering DNA sequences is crucial in many normal cellular functions. Aberrant epigenetic alterations are present in myriad disease states. Pharmacological manipulation of the various enzymes involved in epigenetic changes in pathological states is an important new target in drug discovery. Writers (methyl and acetyl transferases) are enzymes capable of modifying nucleotide bases and amino acid residues on histones. Erasers (demethylases and deacetylases) remove these same modifications. Readers (bromodomains) are enzymes capable of recognizing specific epigenetic marks that direct a particular transcriptional outcome.

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