Advances of targeting the YAP/TAZ-TEAD complex in the hippo pathway for the treatment of cancers

The Hippo pathway is an evolutionarily conserved signaling pathway that plays critical roles in the tumori-genesis and progression of breast cancer, oral cancer, rectal cancer, colloid cancer, and so on. YAP/TAZ-TEAD complex is a key knot in the Hippo pathway regulating cell proliferation and stem cell functions. Activation or overexpression of this complex has been proved to lead to cell transformation, proliferation and eventually cancerization. In this review, the association between the alterations of hippo pathway and tumorigenesis of various cancer had been elucidated. The structural basis of YAP/TAZ-TEAD complex is analyzed, and the tar-geting inhibitors are summarized within the medicinal chemistry classification. Moreover, we have also dis-cussed the clinical status and current challenges of these drug candidates, and provide guidance for the future development of inhibitors targeting this pathway, especially YAP/TAZ-TEAD complex.

Automated summary

This review discusses the role of the Hippo pathway in the tumorigenesis of breast cancer, oral cancer, rectal cancer, colloid cancer, and more. It analyzes the structural basis of the YAP/TAZ-TEAD complex and summarizes the targeting inhibitors within medicinal chemistry classification. The clinical status and current challenges of these drug candidates are also discussed, providing guidance for future development of inhibitors, particularly targeting the YAP/TAZ-TEAD complex.