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Cover Picture: ChemBioChem 10/2002
The cover picture shows bovine rhodopsin, the first G-protein-coupled receptor (GPCR) structure determined at atomic resolution. It is embedded into the cell membrane with the conserved seven transmembrane helices. Rhodopsin is unique among GPCRs due to its activation mechanism: The covalently bound ligand retinal (shown in red) undergoes a light-induced isomerization, thus activating the receptor. For other GPCRs intracellular responses are modulated by binding of extracellular signal molecules and drugs. Valsartan, fexofenadine, montelukast, and clapidogrel are examples of drug compounds acting on GPCRs that bind peptides, biogenic amines, lipids, and nucleotides, respectively. Further details can be found in the review article by Klabunde and Hessler on p. 928 ff.