Inside Cover: Structural Characterization and Computer-Aided Optimization of a Small-Molecule Inhibitor of the Arp2/3 Complex, a Key Regulator of the Actin Cytoskeleton (ChemMedChem 7/2012)



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The inside cover picture shows the optimization of a small-molecule inhibitor of Arp2/3 complex, a seven-subunit 225 kD protein that nucleates branched actin filaments. The X-ray structure of the complex bound to a known inhibitor, CK-666, was solved, and computational, synthetic, and biochemical methods were used to generate a novel inhibitor with improved potency—an important tool compound for dissecting the cellular functions of Arp2/3 complex. For more details, see the Full Paper by Brad J. Nolen et al. on p. 1286 ff.