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The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?

Youchao Qi1,2,3,4, Guozhen Duan2, Dengbang Wei4

  • 1Department of Veterinary Medicine, College of Agriculture and Animal Husbandry, Qinghai University, Xining 810016, China.

Molecules (Basel, Switzerland)
|August 26, 2022
PubMed

Insights

The G-protein-coupled bile acid receptor TGR5 (Gpbar1) influences various cellular processes and is found throughout the body. TGR5 exhibits dual roles in cancer, acting as both a tumor suppressor and an oncogene.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Oncology

Background:

  • G-protein-coupled bile acid receptor (Gpbar1), also known as TGR5, is a membrane receptor activated by bile acids.
  • TGR5 activation triggers multiple signaling pathways, including AKT, NF-κB, ERK1/2, STAT3, cAMP, RhoA, Epac, and TRPA1.
  • This receptor is broadly distributed across various tissues, including the brain, liver, adipose tissue, and digestive system.

Purpose of the Study:

  • To review the dual role of TGR5 in cancer development.
  • To summarize the tumor-suppressing and oncogenic functions of TGR5.
  • To elucidate the mechanisms underlying TGR5's contradictory effects in different cancer cells.

Main Methods:

  • Literature review of recent studies on TGR5.
  • Analysis of TGR5 signaling pathways and their downstream effects.
  • Examination of TGR5 agonist effects (e.g., INT-777, UDCA, TLCA) on cancer cells.

Main Results:

  • TGR5 regulates key cellular functions such as proliferation, inflammation, adhesion, migration, and insulin release.
  • TGR5 activation by agonists shows inconsistent effects on different cancer cells.
  • Evidence suggests both tumor-suppressing and oncogenic activities of TGR5.

Conclusions:

  • TGR5 plays a complex and context-dependent role in cancer.
  • Understanding TGR5's 'friend' and 'foe' features is crucial for targeted cancer therapies.
  • Further research is needed to fully delineate TGR5's mechanisms in tumorigenesis.
Keywords:
TGR5bile acidscanceroncogenic functions

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