Heterobifunctional molecules tackle targeted protein dephosphorylation

Trends Pharmacol Sci. 2022 Apr;43(4):263-265. doi: 10.1016/j.tips.2022.01.005. Epub 2022 Jan 31.

Abstract

Recently, Chen and colleagues reported the development of phosphatase-targeting chimeric molecules (PhosTACs), heterobifunctional small molecules that promote targeted, proximity-induced protein dephosphorylation. This strategy represents an innovative approach to selectively manipulate phosphoprotein function and provides proof-of-concept for a new class of bifunctional small molecules in the chemical biologist's toolbox.

Keywords: PhosTACs; dephosphorylation; heterobifunctional; phosphatase; phosphoprotein.

MeSH terms

  • Humans
  • Phosphoproteins* / metabolism
  • Phosphorylation
  • Protein Processing, Post-Translational*

Substances

  • Phosphoproteins