Targeting YAP/TAZ-TEAD and their protein-protein interaction for precision cancer therapy

Fangyuan Chen1, Jinxuan Su2, Yongqi Liu3

  • 1Department of Ophthalmology, Guangzhou Red Cross Hospital of Jinan University, Guangzhou, 510220, China.

Insights

The Hippo pathway

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • The Hippo signaling pathway regulates cell proliferation and organ size.
  • Its dysregulation is linked to various human cancers.
  • YAP (Yes-associated protein) and TAZ (transcriptional coactivator with PDZ-binding motif) are key effectors, interacting with TEAD transcription factors.

Purpose of the Study:

  • To review the structure and mechanisms of YAP/TAZ-TEAD interactions.
  • To provide an overview of therapeutic strategies targeting the YAP/TAZ-TEAD axis in cancer.
  • To highlight the potential of targeting YAP/TAZ-TEAD for precision cancer therapy.

Main Methods:

  • Literature review of YAP/TAZ-TEAD interactions.
  • Analysis of recent advances in chemical compounds targeting YAP, TAZ, and TEAD.
  • Discussion of protein-protein interaction inhibitors and PROTAC technology.

Main Results:

  • The YAP/TAZ-TEAD axis drives oncogenic gene expression.
  • Targeting YAP/TAZ-TEAD interactions is a promising therapeutic strategy.
  • Novel inhibitors and PROTACs targeting this axis are under development and in clinical trials.

Conclusions:

  • The YAP/TAZ-TEAD axis is a critical target for cancer therapy.
  • Inhibiting YAP/TAZ-TEAD interactions offers potential for precision oncology.
  • Recent breakthroughs enhance the therapeutic prospects of targeting this pathway.

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