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Identification of adropin as a secreted factor linking dietary macronutrient intake with energy homeostasis and lipid metabolism.
TLDR
Adropinregulated expression of hepatic lipogenic genes and adipose tissue peroxisome proliferator-activated receptor gamma, a major regulator of lipogenesis, may be a factor governing glucose and lipid homeostasis, which protects against hepatosteatosis and hyperinsulinemia associated with obesity. Expand
Structure of the intact PPAR-γ–RXR-α nuclear receptor complex on DNA
TLDR
Structures of intact PPAR-γ and RXR-α are presented as a heterodimer bound to DNA, ligands and coactivator peptides, allowing the ligand-binding domain (LBD) of PPar-γ to contact multiple domains in both proteins. Expand
Regulation of Circadian Behavior and Metabolism by Synthetic REV-ERB Agonists
TLDR
Treatment of diet-induced obese mice with a REV-ERB agonist decreased obesity by reducing fat mass and markedly improving dyslipidaemia and hyperglycaemia, indicating that synthetic REV -ERB ligands that pharmacologically target the circadian rhythm may be beneficial in the treatment of sleep disorders as well as metabolic diseases. Expand
Identification of heme as the ligand for the orphan nuclear receptors REV-ERBα and REV-ERBβ
TLDR
Results from experiments of heme depletion in mammalian cells indicate that heme binding to REV-ERB causes the recruitment of the co-repressor NCoR, leading to repression of target genes including BMAL1, an essential component of the circadian oscillator. Expand
REV-ERB and ROR nuclear receptors as drug targets
TLDR
This Review focuses on the latest developments in ROR and REV-ERB pharmacology indicating that these nuclear receptors are druggable targets and that ligands targeting these receptors may be useful in the treatment of several disorders. Expand
Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta.
TLDR
Results from experiments of heme depletion in mammalian cells indicate that heme binding to REV-ERB causes the recruitment of the co-repressor NCoR, leading to repression of target genes including BMAL1, an essential component of the circadian oscillator. Expand
Suppression of TH17 Differentiation and Autoimmunity by a Synthetic ROR Ligand
TLDR
The data demonstrate the feasibility of targeting the orphan receptors RORα and RORγt to inhibit specifically TH17 cell differentiation and function, and indicate that this novel class of compound has potential utility in the treatment of autoimmune diseases. Expand
The tau 4 activation domain of the thyroid hormone receptor is required for release of a putative corepressor(s) necessary for transcriptional silencing.
TLDR
This study has identified and characterized several functional domains within the ligand binding domain of the human thyroid hormone receptor (TR beta) conferring transactivation and proposed a general model in which the role of hormone is to induce a conformational change in the receptor that subsequently affects the action of tau 4, leading to both relief of silencing and transcriptional activation. Expand
T0901317 is a dual LXR/FXR agonist.
TLDR
Although T0901317 is a much more potent activator of LXR than FXR, this ligand actually activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. Expand
Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy
TLDR
It is shown that Rev-erb-α is highly expressed in oxidative skeletal muscle and that its deficiency in muscle leads to reduced mitochondrial content and oxidative function, as well as upregulation of autophagy, which results in compromised exercise capacity. Expand
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