Inside Cover: Design and Biological Evaluation of Novel, Balanced Dual PPARα/γ Agonists (ChemMedChem 6/2009)

The inside cover picture shows the X‐ray‐determined binding of an α‐ethoxy‐phenyl‐propionic acid‐derived dual PPARα/γ agonist in complex with PPARα (yellow) and PPARγ (blue). The high α‐selectivity of this phenylthiazole (IC 50 γ/α = 37; EC 50 γ/α = 7) can be rationalized mainly by a single residue difference, Cys 275 (α) vs. Gly 284 (γ), leading to three additional interactions with the terminal p ‐Cl‐Ph group. In addition, its binding site is highlighted in a surface representation of the PPARα protein. For more details, see the Communication by U. Grether et al. on p. 951 ff.