Chemical epigenetics: the impact of chemical‐ and chemical biology techniques on bromodomain target validation

Epigenetics is currently the focus of intense research across a broad range of disciplines due to its involvement in a multitude of biological processes and disease states. At the molecular level, epigenetic functions result partly from modification of the nucleobases in DNA and RNA, and/or post‐translational modifications (PTMs) of histone proteins. Much evidence has emerged to demonstrate that these modifications are dynamic, with cellular machinery identified to modulate and interpret the marks. Our focus is on bromodomains that bind to acetylated lysine (KAc) residues. Progress in the study of bromodomains, and the development of bromodomain ligands, has been rapid. These advances have been underpinned by many disciplines, but chemistry and chemical biology techniques have undoubtedly played a very significant role. Here we review the key chemistry and chemical biology techniques and approaches that have furthered our study of bromodomains, enabled the development of bromodomain ligands, and played a critical role in the validation of bromodomains as therapeutic targets.

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