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PTPs: Degrading the Undruggable.

Amy M Barrios
Published in: Journal of medicinal chemistry (2020)
By using a proteolysis-targeting chimera (PROTAC) strategy that couples an allosteric, reversible PTP inhibitor with an E3 ligase targeting ligand through a well-designed linker, the first molecule to successfully inhibit PTP activity through degradation has been developed.
Keyphrases
  • cancer therapy
  • small molecule
  • structural basis