From hit seeking to magic bullets: The successful union of epigenetic and fragment based drug discovery (EPIDD + FBDD)

Miguel M. Vaidergorn, Flavio da Silva Emery, A. Ganesan

Research output: Contribution to journalArticlepeer-review

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.
Original languageEnglish
Pages (from-to)13980-14010
Number of pages31
JournalJournal of Medicinal Chemistry
Volume64
Issue number19
Early online date30 Sep 2021
DOIs
Publication statusPublished - 14 Oct 2021

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