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Small Molecule Palmatine Targeting Musashi-2 in Colorectal Cancer

Xue Zhang1, Kaiyan Su1,2, Yifan Liu1

  • 1Shanghai Frontiers Science Center for Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, China.

Frontiers in Pharmacology
|February 14, 2022
PubMed

Insights

Musashi-2 (MSI2) is crucial for colorectal cancer survival. Researchers identified palmatine as a direct MSI2 antagonist, offering a potential new therapy for this malignancy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Musashi-2 (MSI2) is an evolutionarily conserved RNA-binding protein implicated as a therapeutic target in various cancers.
  • The specific mRNAs regulated by MSI2 and functional MSI2 antagonists remain largely uncharacterized.
  • Understanding MSI2's role and identifying antagonists are critical for developing targeted cancer therapies.

Purpose of the Study:

  • To investigate the role of MSI2 in cancer cell survival and identify MSI2-targeted genes.
  • To discover and characterize a functional MSI2 antagonist for potential colorectal cancer therapy.

Main Methods:

  • Generation and analysis of MSI2 knockout cancer cell lines (colorectal HCT116 and non-small cell lung A549).
  • Global transcriptome and proteomic profiling of MSI2 knockout colorectal cancer cells.
  • Loss-rescue screening to identify MSI2 antagonists.
  • Biochemical validation of palmatine's direct binding to MSI2.

Main Results:

  • MSI2 is essential for the survival of colorectal cancer HCT116 cells but not A549 cells.
  • Global profiling identified 38 candidate MSI2-targeted genes in colorectal cancer cells.
  • Palmatine was identified as a functional MSI2 antagonist that inhibits MSI2-dependent colorectal cancer cell growth.
  • Palmatine directly binds to the C-terminal region of MSI2.

Conclusions:

  • MSI2 is a promising therapeutic target for colorectal cancer.
  • Palmatine serves as a direct and functional MSI2 antagonist, indicating its potential for cancer therapy.
Keywords:
RNA-binding proteincolorectal cancermusashi-2musashi-2 targetspalmatine

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