Cover Picture: Breaking the Dogma of the Metal‐Coordinating Carboxylate Group in Integrin Ligands: Introducing Hydroxamic Acids to the MIDAS To Tune Potency and Selectivity (Angew. Chem. Int. Ed. 24/2009)

Abstract

AbstractThe binding of the carboxyl group of an aspartate residue in the metal‐ion‐dependent adhesion site (MIDAS) is a key feature in the binding of ligands to integrins. This finding was demonstrated by the binding of the cyclic pentapeptide cyclo(RGDfNMeV) (Cilengitid) to the integrin αvβ3 (see picture). In their Communication on p. 4436 ff, H. Kessler and co‐workers show that the carboxyl group previously considered essential for binding can be replaced by a hydroxamic acid unit.magnified image