Abstract
A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal development. Disruption of epigenetic control is a frequent event in disease, and the first epigenetic-based therapies for cancer treatment have been approved. A generation of new classes of potent and specific inhibitors for several chromatin-associated proteins have shown promise in preclinical trials. Although the biology of epigenetic regulation is complex, new inhibitors such as these will hopefully be of clinical use in the coming years.
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Acknowledgements
Work in the Helin laboratory is supported by the Danish National Research Foundation, the Danish Cancer Society, the Novo Nordisk Foundation, the Lundbeck Foundation, the European Union, The European Research Council and the Excellence Programme of the University of Copenhagen.
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K.H. is a co-founder of EpiTherapeutic, and is a consultant for and has shares and warrants in the company. D.D. is a GSK shareholder and an employee of Jansen Pharmaceuticals.
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Helin, K., Dhanak, D. Chromatin proteins and modifications as drug targets. Nature 502, 480–488 (2013). https://doi.org/10.1038/nature12751
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DOI: https://doi.org/10.1038/nature12751
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