Inside Cover: Silicon Analogues of the RXR-Selective Retinoid Agonist SR11237 (BMS649): Chemistry and Biology (ChemMedChem 7/2009)

The inside cover picture shows a carbon-based (left) and the analogous silicon-based (right) derivative of the highly potent pan-RXR-selective retinoid agonist SR11237. Switching from carbon to silicon increased the biological activity by a factor of ten. To further understand this effect, both agonists were co-crystallized with the ligand-binding domain of hRXRα (superposition of the two crystal structures shown). For more details, see the Full Paper by R. Tacke et al. on p. 1143 ff.