Freya Klepsch and Gerhard F. Ecker, University of Vienna, Austria, highlight the Impact of the recent mouse P-glycoprotein structure for structure-based ligand design.

P-Glycoprotein (P-gp) has attracted considerable interest both with respect to its role in tumour cell multidrug resistance and in absorption-distribution and elimination of drugs. Although known for more than 30 years, the understanding of the molecular basis of drug/transporter interaction is still limited, mainly due to the lack of structural information available. Structures of several bacterial homologues and, very recently, of mouse P-gp have become available.

These discoveries are reviewed along with the current status of structural information available and its impact on structure-based drug design.

• Impact of the Recent Mouse P-Glycoprotein Structure for Structure-Based Ligand Design
  F. Klepsch, G. F. Ecker
  Mol. Inf. 2010, 29, 276–286