Cover Picture: Studies of Glutathione Transferase P1‐1 Bound to a Platinum(IV)‐Based Anticancer Compound Reveal the Molecular Basis of Its Activation (Chem. Eur. J. 28/2011)

Abstract

The effectiveness…︁ of platinum‐based cancer drugs are limited by drug resistance and pi class glutathione S‐transferase, a major detoxifying enzyme, plays a role in this resistance. X‐ray crystallography and molecular modeling have been used to visualize how a platinum cancer drug (shown in ball‐and‐stick) is recognized by the dimeric enzyme (protein backbone shown as pink ribbons). The ethacrynate ligands (orange spheres), potent inhibitors of the enzyme, dissociate from the metal‐bound enzyme complex, where they likely diffuse through a surface cavity (grey surface) a short distance to the active sites of each monomer leading to enzymatic inhibition. For more details see the Full Paper by..