Obesity induced in mice by high-fat feeding activates the protein kinase Cdk5 (cyclin-
dependent kinase 5) in adipose tissues. This results in phosphorylation of the nuclear
receptor PPARγ (peroxisome proliferator-activated receptor γ), a dominant regulator of …

PPARγ is the functioning receptor for the thiazolidinedione (TZD) class of antidiabetes drugs
including rosiglitazone and pioglitazone 1. These drugs are full classical agonists for this
nuclear receptor, but recent data have shown that many PPARγ-based drugs have a …

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 …

Binding to helix 12 of the ligand-binding domain of PPARγ is required for full agonist activity.
Previously, the degree of stabilization of the activation function 2 (AF-2) surface was thought
to correlate with the degree of agonism and transactivation. To examine this mechanism, we …

Damage to the insular cortex can profoundly disrupt tobacco addiction in human smokers,
reflected in spontaneous cessation of the tobacco habit and persistently decreased urge to
smoke. Little is known concerning the neurobiological mechanisms through which the insula …

PGC1α is a key transcriptional coregulator of oxidative metabolism and thermogenesis.
Through a high-throughput chemical screen, we found that molecules antagonizing the
TRPVs (transient receptor potential vanilloid), a family of ion channels, induced PGC1α …

The nuclear receptor Rev-erb-α modulates hepatic lipid and glucose metabolism,
adipogenesis and the inflammatory response in macrophages. We show here that Rev-erb-
α is highly expressed in oxidative skeletal muscle and that its deficiency in muscle leads to …

A total synthesis of a structure proposed for himastatin was accomplished. The non‐identity
of the fully synthetic material with himastatin necessitated a revision of the assigned
structure. Confirmation of the revised stereostructure was subsequently confirmed through …

Hypocretin (orexin) and dynorphin are neuropeptides with opposing actions on motivated
behavior. Orexin is implicated in states of arousal and reward, whereas dynorphin is
implicated in depressive-like states. We show that, despite their opposing actions, these …