Vaidergorn, Miguel M.
Emery, Flavio da Silva
Total Authors: 3
 Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil
 Univ East Anglia, Sch Pharm, Norwich NR4 7TJ, Norfolk - England
Total Affiliations: 2
Journal of Medicinal Chemistry;
OCT 14 2021.
Web of Science Citations:
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. (AU)