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

Endogenous ligands for nuclear receptors: digging deeper

Michael Schupp  1 , Mitchell A Lazar
Affiliations
Review

Endogenous ligands for nuclear receptors: digging deeper

Michael Schupp et al. J Biol Chem. .

Abstract

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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Figures

FIGURE 1.
FIGURE 1.
Summary of metabolic precursors and biosynthetic enzymes of putative ligands for PPARα and PPARγ. Both receptors bind DNA as heterodimers with RXRα to specific PPAR-response elements (PPREs) in _target genes, although the binding is cell type-specific. oxLDL, oxidized LDL; LPL, lipoprotein lipase; 8(S)-HETE, (8S)-hydroxyeicosatetraenoic acid; LNO2, nitrolinoleic acid; 15-dPGJ2, 15-deoxy-Δ12,14-prostaglandin J2.
FIGURE 2.
FIGURE 2.
Heme and cholesterol derivatives as endogenous ligands for Rev-erbα and RORα. Transcriptional control of the heme biosynthesis via the regulation of ALAS1 is shown on the left. Both NRs compete for the same ROR-response element (RORE)-binding site for repression or activation of gene transcription.
See this image and copyright information in PMC

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