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Department of Pharmacology

 
Read more at: CGMP and glutathione-conjugate transport in human erythrocytes - The roles of the multidrug resistance-associated proteins, MRP1, MRP4 and MRP5

CGMP and glutathione-conjugate transport in human erythrocytes - The roles of the multidrug resistance-associated proteins, MRP1, MRP4 and MRP5


Read more at: An ABC-type multidrug transporter of Lactococcus lactis possesses an exceptionally broad substrate specificity

An ABC-type multidrug transporter of Lactococcus lactis possesses an exceptionally broad substrate specificity


Read more at: Ligand-induced tertiary structure changes in membrane and cytosolic domains of reconstituted LmrA.

Ligand-induced tertiary structure changes in membrane and cytosolic domains of reconstituted LmrA.


Read more at: Restrictive use of detergents in the functional reconstitution of the secondary multidrug transporter LmrP.

Restrictive use of detergents in the functional reconstitution of the secondary multidrug transporter LmrP.

The histidine-tagged secondary multidrug transporter LmrP was overexpressed in Lactococcus lactis, using a novel protein expression system for cytotoxic proteins based on the tightly regulated, nisin-inducible nisA promoter. LmrP-mediated H+/drug antiport activity in inside-out membrane vesicles was inhibited by detergents, such as Triton X-100, Triton X-114, and Tween 80, at low concentrations that did not affect the magnitude or composition of the proton motive force.


Read more at: The ABC family of multidrug transporters in microorganisms.

The ABC family of multidrug transporters in microorganisms.

Multidrug transporters are membrane proteins that are able to expel a broad range of toxic molecules from the cell. In humans, the overexpression of the multidrug resistance P-glycoprotein (Pgp) and the multidrug resistance-associated protein MRP1 (MRP) is a principal cause of resistance of cancers to chemotherapy. These multidrug transporters belong to the ATP-binding cassette (ABC) family of transport proteins that utilize the energy of ATP hydrolysis for activity. In microorganisms, multidrug transporters play an important role in conferring antibiotic resistance on pathogens.


Read more at: Phosphate transport in prokaryotes: molecules, mediators and mechanisms.

Phosphate transport in prokaryotes: molecules, mediators and mechanisms.

Bacteria have evolved sophisticated Pi transport systems which combine high affinity with coupling to metabolic energy. This review discusses the current evidence concerning the physiological, biochemical, and molecular properties of these Pi transport systems in prokaryotes. Major developments of the past years will be presented with emphasis on three kinds of issues.


Read more at: Multidrug transporters from bacteria to man: similarities in structure and function.

Multidrug transporters from bacteria to man: similarities in structure and function.

Organisms ranging from bacteria to man possess transmembrane transporters which confer resistance to toxic compounds. Underlining their biological significance, prokaryotic and eukaryotic multidrug transport proteins are very similar in structure and function. Therefore, a study of the factors which determine the substrate specificity and energy coupling to drug translocation in 'simple' microorganisms has significance for multidrug resistance of mammalian cells.


Read more at: A bacterial antibiotic-resistance gene that complements the human multidrug-resistance P-glycoprotein gene.

A bacterial antibiotic-resistance gene that complements the human multidrug-resistance P-glycoprotein gene.

Bacteria have developed many fascinating antibiotic-resistance mechanisms. A protein in Lactococcus lactis, LmrA, mediates antibiotic resistance by extruding amphiphilic compounds from the inner leaflet of the cytoplasmic membrane. Unlike other known bacterial multidrug-resistance proteins, LmrA is an ATP-binding cassette (ABC) transporter. The human multidrug-resistance P-glycoprotein, encoded by the MDR1 gene, is also an ABC transporter, overexpression of which is one of the principal causes of resistance of human cancers to chemotherapy. We expressed lmrA in human lung fibroblast cells.


Read more at: Drug efflux proteins in multidrug resistant bacteria.

Drug efflux proteins in multidrug resistant bacteria.

Bacteria contain an array of transport proteins in their cytoplasmic membrane. Many of these proteins play an important role in conferring resistance to toxic compounds. The multidrug efflux systems encountered in prokaryotic cells are very similar to those observed in eukaryotic cells. Therefore, a study of the factors which determine the substrate specificity and energy coupling to drug translocation in bacteria has significance for the general field of multidrug resistance. Three issues will be dealt with in this review.


Read more at: Mechanisms of multidrug transporters.

Mechanisms of multidrug transporters.

Drug resistance, mediated by various mechanisms, plays a crucial role in the failure of the drug-based treatment of various infectious diseases. As a result, these infectious diseases re-emerge rapidly and cause many victims every year. Another serious threat is imposed by the development of multidrug resistance (MDR) in eukaryotic (tumor) cells, where many different drugs fail to perform their therapeutic function.