Background: The Caco-2 monolayer has been used extensively for the high-throughput
screening of drug permeability and identification of substrates, inhibitors, and inducers of …

Human jejunal permeability (P eff) is determined in the intestinal region with the highest
expression of carrier proteins and largest surface area. Intestinal P eff are often based on …

Chemotherapy forms the mainstay of cancer treatment particularly for patients who do not
respond to local excision or radiation treatment. However, cancer treatment by drugs is …

While drug toxicity (especially hepatotoxicity) is the most frequent reason cited for
withdrawal of an approved drug, no simple solution exists to adequately predict such …

It is now well recognized that membrane efflux transporters, especially P-glycoprotein (P-gp;
ABCB1), play a role in determining the absorption, distribution, metabolism, excretion, and …

We systematically validated a robust 96-well Caco-2 assay via an extended set of 93
marketed drugs with diverse transport mechanisms and quantified by LC/MS/MS, to …

As discussed in earlier articles, predictions of in vivo drug-drug interactions from in vitro
studies is a subject of high interest with obvious therapeutic as well as economic benefits …

MDR1/ABCB1, MRP2/ABCC2, and breast cancer resistance protein (BCRP)/ABCG2 are
expressed in the liver and intestine and contribute to the disposition of many drugs …

This report describes the discovery of the first centrally active allosteric modulators of the
metabotropic glutamate receptor subtype 5 (mGluR5). Appropriately substituted N-(1, 3 …

The blood-brain barrier (BBB) remains one of the greatest challenges for the discovery and
development of treatments for CNS disorders, which to this day remains one of the riskiest …