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Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
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Targeting TEAD in cancer.

Rohith Battina1, Raneen Rahhal1, Anton Wellstein1

  • 1Lombardi Comprehensive Cancer Center, Georgetown University Medical Center, Washington D.C., United States.

Frontiers in Oncology
|December 5, 2025
PubMed
Summary

Targeting the TEAD-YAP/TAZ complex is a promising cancer therapy. Inhibitors disrupting this interaction are in clinical trials, offering new hope for treating various cancers.

Keywords:
TAZ (Hippo) signalingTEAD familyTEAD inhibitorsYAP (Hippo) signalingYAP/TAZ TEAD signaling

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The Hippo pathway is frequently dysregulated in cancers, promoting tumor growth.
  • The transcription factor TEAD, binding YAP/TAZ co-activators, is crucial for cell proliferation and linked to poor cancer prognosis.

Purpose of the Study:

  • To review the therapeutic potential of targeting TEAD interactions with YAP/TAZ in oncology.
  • To discuss the structure, function, and inhibition of the YAP/TAZ-TEAD complex for cancer treatment.

Main Methods:

  • Review of existing literature on the Hippo pathway, TEAD, YAP/TAZ, and cancer.
  • Analysis of protein-protein interactions and structural data of the TEAD-YAP/TAZ complex.
  • Examination of pharmacological agents targeting the YAP/TAZ-TEAD complex and their clinical trial status.

Main Results:

  • TEAD-YAP/TAZ interactions are critical for oncogenic gene transcription.
  • Several agents targeting the YAP/TAZ-TEAD complex have been developed.
  • TEAD inhibitors are progressing through clinical trials for various cancer types.

Conclusions:

  • Targeting TEAD-YAP/TAZ interactions is a viable therapeutic strategy in oncology.
  • Understanding the YAP/TAZ-TEAD complex informs the development of novel anti-cancer drugs.
  • Clinical trials are evaluating TEAD inhibitors for their efficacy and safety in cancer patients.