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 …

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 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 …

Will the real dictyostatin please stand up? There were five finalists as stereostructures for the
potent anticancer agent dictyostatin; ten, if one were to include enantiomers. A total
synthesis of (−)‐dictyostatin (1) has ended the decade‐old masquerade and identified the …

(−)-Dictyostatin is a sponge-derived, 22-member macrolactone natural product shown to
cause cells to accumulate in the G2/M phase of the cell cycle, with changes in intracellular
microtubules analogous to those observed with paclitaxel treatment. Dictyostatin also …

Structures of 1 and 2 have notable similarities, although the carbon backbone of dictyostatin
2 is two atoms longer and there are stereochemical and other differences. A hypothetical condensation
of the carbamate NH 2 group of discodermolide 1 with the proximate 6 lactone carbonyl group …

The proposed gross structure and relative configuration of gliocladin C (1) was based on mass
spectrometric and spectroscopic data, with the absolute configuration being undefined. 2 The
most novel structural feature of gliocladin C is the trioxopiperazine ring, which is an extremely …

A mixture of four stereoisomers whose configurations are encoded by fluorous silyl
protecting groups has been prepared and converted over 22 steps to a mixture of protected
dictyostatins. Demixing by fluorous HPLC followed by removal of the fluorous protecting …

PPARγ is a target for insulin-sensitizing drugs such as glitazones, which improve plasma
glucose maintenance in patients with diabetes. Synthetic ligands have been designed to
mimic endogenous ligand binding to a canonical ligand-binding pocket to hyperactivate …

(−)-16-Normethyldictyostatin has been made by total synthesis and is a potent antitumor
agent in cells expressing wild-type tubulin and in one mutant cell line that is resistant to
paclitaxel, but it is much less active than dictyostatin in another paclitaxel-resistant cell line …