BBA - Proteins and Proteomics
Mechanisms of Drug Efflux and Strategies to Combat Them
Edited by Helen Zgurskaya
Volume 1794, Issue 5, Pages 723-870 (May 2009)

The phenomenon of multidrug resistance (MDR) is associated with the ability of a single transporter to expel from cells multiple drugs with different modes of action. By preventing drugs from reaching their targets, multidrug efflux or MDR transporters provide clinically significant resistance against many important chemotherapeutic agents. MDR is a serious problem in treatment of human ailments caused by pathogenic bacteria, fungi, parasites, and cancer.

Functional studies identified MDR transporters in three large, well-characterized superfamilies of proteins: ATP-binding Cassette (ABC), Major Facilitator (MFS), and Resistance-Nodulation-cell Division (RND). In addition, some MDR transporters form a core of the smaller families of transporters such as Small Multidrug Resistance (SMR) (now part of the Drug/Metabolite transporter (DMT) superfamily) and Multidrug and Toxic Extrusion (MATE) families (part of the Multidrug/Pligosaccharidyl-lipid/Polysaccharide (MOP) superfamily).

Genomic studies indicate that the total number of MDR systems is approximately proportional to the total number of all of the transport systems identified in a given organism. A transporter complement itself appears to correlate to both evolutionary history and overall physiology and lifestyles of the organisms. Accordingly, intracellular pathogens seem to contain somewhat limited repertoire of MDRs, presumably due to their stable environment. On the contrary, soil- and plant-associated bacteria generally appear to encode larger variety and a number of MDR transporters, perhaps reflecting much more variable conditions of their own ecological niches. ... Read the full Guest Editor introduction

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