Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader

J Med Chem. 2023 Nov 23;66(22):15269-15287. doi: 10.1021/acs.jmedchem.3c01348. Epub 2023 Nov 15.

Abstract

Protein tyrosine phosphatase nonreceptor Type 2 (PTPN2) is an attractive target for cancer immunotherapy. PTPN2 and another subtype of PTP1B are highly similar in structure, but their biological functions are distinct. Therefore, subtype-selective targeting of PTPN2 remains a challenge for researchers. Herein, the development of small molecular PTPN2 degraders based on a thiadiazolidinone dioxide-naphthalene scaffold and a VHL E3 ligase ligand is described, and the PTPN2/PTP1B subtype-selective degradation is achieved for the first time. The linker structure modifications led to the discovery of the subtype-selective PTPN2 degrader PVD-06 (PTPN2/PTP1B selective index > 60-fold), which also exhibits excellent proteome-wide degradation selectivity. PVD-06 induces PTPN2 degradation in a ubiquitination- and proteasome-dependent manner. It efficiently promotes T cell activation and amplifies IFN-γ-mediated B16F10 cell growth inhibition. This study provides a convenient chemical knockdown tool for PTPN2-related research and a paradigm for subtype-selective PTP degradation through nonspecific substrate-mimicking ligands, demonstrating the therapeutic potential of PTPN2 subtype-selective degradation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Phosphorylation
  • Proteasome Endopeptidase Complex / metabolism
  • Protein Tyrosine Phosphatase, Non-Receptor Type 2* / genetics
  • Protein Tyrosine Phosphatase, Non-Receptor Type 2* / metabolism
  • Ubiquitin-Protein Ligases* / metabolism
  • Ubiquitination

Substances

  • Protein Tyrosine Phosphatase, Non-Receptor Type 2
  • Ubiquitin-Protein Ligases
  • Proteasome Endopeptidase Complex