The Hippo Pathway as Drug Targets in Cancer Therapy and Regenerative Medicine

Shunta Nagashima, Yijun Bao, Yutaka Hata1

  • 1Department of Medical Biochemistry, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, 1-5-45 Yushima, Bunkyo-ku, Tokyo 113-8519, Japan.

Current Drug Targets
|January 14, 2016
PubMed

Insights

Yes-associated protein 1 (YAP1) and its partner TAZ are key regulators of gene transcription. Their dysregulation in cancer drives disease progression and drug resistance, while their activation is beneficial for tissue repair and regenerative medicine.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Oncology

Background:

  • Yes-associated protein 1 (YAP1) and transcriptional co-activator with PDZ-binding motif (TAZ) are crucial transcriptional co-activators.
  • The Hippo pathway negatively regulates YAP1 and TAZ activity.
  • Deregulation of the Hippo pathway leads to YAP1/TAZ hyperactivation in human cancers.

Purpose of the Study:

  • To discuss the dual role of YAP1 and TAZ in cancer and regenerative medicine.
  • To review the progress in developing YAP1 and TAZ inhibitors and activators as therapeutic agents.

Main Methods:

  • Review of existing literature on YAP1 and TAZ.
  • Analysis of drug screening progress for YAP1 and TAZ modulators.

Main Results:

  • YAP1 and TAZ upregulation promotes epithelial-mesenchymal transition, drug resistance, and cancer stemness, correlating with poor prognosis.
  • YAP1 and TAZ are essential for tissue stem cell function and repair.

Conclusions:

  • Inhibitors of YAP1 and TAZ show promise for cancer therapy.
  • Activators of YAP1 and TAZ are valuable for regenerative medicine applications.
  • Targeting YAP1 and TAZ offers therapeutic potential for various human diseases.

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