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Updated: Jun 19, 2025

Monitoring Hippo Signaling Pathway Activity Using a Luciferase-based Large Tumor Suppressor LATS Biosensor
Published on: September 13, 2018
Strategies that regulate Hippo signaling pathway for novel anticancer therapeutics
Na Li1, Yun-He Liu1, Ji Wu1
1School of Pharmaceutical Sciences, Institute of Drug Discovery & Development, Key Laboratory of Advanced Drug Preparation Technologies (Ministry of Education), Zhengzhou University, Zhengzhou, 450001, China.
Abstract:
As a highly conserved signaling network across different species, the Hippo pathway is involved in various biological processes. Dysregulation of the Hippo pathway could lead to a wide range of diseases, particularly cancers. Extensive researches have demonstrated the close association between dysregulated Hippo signaling and tumorigenesis as well as tumor progression. Consequently, targeting the Hippo pathway has emerged as a promising strategy for cancer treatment. In fact, there has been an increasing number of reports on small molecules that target the Hippo pathway, exhibiting therapeutic potential as anticancer agents. Importantly, some of Hippo signaling pathway inhibitors have been approved for the clinical trials. In this work, we try to provide an overview of the core components and signal transduction mechanisms of the Hippo signaling pathway. Furthermore, we also analyze the relationship between Hippo signaling pathway and cancers, as well as summarize the small molecules with proven anti-tumor effects in clinical trials or reported in literatures. Additionally, we discuss the anti-tumor potency and structure-activity relationship of the small molecule compounds, providing a valuable insight for further development of anticancer agents against this pathway.
Insights
The Hippo pathway is crucial for biological processes and its dysregulation is linked to cancer. This study reviews Hippo pathway inhibitors as potential anticancer agents, discussing their efficacy and structure-activity relationships for future drug development.
Area of Science:
- Molecular Biology
- Oncology
- Pharmacology
Background:
- The Hippo pathway is a conserved signaling network regulating organ size and development.
- Dysregulation of the Hippo pathway is implicated in various diseases, notably cancer, affecting tumorigenesis and progression.
Purpose of the Study:
- To provide an overview of the Hippo signaling pathway's core components and mechanisms.
- To analyze the link between Hippo signaling and cancer.
- To summarize small molecule inhibitors targeting the Hippo pathway with demonstrated anti-tumor effects.
Main Methods:
- Literature review of Hippo pathway signaling.
- Analysis of the relationship between Hippo pathway dysregulation and cancer.
- Compilation and discussion of small molecule inhibitors targeting the Hippo pathway.
Main Results:
- The Hippo pathway plays a significant role in cell proliferation, apoptosis, and tissue homeostasis.
- Numerous small molecules targeting the Hippo pathway have shown therapeutic potential.
- Some Hippo pathway inhibitors are progressing through clinical trials for cancer treatment.
Conclusions:
- Targeting the Hippo pathway represents a promising strategy for cancer therapy.
- Understanding the structure-activity relationships of small molecule inhibitors is key for developing effective anticancer agents.
- Further research into Hippo pathway modulators could lead to novel cancer treatments.
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