Heterobifunctional molecules tackle targeted protein dephosphorylation.

Trends Pharmacol Sci

Chemical Biology Laboratory, National Cancer Institute, Frederick, MD 21702, USA. Electronic address:

Published: April 2022

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.

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http://dx.doi.org/10.1016/j.tips.2022.01.005DOI Listing

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