2. Academic Validation
  3. From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD)

From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD)

  • J Med Chem. 2021 Oct 14;64(19):13980-14010. doi: 10.1021/acs.jmedchem.1c00787.
Miguel M Vaidergorn 1,  Flavio da Silva Emery 1,  A Ganesan 2
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo 14040-903, Brazil.
  • 2 School of Pharmacy, University of East Anglia, Norwich NR4 7TJ, United Kingdom.
PMID: 34591474 DOI: 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.

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