Miguel M. Vaidergorn; Flavio da Silva Emery; A. Ganesan
J. Med. Chem., 2021, 64(19), 13980-14010
https://doi.org/10.1021/acs.jmedchem.1c00787

Abstract

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.