Targeting epigenetic reader domains by chemical biology

Alessandra Cipriano, Gianluca Sbardella (Lead / Corresponding author), Alessio Ciulli (Lead / Corresponding author)

Research output: Contribution to journalReview article

Abstract

Over the past years, growing interest toward post-translational modifications (PTMs) of histones and nonhistone proteins has prompted academia and industrial research groups to develop different approaches to better understand the link between PTMs and pathological states. Selective recognition of PTMs is carried out by reader modules, which mediate the biological readout of epigenetic mechanisms. Progress in medicinal chemistry and chemical biology has contributed to corroborate the role of reader domains in chromatin-binding proteins as potential therapeutic targets. Here, we review the state-of-the-art of the most important small molecules developed to date, with a particular attention on contemporary chemical biology approaches, including photoaffinity probes, cyclic peptides, bifunctional inhibitors, and PROTAC degraders.

Original languageEnglish
Pages (from-to)82-94
Number of pages13
JournalCurrent Opinion in Chemical Biology
Volume57
Early online date30 Jul 2020
DOIs
Publication statusPublished - Aug 2020

Keywords

  • Bromodomain
  • Photo-affinity probes
  • Post-translational modifications
  • PROTACs
  • Reader domains

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