The blood-brain barrier is the capillary endothelium between blood and brain that controls what goes in and comes out of the cNs. one major factor contributing to barrier function is a group of ATP-binding cassette (ABC) drug efflux transporters that restrict brain uptake of xenobiotics including a large number of cNs therapeutics. recent research has focused on the regulation of these transpor...

Multidrug resistance efflux transporters threaten to reverse the progress treating infectious disease by extruding a wide range of drug and other cytotoxic compounds. One such drug transporter, EmrE, from the small multidrug resistance family, utilizes proton gradients as an energy source to drive substrate translocation. In an effort to understand the molecular structural basis of this transpo...

1. Abstract 2. Basic principle for corporal drug movement 2.1. Membrane transporters 2.2. Cardiac output distribution 2.3. Gastrointestinal-blood cycling 2.4. Drug distribution throughout the splanchnic organs 2.5. Efflux transportation, blood flow fraction, and drug recycling 3. Phenytoin 3.1. Michaelis-Menten consideration 3.2. Hepatic, intestinal, and renal contribution to phenytoin clearanc...

The multidrug-resistant phenotype of tumor cells is acquired via an increased capability of drug efflux by ABC transporters and causes serious problems in cancer treatment. With the aim to uncover whether changes induced by epigenetic mechanisms in the expression level of drug transporter genes correlates with changes in the drug resistance phenotypes of resistant cells, we studied the expressi...

OBJECTIVE Research identified promising therapeutics in cell models of Amyotrophic Lateral Sclerosis (ALS), but there is limited progress translating effective treatments to animal models and patients, and ALS remains a disease with no effective treatment. One explanation stems from an acquired pharmacoresistance driven by the drug efflux transporters P-glycoprotein (P-gp) and breast cancer-res...

P-glycoprotein (Pgp) and multidrug resistance-associated proteins (MRPs) are ATP-dependent transporters involved in efflux of toxins and xenobiotics from cells. When overexpressed, these transporters can mediate multidrug resistance (MDR) in mammalian cells, and changes in Pgp expression and sequence are associated with drug resistance in helminths. In addition to the role they play in drug eff...

Multi-drug resistance (MDR) of cancer cells severely limits therapeutic outcomes. A proposed mechanism for MDR involves the efflux of anti-cancer drugs from cancer cells, primarily mediated by ATP-binding cassette (ABC) membrane transporters including P-glycoprotein. This article reviews the recent progress of using active ingredients, extracts and formulae from Chinese medicine (CM) in circumv...