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Updated: Oct 9, 2025

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The Small-Molecule Wnt Inhibitor ICG-001 Efficiently Inhibits Colorectal Cancer Stemness and Metastasis by

Jang-Hyun Choi1, Tae-Young Jang1, So-El Jeon1

  • 1School of Life Sciences, Gwangju Institute of Science and Technology, Gwangju 61005, Korea.

International Journal of Molecular Sciences
|December 24, 2021
PubMed

Insights

A new Wnt inhibitor, ICG-001, effectively reduces cancer stemness and metastasis in colorectal cancer (CRC) by targeting MEIS1. This offers a promising new therapeutic strategy for treating metastatic CRC and overcoming treatment resistance.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Stem Cell Research

Background:

  • Colorectal cancer (CRC) recurrence and metastasis are significant challenges in treatment.
  • Cancer stem-like cells (CSCs) drive CRC progression, but effective inhibitors are lacking.
  • Wnt pathway activation and stemness gene upregulation are observed in metastatic CRC.

Purpose of the Study:

  • To investigate the therapeutic potential of the Wnt inhibitor ICG-001 against colorectal cancer stemness and metastasis.
  • To elucidate the molecular mechanisms underlying ICG-001's effects, focusing on the Wnt pathway and stemness genes.

Main Methods:

  • Transcriptomic profiling of metastatic CRC tumors.
  • Treatment of CRC cells with the small-molecule Wnt inhibitor ICG-001.
  • Assessment of self-renewal activity and metastatic potential.
  • Identification and functional analysis of ICG-001 target genes, including MEIS1.

Main Results:

  • ICG-001 treatment significantly reduced cancer stem cell self-renewal and metastatic potential in CRC.
  • MEIS1 was identified as a direct target gene of ICG-001, regulated by Wnt signaling.
  • MEIS1 was found to enhance CSC behavior and metastatic potential in CRC cells.

Conclusions:

  • ICG-001 effectively inhibits colorectal cancer stemness and metastasis by suppressing MEIS1 expression.
  • These findings support the clinical investigation of ICG-001 as a targeted therapy for CSCs in CRC.
  • ICG-001 represents a potential new therapeutic avenue for treating metastatic colorectal cancer.
Keywords:
ICG-001MEIS1Wntcancer stem-like cellscolorectal cancermetastasis

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