The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism.

@article{Jin2013TheAD,
  title={The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism.},
  author={Lihua Jin and Xuhui Feng and Hui Rong and Zhifu Pan and Yuka Inaba and Lin Qiu and Weili Zheng and Shengchen Lin and Rui Wang and Zhao Wang and Shanshan Wang and Hongyan Liu and Song Li and Wen Xie and Yong Li},
  journal={Nature communications},
  year={2013},
  volume={4},
  pages={1937}
}
Farnesoid X receptor (FXR) has important roles in maintaining bile acid and cholesterol homeostasis. Here we report that the antiparasitic drug ivermectin is a ligand for nuclear FXR. We identify ivermectin using a high-throughput compound library screening and show that it induces the transcriptional activity of the FXR with distinctive properties in modulating coregulator recruitment. The crystal structure of ivermectin complexed with the ligand-binding domain of FXR reveals a unique binding… CONTINUE READING
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Identification of novel pathways that control farnesoid X receptor-mediated hypocholesterolemia

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