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

doi:10.1126/science.284.5418.1365

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

Research output: Contribution to journal › Article › peer-review

1938 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 language	English (US)
Pages (from-to)	1365-1368
Number of pages	4
Journal	Science
Volume	284
Issue number	5418
DOIs	https://doi.org/10.1126/science.284.5418.1365
State	Published - May 21 1999

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title = "Bile acids: Natural ligands for an orphan nuclear receptor",

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.",

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T2 - Natural ligands for an orphan nuclear receptor

AU - Parks, Derek J.

AU - Blanchard, Steven G.

AU - Bledsoe, Randy K.

AU - Chandra, Gyan

AU - Consler, Thomas G.

AU - Kliewer, Steven A.

AU - Stimmel, Julie B.

AU - Willson, Timothy M.

AU - Zavacki, Ann Marie

AU - Moore, David D.

AU - Lehmann, Jürgen M.

PY - 1999/5/21

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AB - 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.

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Bile acids: Natural ligands for an orphan nuclear receptor

Abstract

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