A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia.

  title={A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia.},
  author={Mark J. Evans and Paige E. Mahaney and Lisa A Borges-Marcucci and Kehdih Lai and Shuguang Wang and Julie A Krueger and Stephen J. Gardell and Christine Huard and Robert V. Martinez and George P. Vlasuk and Douglas C. Harnish},
  journal={American journal of physiology. Gastrointestinal and liver physiology},
  volume={296 3},
The nuclear hormone receptor farnesoid X receptor (FXR) plays a critical role in the regulation of bile acid, triglyceride (TG), and cholesterol homeostasis. WAY-362450 (FXR-450/XL335) is a potent synthetic FXR agonist as characterized in luciferase reporter assays and in mediating FXR target gene regulation in primary human and immortalized mouse hepatocytes. In vivo, WAY-362450 dose dependently decreased serum TG levels after 7 days of oral dosing in western diet-fed low-density lipoprotein… CONTINUE READING


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Publications referenced by this paper.
Showing 1-10 of 38 references

Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c.

The Journal of clinical investigation • 2004
View 6 Excerpts
Highly Influenced

Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice.

Proceedings of the National Academy of Sciences of the United States of America • 2006
View 5 Excerpts
Highly Influenced

FXR, a multipurpose nuclear receptor.

View 3 Excerpts
Highly Influenced

The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice.

The Journal of biological chemistry • 2006
View 4 Excerpts
Highly Influenced

A synthetic farnesoid X receptor ( FXR ) agonist promotes cholesterol lowering in models of dyslipidemia

S Wang, JA Krueger, +4 authors DC Harnish
Am J Physiol Gastrointest Liver Physiol • 2009

Activation of the farnesoid X receptor represses PCSK9 expression in human hepatocytes

C Langhi, C Le May, +5 authors B. Cariou
FEBS Lett 582: • 2008
View 2 Excerpts

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