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Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability.
It is concluded that Caco-2 cells grown on collagen-coated polycarbonate membranes should represent a valuable transport model system for the small intestinal epithelium. Expand
Stability of Protein Pharmaceuticals
Current methodology to stabilize proteins is presented, including additives, excipients, chemical modification, and the use of site-directed mutagenesis to produce a more stable protein species. Expand
The Use of Surfactants to Enhance the Permeability of Peptides Through Caco-2 Cells by Inhibition of an Apically Polarized Efflux System
The results suggest that surfactants, which are commonly added to pharmaceutical formulations, may enhance the intestinal absorption of some drugs by inhibiting this apically polarized efflux system. Expand
Are MDCK Cells Transfected with the Human MDR1 Gene a Good Model of the Human Intestinal Mucosa?
MDCK-MDR1 cells are a useful model for screening the P-gp substrate activity of drugs and drug candidates, however, the apparent kinetics constants and affinities of substrates determined in the MDCk- MDR1 cell model may be different than the values obtained in Caco-2 cells. Expand
Enzymes involved in the bioconversion of ester-based prodrugs.
In this review, the most important enzymes involved in the bioconversion of ester-based prodrugs will be discussed in terms of their biology and biochemistry. Expand
Bovine Brain Microvessel Endothelial Cell Monolayers as a Model System for the Blood‐Brain Barrier a
Using primary cultures of brain microvessel endothelial cells, studies are directed at characterization of the blood-brain barrier permeability and metabolic processes that might be exploited as new schemes for drug delivery to the central nervous system. Expand
Paracellular diffusion in Caco-2 cell monolayers: effect of perturbation on the transport of hydrophilic compounds that vary in charge and size.
These studies established an experimental, theoretical, and quantitative template to assess perturbants of the TJ and define the limits, short of detrimental effects, at which the TJs may be sufficiently perturbed for maximal enhancement of permeation of solutes varying in size and charge. Expand
Structure determination of selenomethionyl S-adenosylhomocysteine hydrolase using data at a single wavelength
The crystallographic structure determination of a selenomethionyl-incorporated AdoHcy hydrolase inhibitor complex was accomplished using single wavelength anomalous diffraction data and the direct methods program, Snb v2.0, which produced the positions of all 30 crystallographically distinct selenium atoms. Expand
Are MDCK Cells Transfected with the Human MRP2 Gene a Good Model of the Human Intestinal Mucosa?
The data suggest that MDCK-MRP2 cells overexpress only the 150 kD isoform of MRP2, which is a good model of the human intestinal mucosa and also shows differences in the ability to inhibit vinblastine efflux in Caco-2 cells as compared to MDCk-MRp2 cells. Expand
Catechol O-methyltransferase.