Caister Academic Press

Structures of Multidrug Efflux Pumps from the MFS, SMR, MATE, and ABC Transporter Families

Geoffrey Chang, Paul Szewczyk and Xiao He
from: Microbial Efflux Pumps: Current Research (Edited by: Edward W. Yu, Qijing Zhang and Melissa H. Brown). Caister Academic Press, U.K. (2013)

Abstract

Drug efflux pumps play an important role in multidrug resistance (MDR) affecting the treatment of several diseases like infection and cancer. In this chapter, we review some of the molecular structures of MDR transporters that have their substrate binding sites located in the lipid bilayer. These transporters include those from the major facilitator superfamily (MFS), small multidrug resistance (SMR) family, the multidrug and toxic-compound extrusion (MATE) family, and the ATP-binding cassette (ABC) family. From these models, common structural themes have emerged that are consistent with their function, including a hydrophobic substrate binding pocket comprising of several aromatic residues facilitating poly-specificity, V-shapes to allow access of substrate from the lipid bilayer, and distinct inward- and outward-facing conformations facilitating transport across the cell membrane read more ...
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