Heterobifunctional molecules tackle targeted protein dephosphorylation

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.