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Chemical Features Important for Activity in a Class of Inhibitors Targeting the Wip1 Flap Subdomain

Harichandra D Tagad1, Subrata Debnath1, Victor Clausse2

  • 1Laboratory of Cell Biology, National Cancer Institute, US National Institutes of Health, Bethesda, MD, 20892, USA.

Chemmedchem
|February 25, 2018
PubMed

Insights

Wild-type p53 induced phosphatase 1 (Wip1) negatively regulates tumor suppressors. Researchers analyzed Wip1 inhibitors, discovering new analogues with improved specificity and bioavailability for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Wip1 (PP2Cδ) is a serine/threonine phosphatase that negatively regulates tumor suppressor p53 and its activators.
  • Wip1 dephosphorylates key proteins in cellular stress responses.
  • Wip1 is overexpressed in many human cancers, making it a therapeutic target.

Purpose of the Study:

  • To conduct a structure-activity relationship (SAR) analysis of a Wip1 inhibitor (G-1).
  • To identify novel Wip1 chemical analogues with enhanced specificity and bioavailability.

Main Methods:

  • Extensive structure-activity relationship (SAR) analysis.
  • Chemical synthesis and characterization of Wip1 analogues.

Main Results:

  • Identified key SAR trends for Wip1 inhibition.
  • Discovered novel chemical analogues of G-1 with potent Wip1 inhibitory activity.
  • Demonstrated good specificity and bioavailability for the new analogues.

Conclusions:

  • Wip1 is a viable therapeutic target in cancer.
  • The SAR analysis provides a foundation for developing Wip1-targeted cancer therapies.
  • Novel Wip1 inhibitors with improved pharmacological properties were discovered.
Keywords:
ELISAWip1enzyme kineticsinhibitors

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