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From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD)
Journal of Medicinal Chemistry  (IF7.446),  Pub Date : 2021-09-30, DOI: 10.1021/acs.jmedchem.1c00787
Miguel M. Vaidergorn, Flavio da Silva Emery, A. Ganesan

We review progress in the application of fragment-based drug discovery (FBDD) to epigenetic drug discovery (EPIDD) targeted at epigenetic writer and eraser enzymes as well as reader domains over the last 15 years. The greatest successes to date are in prospecting for bromodomain binding ligands. From a diverse array of fragment hits, multiple potent and selective compounds ensued, including the oncology clinical candidates mivebresib, ABBV-744, pelabresib, and PLX51107.