Related Experiment Video

Updated: May 23, 2025

Monitoring Hippo Signaling Pathway Activity Using a Luciferase-based Large Tumor Suppressor LATS Biosensor
07:16

Monitoring Hippo Signaling Pathway Activity Using a Luciferase-based Large Tumor Suppressor LATS Biosensor

Published on: September 13, 2018

19.6K

Gracillin suppresses cancer progression through inducing Merlin/LATS protein-protein interaction and activating Hippo

Jin-Xuan Su1, Hai-Xia Zhou1, Zhi-Jing Zhang1,2

  • 1State Key Laboratory of Bioactive Molecules and Druggability Assessment, MOE Key Laboratory of Tumor Molecular Biology, Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Department of Pharmacology, School of Medicine, Jinan University, Guangzhou, 510632, China.

Acta Pharmacologica Sinica
|March 7, 2025
PubMed

Insights

Gracillin, a natural compound, effectively inhibits cancer cell growth and tumor development by activating the Hippo signaling pathway through Merlin/LATS protein interactions. This natural targeted therapy offers a promising new avenue for cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Natural Product Chemistry

Background:

  • Emerging cancer therapies include gene therapy, epigenetic modifications, natural compounds, and precision medicine.
  • Gracillin, a steroidal saponin from herbs, exhibits significant anticancer properties against various malignancies.

Purpose of the Study:

  • To elucidate the molecular mechanisms underlying gracillin's anticancer effects.
  • To investigate gracillin's impact on the Hippo signaling pathway and YAP activity.

Main Methods:

  • In vitro studies using breast cancer, liver cancer, and glioblastoma cell lines.
  • In vivo xenograft tumor models in nude mice.
  • Analysis of protein-protein interactions (PPI) and signaling pathway activation.

Main Results:

  • Gracillin suppressed cancer cell proliferation, migration, and invasion (IC50 ≈ 1 μM).
  • Gracillin activated the Hippo signaling pathway via Merlin/LATS PPI, reducing YAP activity.
  • Gracillin administration inhibited xenograft tumor growth in vivo.

Conclusions:

  • Gracillin demonstrates potent anticancer efficacy through the induction of Merlin/LATS PPI and Hippo signaling activation.
  • Targeting Merlin/LATS PPI represents a viable strategy for developing novel cancer therapeutics.
Keywords:
Hippo signaling pathwayLATSMerlincancer progressiongracillinprotein-protein interaction

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