Our review on advanced chemical genetics for epigenetics is now published in Current Opinion in Chemical Biology!

  • Graphical abstract
  • Figure 1. Chemical genetics, and its use in epigenetics.
  • Figure 2. Chemical probes as chemical tools.
  • Figure 3. Selective target inhibition via bump-and-hole.
  • Figure 4. Chemically induced protein degradation via PROTAC.
  • Publication Certificate

Well done Andrew, Kwok-Ho and Michael!

Read our review open access here.

Review synopsis: In conventional chemical genetics, cell-active small-molecules directly block protein activity, altering phenotype. However these molecules may not be sufficiently selective or effective at modulating complex epigenetic pathways. By mutating the target protein, and creating a mutant-selective inhibitor, the bump-and-hole approach can provide single-target selectivity. PROTAC molecules direct their target to proteosomal degradation by recruiting an E3 ubiquitin ligase, resulting in more efficacious target downregulation.