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Review
. 2018 Nov 5;10(11):422.
doi: 10.3390/cancers10110422.

Targeting the Hippo Pathway for Breast Cancer Therapy

Liqing Wu  1 , Xiaolong Yang  2
Affiliations
Review

Targeting the Hippo Pathway for Breast Cancer Therapy

Liqing Wu et al. Cancers (Basel). .

Abstract

Breast cancer (BC) is one of the most prominent diseases in the world, and the treatments for BC have many limitations, such as resistance and a lack of reliable biomarkers. Currently the Hippo pathway is emerging as a tumor suppressor pathway with its four core components that regulate downstream transcriptional targets. In this review, we introduce the present targeted therapies of BC, and then discuss the roles of the Hippo pathway in BC. Finally, we summarize the evidence of the small molecule inhibitors that target the Hippo pathway, and then discuss the possibilities and future direction of the Hippo-targeted drugs for BC therapy.

Keywords: LATS; MST; TAZ; YAP; breast cancer; hippo pathway; targeted therapy.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Main components of the Hippo pathway and the current Hippo-targeted inhibitors discussed in this review. In mammals, the canonical Hippo pathway consists of four core components that function through phosphorylation: MST, SAV1, LATS, MOB1. Activated LATS phosphorylates YAP/TAZ, preventing them from entering the nucleus by anchoring them to 14-3-3 protein and/or promoting their degradation in the cytoplasm. This interrupts their interactions with the transcription factor TEAD family proteins, which subsequently inhibits cell proliferation and oncogenic transformation and induces apoptosis. Besides, current Hippo-targeted inhibitors discussed in this review, as well as their targets and major mechanisms, are shown in the figure.
See this image and copyright information in PMC

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