Bile acids: Natural ligands for an orphan nuclear receptor

Derek J. Parks, Steven G. Blanchard, Randy K. Bledsoe, Gyan Chandra, Thomas G. Consler, Steven A. Kliewer, Julie B. Stimmel, Timothy M. Willson, Ann Marie Zavacki, David D. Moore, Jürgen M. Lehmann

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1528 Scopus citations

Abstract

Bite 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 bite acids and their conjugates modulated interaction of FXR with a peptide derived from steroid receptor coactivator 1. These results provide evidence for a nuclear bite acid signaling pathway that may regulate cholesterol homeostasis.

Original languageEnglish (US)
Pages (from-to)1365-1368
Number of pages4
JournalScience
Volume284
Issue number5418
DOIs
StatePublished - May 21 1999

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ASJC Scopus subject areas

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Cite this

Parks, D. J., Blanchard, S. G., Bledsoe, R. K., Chandra, G., Consler, T. G., Kliewer, S. A., Stimmel, J. B., Willson, T. M., Zavacki, A. M., Moore, D. D., & Lehmann, J. M. (1999). Bile acids: Natural ligands for an orphan nuclear receptor. Science, 284(5418), 1365-1368. https://doi.org/10.1126/science.284.5418.1365