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J Biol Chem. 2010 Dec 24;285(52):40409-15. doi: 10.1074/jbc.R110.182451. Epub 2010 Oct 18.

Endogenous ligands for nuclear receptors: digging deeper.

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  • 1Department of Endocrinology, Diabetes, and Nutrition and Center for Cardiovascular Research, Institute of Pharmacology, Charité-University Medicine Berlin, 10115 Berlin, Germany.


Nuclear receptors (NRs) are hormone-sensing transcription factors that translate dietary or endocrine signals into changes in gene expression. Therefore, the adoption of orphan NRs through the identification of their endogenous ligands is a key element for our understanding of their biology. In this minireview, we give an update on recent progress in regard to endogenous ligands for a cluster of NRs with high sequence homology, namely peroxisome proliferator-activated receptors α and γ, Rev-erbα, and related receptors. This knowledge about the nature and physiology of these ligands may create new opportunities for therapeutic drug development.

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