Farnesoid X receptor: From Structure to Function and Its Pharmacology in Liver Fibrosis

Chuan Ding1,2, Zeping Wang1, Xinyue Dou1

  • 1School of Pharmacy, Zhejiang Chinese Medical University, Hangzhou, China.

Aging and Disease
|October 10, 2023
PubMed

Insights

Farnesoid X receptor (FXR) shows promise for treating liver fibrosis by modulating bile acid metabolism. Research highlights FXR’s potential in combating liver disease progression and improving therapeutic options.

Area of Science:

  • Hepatology
  • Molecular Biology
  • Pharmacology

Background:

  • The farnesoid X receptor (FXR) regulates bile acid metabolism and impacts liver health.
  • Liver fibrosis, a precursor to cirrhosis and cancer, has limited FDA-approved treatments.
  • FXR is involved in metabolic disorders, immune function, and liver disease.

Purpose of the Study:

  • To review recent advancements in farnesoid X receptor (FXR) research for liver fibrosis.
  • To explore the potential pharmacological role of FXR in treating hepatic fibrosis.
  • To highlight challenges and mechanisms of FXR in liver fibrosis treatment.

Main Methods:

  • Review of recent fundamental research and clinical investigations on FXR.
  • Analysis of FXR's structure and its implications for drug development.
  • Examination of FXR's role in bile acid metabolism and liver disease progression.

Main Results:

  • FXR plays a critical role in enterohepatic circulation and liver homeostasis.
  • Recent studies reveal FXR's potential as a therapeutic target for liver fibrosis.
  • Progress in understanding FXR's mechanisms offers new avenues for treatment.

Conclusions:

  • FXR is a promising target for developing novel therapies for liver fibrosis.
  • Further research into FXR mechanisms can overcome current therapeutic limitations.
  • Targeting FXR may offer a new strategy to manage liver disease progression.

Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
1.4K
Ultrasound II: Endoscopic Ultrasound and FibroScan01:25

Ultrasound II: Endoscopic Ultrasound and FibroScan

Endoscopic Ultrasound (EUS) and FibroScan are valuable diagnostic tools in gastroenterology and hepatology, each with specific applications and techniques.
Endoscopic Ultrasound (EUS):
131
Liver Regeneration01:24

Liver Regeneration

The liver is an important organ in vertebrates that plays an essential role in metabolism. It is also responsible for storing and redistributing nutrients such as carbohydrates, fats, and vitamins in the body. Additionally, the liver releases bile salts which are critical for digesting food and eliminating toxic metabolites from the body.
Cells of Liver
The liver comprises four major types of cells— hepatocytes, stellate, Kupffer, and sinusoidal endothelial cells. The hepatocytes are...
3.3K
Liver Physiology01:30

Liver Physiology

The liver, an essential organ in the human body, performs over 200 vital functions that can be broadly categorized into metabolic, hematological, endocrine regulation, and bile production.
Metabolic Regulation:
The liver is the central organ involved in regulating blood composition. It stabilizes blood glucose levels, maintaining them within the range of  70–110 mg/dL. When these levels drop, the liver breaks down glycogen reserves and releases glucose into the bloodstream. It can...
593
Introduction to Fibroblasts01:09

Introduction to Fibroblasts

Rudolph Virchow discovered spindle-shaped cells called fibroblasts in 1858. Inactive fibroblasts, called fibrocytes, become activated by various stimuli, such as growth factors and inflammatory cytokines. Activated fibroblasts play a crucial role in wound healing, inflammation, formation of new blood vessels, and cancer progression. Uncontrolled activation of fibroblasts results in fibrosis, the excess deposition of fibrous tissue, which can lead to scarring and affect normal organs. This...
3.1K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
2.0K