Bile Acids: Natural Ligands for an Orphan Nuclear Receptor-Reference-Cited by-同舟云学术

Bile Acids: Natural Ligands for an Orphan Nuclear Receptor

Published:1999-05-21 Issue:5418 Volume:284 Page:1365-1368
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Parks Derek J.¹,Blanchard Steven G.¹,Bledsoe Randy K.²,Chandra Gyan³,Consler Thomas G.²,Kliewer Steven A.³,Stimmel Julie B.²,Willson Timothy M.⁴,Zavacki Ann Marie⁵,Moore David D.⁵,Lehmann Jürgen M.³

Affiliation:

1. Molecular Biochemistry,

2. Molecular Sciences,

3. Molecular Endocrinology,

4. Medicinal Chemistry, Glaxo Wellcome Research and Development, Research Triangle Park NC, 27709, USA.

5. Department of Cell Biology, Baylor College of Medicine, Houston, TX 77030, USA.

Abstract

Bile acids regulate the transcription of genes that control cholesterol homeostasis through molecular mechanisms that are poorly understood. Physiological concentrations of free and conjugated chenodeoxycholic acid, lithocholic acid, and deoxycholic acid activated the farnesoid X receptor (FXR; NR1H4), an orphan nuclear receptor. As ligands, these bile acids and their conjugates modulated interaction of FXR with a peptide derived from steroid receptor coactivator 1. These results provide evidence for a nuclear bile acid signaling pathway that may regulate cholesterol homeostasis.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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