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The role of bile acid-activated receptor TGR5 in inflammation and liver diseases

Hongyan Xiang1, Huanyu Xiang1, Shuyun Wang1

  • 1Department of Geriatrics, Chongqing General Hospital, Chongqing University, Chongqing, China.

Frontiers in Physiology
|March 5, 2026
PubMed

Insights

Takeda G-protein-coupled receptor 5 (TGR5) is a bile acid receptor crucial for liver health. Targeting TGR5 shows promise for treating chronic liver diseases by modulating inflammation and metabolism.

Area of Science:

  • Hepatology and Gastroenterology
  • Immunology
  • Metabolic Diseases

Background:

  • Takeda G-protein-coupled receptor 5 (TGR5) is a bile acid receptor with functions beyond bile acid homeostasis.
  • TGR5 activation influences metabolic disorders and inflammatory responses via multiple mechanisms.
  • The receptor is widely expressed in liver cells, highlighting its central role in hepatic physiology and pathology.

Purpose of the Study:

  • To review the involvement of TGR5 in diverse liver diseases.
  • To summarize TGR5's regulatory roles in immune cells and inflammatory pathways.
  • To evaluate TGR5 as a therapeutic target for chronic liver conditions.

Main Methods:

  • Literature review consolidating current evidence on TGR5 in liver pathologies.
  • Summary of TGR5's regulatory functions in immune and inflammatory pathways.
  • Analysis of TGR5's therapeutic potential and future research directions.

Main Results:

  • TGR5 is implicated in metabolic dysfunction-associated steatohepatitis, cholestatic diseases, liver fibrosis, and hepatocellular carcinoma.
  • TGR5 modulates immune cell function and inflammatory signaling.
  • The receptor plays a pivotal role in regulating liver metabolism and inflammation.

Conclusions:

  • TGR5 is a promising therapeutic target for chronic liver diseases due to its role in inflammation and metabolism.
  • Future research should focus on developing tissue-specific TGR5 agonists for enhanced efficacy and reduced side effects.
  • Further elucidation of TGR5's dual roles in hepatocarcinogenesis is necessary for safe clinical application.
Keywords:
bile acidshepatocellular carcinomainflammationliver fibrosismetabolic dysfunction-associated fatty liver diseasetgr5

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