Nuclear receptors are multi-domain transcription factors that bind to DNA elements from
which they regulate gene expression. The peroxisome proliferator-activated receptors
(PPARs) form heterodimers with the retinoid X receptor (RXR), and PPAR-γ has been …

The nuclear receptors REV-ERBα (encoded by NR1D1) and REV-ERBβ (NR1D2) have
remained orphans owing to the lack of identified physiological ligands. Here we show that
heme is a physiological ligand of both receptors. Heme associates with the ligand-binding …

The oxysterol receptors LXR (liver X receptor)-α and LXRβ are nuclear receptors that play a
key role in regulation of cholesterol and fatty acid metabolism. We found that LXRs also play
a significant role in glucose metabolism. Treatment of diabetic rodents with the LXR agonist …

T-helper cells that produce interleukin-17 (TH 17 cells) are a recently identified CD4+ T-cell
subset with characterized pathological roles in autoimmune diseases 1, 2, 3. The nuclear
receptors retinoic-acid-receptor-related orphan receptors α and γt (RORα and RORγt …

Synchronizing rhythms of behaviour and metabolic processes is important for cardiovascular
health and preventing metabolic diseases. The nuclear receptors REV-ERB-α and REV-
ERB-β have an integral role in regulating the expression of core clock proteins driving …

The nuclear receptor peroxisome proliferator-activated receptor γ (PPARγ) promotes
adipocyte differentiation, exerts atherogenic and anti-inflammatory effects in monocyte/
macrophages, and is believed to mediate the insulin-sensitizing action of antidiabetic …

The C terminus of nuclear hormone receptors is a complex structure that contains multiple
functions. We are interested in the mechanism by which thyroid hormone converts its
receptor from a transcriptional silencer to an activator of transcription. Both regulatory …

The farnesoid X receptor (FXR; NR1H4) is a nuclear hormone receptor that functions as the
bile acid receptor. In addition to the critical role FXR plays in bile acid metabolism and
transport, it regulates a variety of genes important in lipoprotein metabolism. We …

The interaction between nuclear receptors and coactivators provides an arena for testing
whether protein–protein interactions may be inhibited by small molecule drug candidates.
We provide evidence that a short cyclic peptide, containing a copy of the LXXLL nuclear …

We characterize the ability of the liver X receptor (LXRα [NR1H3] and LXRβ [NR1H2])
agonist, T0901317, to activate the farnesoid X receptor (FXR [NR4H4]). Although T0901317
is a much more potent activator of LXR than FXR, this ligand actually activates FXR more …