Related Experiment Video

Updated: Jun 14, 2025

Evaluation of Substrate Ubiquitylation by E3 Ubiquitin-ligase in Mammalian Cell Lysates
09:47

Evaluation of Substrate Ubiquitylation by E3 Ubiquitin-ligase in Mammalian Cell Lysates

Published on: May 10, 2022

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Oleuropein regulates ubiquitination-mediated Mcl-1 turnover and exhibits antitumor activity

Wen Liu1,2, Song Peng1,2, Jinzhuang Liao1,2

  • 1Department of Radiology, The Third Xiangya Hospital of Central South University, Changsha, Hunan, PR China.

Cancer Gene Therapy
|June 12, 2025
PubMed

Insights

Oleuropein (Ole) effectively inhibits oral squamous cell carcinoma (OSCC) growth by targeting Mcl-1. This natural compound shows promise as an anti-cancer agent, even overcoming radioresistance in OSCC.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Oral squamous cell carcinoma (OSCC) is a prevalent malignancy with a poor 5-year survival rate, necessitating novel therapeutic approaches.
  • Myeloid leukemia 1 (Mcl-1) is a key oncogenic driver in various cancers, making it a potential therapeutic target.

Purpose of the Study:

  • To investigate the therapeutic potential of oleuropein (Ole) against OSCC.
  • To elucidate the molecular mechanisms underlying Ole's anti-cancer effects in OSCC, focusing on Mcl-1.

Main Methods:

  • In vitro studies assessing OSCC cell viability and molecular pathways.
  • In vivo studies using animal models to evaluate tumor growth and toxicity.
  • Investigation of the Akt-GSK3β-Mcl-1 pathway and β-TRCP-mediated Mcl-1 degradation.

Main Results:

  • Ole dose-dependently suppressed OSCC cell viability.
  • Ole induced Mcl-1 degradation by inhibiting the Akt-GSK3β-Mcl-1 pathway and promoting β-TRCP-mediated ubiquitination.
  • Ole treatment significantly delayed tumor growth in vivo without observable toxicity.
  • Ole demonstrated efficacy in overcoming radioresistance in OSCC, both alone and in combination with radiation.

Conclusions:

  • Ole exhibits significant anti-tumor activity against OSCC by targeting Mcl-1.
  • Ole represents a promising therapeutic agent for OSCC treatment, with potential to enhance radiotherapy efficacy.

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