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Selective targeting of epigenetic reader domains.

Holger Greschik1, Roland Schüle1,2,3, Thomas Günther1

  • 1a Urologische Klinik und Zentrale Klinische Forschung , Universitätsklinikum Freiburg, Medizinische Fakultät, Albert-Ludwigs-Universität Freiburg , Freiburg , Germany.

Expert Opinion on Drug Discovery
|March 10, 2017
PubMed
Summary

Targeting epigenetic readers, crucial in disease, is advancing with new chemical probes. Rigorous validation of these probes is essential for understanding their biological roles and therapeutic potential.

Keywords:
Acetyl-lysine readerchemical probedruggabilityepigenetic readermethyl-lysine readerselectivity

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Area of Science:

  • Epigenetics
  • Chemical Biology
  • Drug Discovery

Background:

  • Epigenetic regulators (writers, erasers, readers) are implicated in diseases.
  • Targeting epigenetic readers, particularly non-BET readers, has lagged behind writers and erasers.
  • Recent development of selective inhibitors and chemical probes for readers offers new therapeutic avenues.

Purpose of the Study:

  • To review recent advances in identifying and validating inhibitors and chemical probes for epigenetic reader domains.
  • To discuss key issues including druggability, probe quality, cellular effects, and cross-talk.
  • To provide expert opinion on the future of targeting epigenetic readers.

Main Methods:

  • Literature review of recent advances in epigenetic reader inhibitor and chemical probe development.
  • Analysis of challenges and requirements for chemical probes targeting epigenetic readers.
  • Discussion of expert opinions on validation and future directions.

Main Results:

  • Significant progress has been made in developing selective inhibitors and chemical probes for various epigenetic reader domains.
  • The importance of stringent validation for chemical probes, including potency, selectivity, and target engagement, is highlighted.
  • Potential challenges such as off-target effects and cross-talk require careful consideration.

Conclusions:

  • Chemical probes are vital tools for elucidating epigenetic reader functions and assessing their therapeutic potential.
  • Future chemical probes must meet higher standards for specificity and potentially target readers within complexes.
  • Further research is needed to fully harness the therapeutic potential of targeting epigenetic readers.