Elucidation of the Structure and Intermolecular Interactions of a Reversible Cyclic-Peptide Inhibitor of the Proteasome by NMR Spectroscopy and Molecular Modeling
Angewandte Chemie International Edition 49, 3934β3938 (2010)
Complex considerations: The proteasome plays a key role in diseases and is thus an appealing drug target. A structural model (see picture) of the proteasome as a complex with argyrin, a cyclic heptapeptide with antitumoral activity, provides a rationale for the high biological activity of this natural product. The structureβactivity-relationship data available for the drug are discussed on the basis of this model.