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Systematic identification of Celastrol-binding proteins reveals that Shoc2 is inhibited by Celastrol

Huang Xiao-Pei1, Chen Ji-Kuai1, Wei Xue1

  • 1Department of Health Toxicology, Faculty of Naval Medicine, Second Military Medical University, Shanghai 200433, P.R. China.

Bioscience Reports
|October 19, 2018
PubMed

Insights

Celastrol, a natural compound, effectively combats colorectal cancer (CRC) by inhibiting tumor growth and metastasis. It targets the Shoc2 protein, thereby suppressing the ERK pathway crucial for cancer cell proliferation and migration.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Colorectal cancer (CRC) is a leading cause of cancer death globally.
  • Celastrol shows potential anti-tumor properties across various cancer types.
  • The specific anti-CRC mechanisms of Celastrol remain largely uncharacterized.

Purpose of the Study:

  • To investigate the anti-tumor effects of Celastrol on human colorectal cancer (CRC).
  • To elucidate the underlying molecular mechanisms of Celastrol's action in CRC.
  • To explore Celastrol's therapeutic potential using in vitro and in vivo models.

Main Methods:

  • Utilized in vitro cell culture and in vivo xenograft models to assess Celastrol's efficacy.
  • Employed protein microarrays to identify key proteins modulated by Celastrol.
  • Investigated the role of Shoc2 and the ERK pathway in Celastrol's anti-cancer effects.

Main Results:

  • Celastrol significantly inhibited proliferation of SW480 CRC cells and reduced xenograft tumor growth in mice.
  • Protein microarray analysis identified Shoc2 as a highly enriched protein affected by Celastrol.
  • Celastrol suppressed ERK1/2 phosphorylation, an effect mimicked by Shoc2 knockdown, which also reduced tumor cell proliferation, colony formation, and migration.

Conclusions:

  • Celastrol demonstrates significant anti-cancer activity against colorectal cancer.
  • Celastrol exerts its effects by targeting the Shoc2 protein and inhibiting the ERK1/2 signaling pathway.
  • These findings establish Celastrol as a potential therapeutic agent for CRC, highlighting its mechanism of action.
Keywords:
CelastrolColorectal cancerERKHuman proteome microarrayShoc2

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