Environmental Research. Crystal Structure of the EmrE Multidrug Transporter with a Substrate

A major obstacle to effective treatment of bacterial infections is the emergence of drug-resistant strains. Multidrug resistance arises, in part, through the action of integral membrane proteins called multidrug transporters. Multidrug resistance transporters threaten to reverse the progress in treating infectious disease by extruding a wide range of drug and other cytotoxic compounds. Proteins that pump drugs out of bacterial cells contribute to the problem of multidrug resistance in diseases such as tuberculosis. One such drug transporter, EmrE, from the small multidrug resistance family, utilizes proton gradients as an energy source to drive substrate translocation. EmrE makes bacteria resistant to tetracycline, ethidium, and other cationic antibiotics. Developing inhibitors of such proteins could make old drugs effective again. Using the x-ray diffraction data collected on BL11-1 at SSRL, ALS, and APS, Geoffrey Chang’s group at The Scripp