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[Progress in the ligands and their complex structures of farnesoid X receptor]

Wei-Hu Li1, Jing Fu, Ming-Yue Zheng

  • 1School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.

Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|August 25, 2012
PubMed

Insights

Farnesoid X receptor (FXR) is a key target for metabolic diseases and diabetes. This review covers diverse FXR ligands, their structure-activity relationships, and recent crystal structure advances.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Farnesoid X receptor (FXR) is a nuclear receptor superfamily member.
  • FXR plays a crucial role in metabolic syndrome and glucose homeostasis.
  • FXR is an important therapeutic target for metabolic diseases and diabetes.

Purpose of the Study:

  • To review diverse Farnesoid X receptor (FXR) ligands.
  • To discuss the structure-activity relationship of FXR ligands.
  • To introduce advances in the crystal structures of FXR in complex with various ligands.

Main Methods:

  • Literature review of FXR agonists and antagonists.
  • Analysis of structure-activity relationships of FXR ligands.
  • Compilation of recent crystal structure data for FXR-ligand complexes.

Main Results:

  • Significant progress has been made in identifying FXR agonists and antagonists.
  • Diverse FXR ligands exhibit varied structure-activity relationships.
  • Recent crystal structures provide insights into FXR-ligand interactions.

Conclusions:

  • FXR remains a promising drug target for metabolic disorders.
  • Understanding FXR ligand interactions is crucial for drug development.
  • Advances in structural biology enhance the design of FXR-modulating therapies.

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