Drag transporter

Substrates are usually identified using transfected MDCK, Caco-2, or endothelial cell lines that express the transporter of interest. These cell types are grown in a monolayer on a membrane separating two chambers of culture medium (i.e., the TransweU Cell Culture Assay, Coming Costar Corp., Cambridge, MA). Drag is administered into one chamber, and drag transport across the monolayer is... 

Bosch, T.M., Meijerman, I., Beijnen, J.H., et al. (2006) Genetic polymorphisms of drug-metabolising enzymes and drag transporters in the chemotherapeutic treatment of cancer. Clin. Pharmacokinet. 45, 253-285. 

Kotze, A.F., et al. 1999. Enhancement of paracellular drag transport with highly quatemized, Y-trimethyl chitosan chloride in neutral environments In vitro evaluation in intestinal epithelial cells (Caco-2). J Pharm Sci 88 253. 

In addition to the direct interaction with drug transporters, administration of some kinds of drugs (so-called inducers) modulates the expression of drag transporters, and thereby, affects the pharmacokinetics of other drugs one is modulating membrane trafficking of transporter protein and the other is induction/downregulation of transporter mRNA. 

Describe the basic physical chemistry which may be used to model transdermal drag transport. 

Drag Transport Mediated by SLC and ABC Transporters Using Double Transfected Cells 539... 

Schuldiner S. Structural biology the ins and outs of drag transport. Nature 2006 443 156-157. 

Takatsuka Y, Nikaido H. Threonine-978 in the transmembrane segment of the multidrag efflux pump AcrB of Escherichia coh is crucial for drag transport as a probable component of the proton relay network. J. Bacteriol. 2006 188 7284-7289. 

It can be concluded that the LAT1 and -2 transporters are present atthe BBB. The LAT 1 seems to be more expressed than the LAT2, whereas its Km is approximately a factor of 10 less. The applicability of this transporter for targeted drag transport to the brain has been demonstrated. In addition, its role at the BBB in diseases has been demonstrated with phenylketonuria where the transport of phenylalanine into the brain was blocked. 

An Overview of Caco-2 and Alternatives for Prediction of Intestinal Drag Transport and Absorption... 

Figure 3. Potential in vivo effect of surfactants and/or bile salts on drag transporters.

Lin HC, Li H, Cho HJ, et al. Air-liquid interface (ALI) culture of human bronchial epithelial cell monolayers as an in vitro model for airway drag transport studies. J Hiarm Sci 2007 96 341-350. 

The ABC Transporters Structural Insights into Drag Transport... 

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