The Caco-2 cell monolayer: usefulness and limitations
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 …
screening of drug permeability and identification of substrates, inhibitors, and inducers of …
Intestinal permeability and its relevance for absorption and elimination
H Lennernäs - Xenobiotica, 2007 - Taylor & Francis
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 …
expression of carrier proteins and largest surface area. Intestinal P eff are often based on …
Emerging significance of flavonoids as P-glycoprotein inhibitors in cancer chemotherapy
T Bansal, M Jaggi, R Khar… - Journal of pharmacy …, 2009 - journals.library.ualberta.ca
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 …
respond to local excision or radiation treatment. However, cancer treatment by drugs is …
Applications of cytotoxicity assays and pre-lethal mechanistic assays for assessment of human hepatotoxicity potential
JJ Xu, D Diaz, PJ O'Brien - Chemico-biological interactions, 2004 - Elsevier
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 …
withdrawal of an approved drug, no simple solution exists to adequately predict such …
P-glycoprotein recognition of substrates and circumvention through rational drug design
TJ Raub - Molecular pharmaceutics, 2006 - ACS Publications
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 …
ABCB1), play a role in determining the absorption, distribution, metabolism, excretion, and …
Towards prediction of in vivo intestinal absorption using a 96-well Caco-2 assay
S Skolnik, X Lin, J Wang, XH Chen, T He… - Journal of pharmaceutical …, 2010 - Elsevier
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 …
marketed drugs with diverse transport mechanisms and quantified by LC/MS/MS, to …
Transporter-enzyme interactions: implications for predicting drug-drug interactions from in vitro data
LZ Benet, CL Cummins, CY Wu - Current drug metabolism, 2003 - ingentaconnect.com
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 …
studies is a subject of high interest with obvious therapeutic as well as economic benefits …
ATP-dependent transport of rosuvastatin in membrane vesicles expressing breast cancer resistance protein
L Huang, Y Wang, S Grimm - Drug metabolism and disposition, 2006 - ASPET
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 …
expressed in the liver and intestine and contribute to the disposition of many drugs …
Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That …
CW Lindsley, DD Wisnoski, WH Leister… - Journal of medicinal …, 2004 - ACS Publications
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 …
metabotropic glutamate receptor subtype 5 (mGluR5). Appropriately substituted N-(1, 3 …
The role of blood-brain barrier studies in the pharmaceutical industry
A Reichel - Current drug metabolism, 2006 - ingentaconnect.com
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 …
development of treatments for CNS disorders, which to this day remains one of the riskiest …