Targeting Farnesoid X receptor (FXR) for developing novel therapeutics against cancer

Sosmitha Girisa1, Sahu Henamayee1, Dey Parama1

  • 1Department of Biosciences and Bioengineering, Cancer Biology Laboratory and DBT-AIST International Center for Translational and Environmental Research (DAICENTER), Indian Institute of Technology Guwahati, Guwahati, Assam, 781039, India.

Molecular Biomedicine
|January 10, 2022
PubMed

Insights

Farnesoid X receptor (FXR) plays a key role in cancer development and progression. This review explores FXR's diverse roles in various cancers, highlighting its potential as a diagnostic and therapeutic target.

Area of Science:

  • Molecular Biology
  • Oncology
  • Metabolism

Background:

  • Cancer arises from molecular alterations, including differential expression of Farnesoid X receptor (FXR).
  • FXR, a nuclear receptor, regulates bile, cholesterol, lipid, and glucose metabolism.
  • FXR is implicated in cancer and cardiovascular diseases, major global mortality causes.

Purpose of the Study:

  • To review the diverse roles of Farnesoid X receptor (FXR) in various cancers.
  • To explore FXR's potential as a novel biomarker for cancer diagnosis, prognosis, and therapy.
  • To discuss FXR agonists and antagonists in the context of cancer treatment.

Main Methods:

  • Literature review of recent studies on FXR and cancer.
  • Analysis of FXR's association with cancer development and progression.
  • Examination of FXR's modulation of key cell-signalling pathways and targets.

Main Results:

  • FXR overexpression is linked to cancer development and progression in breast, lung, pancreas, and oesophageal cancers.
  • FXR exhibits tissue-specific and cell-specific roles in different cancer types.
  • FXR modulates critical cancer-related pathways including EGFR/ERK, NF-κB, PI3K/AKT, and Wnt/β-catenin.

Conclusions:

  • FXR is a significant factor in cancer biology, influencing multiple signalling pathways.
  • FXR demonstrates high potential as a novel biomarker for cancer diagnosis, prognosis, and therapy.
  • Targeting FXR with agonists or antagonists may offer new therapeutic strategies for cancer.

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