Resistance nodulation cell division (RND)-type efflux transporters play the main role in intrinsic resistance to various antimicrobial agents in many gram-negative bacteria. Here, we estimated 12 RND-type efflux transporter genes in Vibrio parahaemolyticus. Because VmeAB has already been characterized, we cloned the other 11 RND-type efflux transporter genes and characterized them in Escherichi...

INTRODUCTION One of the major patterns of drug-induced liver injury (DILI) observed in man is cholestatic DILI. The mechanisms are complex and include decreased bile formation, which results in increased bile acid levels in blood [1]. Hepatobiliary transporters mediate uptake and excretion of drugs and endogenous substances. It has been proposed that inhibition of biliary efflux transporters ma...

Most members of the large ATP-binding cassette (ABC) gene family are transporters involved in substrate translocation across biological membranes. In eukaryotes, ABC proteins functioning as drug transporters are located in the plasma membrane and mediate the cellular efflux of a wide range of organic chemicals, with some transporters also transporting certain metals. As the enhanced expression ...

Drug transporters are now recognized as major actors in pharmacokinetics, involved notably in drug-drug interactions and drug adverse effects. Factors that govern their activity, localization and expression are therefore important to consider. In the present review, the implications of protein kinases C (PKCs) in transporter regulations are summarized and discussed. Both solute carrier (SLC) an...

Diesel exhaust particles (DEPs) are common environmental air pollutants primarily affecting the lung. DEPs or chemicals adsorbed on DEPs also exert extra-pulmonary effects, including alteration of hepatic drug detoxifying enzyme expression. The present study was designed to determine whether organic DEP extract (DEPe) may target hepatic drug transporters that contribute in a major way to drug d...

The identification and significance of cancer stem-like cells in malignant gliomas remains controversial. It has been proposed that cancer stem-like cells display increased drug resistance, through the expression of ATP-binding cassette transporters that detoxify cells by effluxing exogenous compounds. Here, we investigated the 'side population' phenotype based on efflux properties of ATP-bindi...

The constitutive active/androstane receptor (CAR) is a nuclear that functions as xenobiotic sensor, which regulates the expression of enzymes involved in drug metabolism and efflux transporters. Evaluation binding properties between CAR was assumed to facilitate prediction drug–drug interaction, thereby contributing discovery. purpose this study construct system for rapid evaluation interaction...

Targeted chemotherapy for hepatocellular carcinoma (HCC) is impaired by intrinsic and/or acquired drug resistance. Since drugs used in HCC therapy (e.g. anthracyclines or the tyrosine kinase inhibitor sorafenib) are substrates of uptake and/or efflux transporters, variable expression of these transporters at the plasma membrane of tumor cells may contribute to drug resistance and subsequent cli...

Escherichia coli possesses a number of proteins that transport sugars out of the cell. We identified 31 candidate sugar efflux transporters based on their similarity to known sugar efflux transporters. We then tested whether these transporters affect arabinose and xylose metabolism. We identified 13 transporters - setC, cmr, ynfM, mdtD, yfcJ, yhhS, emrD, ydhC, ydeA, ybdA, ydeE, mhpT, and kgtP -...

The effects of hepatic uptake and efflux transporters on metabolism of digoxin were examined in isolated rat hepatocytes versus microsomes. The metabolic clearance estimated from microsomes was 4.59 +/- 0.69 ml/min/kg. However, the metabolic clearance estimated from hepatocytes was 15.9 +/- 3.0 ml/min/kg. The former did not correlate with in vivo clearance (12.9 ml/min/kg) for digoxin. Rifampin...