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Structure-Based Design of Y-Shaped Covalent TEAD Inhibitors.

Wenchao Lu1, Mengyang Fan2, Wenzhi Ji1

  • 1Department of Chemical and Systems Biology, Chem-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, California 94305, United States.

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Researchers developed MYF-03-176, a selective covalent inhibitor targeting TEAD proteins. This compound effectively inhibits TEAD-regulated gene expression and proliferation in cancer cells, offering a potential therapeutic strategy.

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Area of Science:

  • Molecular Biology
  • Cancer Research
  • Medicinal Chemistry

Background:

  • The Hippo pathway, involving TEAD (Transcriptional Enhanced Associate Domain) proteins, YAP, and TAZ, regulates gene expression.
  • Aberrant TEAD/YAP signaling is linked to various cancers.
  • TEAD proteins are palmitoylated, presenting a druggable target.

Purpose of the Study:

  • To develop a selective, cysteine-covalent inhibitor for TEAD proteins.
  • To evaluate the efficacy of MYF-03-176 (compound 22) in inhibiting TEAD-regulated pathways.

Main Methods:

  • Medicinal chemistry efforts were employed to design and synthesize MYF-03-176.
  • The inhibitor's effect on TEAD-regulated gene expression was assessed.
  • Cell proliferation assays were conducted on TEAD-dependent cancer cell lines.

Main Results:

  • MYF-03-176 was successfully developed as a selective, cysteine-covalent TEAD inhibitor.
  • Compound 22 demonstrated significant inhibition of TEAD-regulated gene expression.
  • MYF-03-176 reduced the proliferation of mesothelioma and liposarcoma cell lines dependent on TEAD.

Conclusions:

  • MYF-03-176 is a potent inhibitor of TEAD proteins.
  • Targeting TEAD palmitoylation offers a promising therapeutic avenue for TEAD-dependent malignancies.