|Testing a Novel Real Time Cell Viability Assay|
Amy Landreman, Sarah Duellman, Wenhui Zhou, Jolanta Vidugiriene, Brad Hook
Recently developed assay technologies make it possible to use multi-well plate readers to measure the number of live or dead cells in culture in real time over a period of days. Live cells are measured in real time by adding a reagent containing a shrimp-derived luciferase and a pro-substrate directly to the culture medium. Only viable cells can convert the pro-substrate into a luciferase substrate and generate light.
|The P450-Glo™ CYP2B6 Assay: a Rapid and Selective Assay for Measuring CYP2B6 Induction and Inhibition|
Dongping Ma, Hui Wang, Poncho Meisenheimer, James J. Cali
We have developed a luminogenic CYP2B6 assay for biochemical CYP2B6 inhibition and for cell-based CYP2B6 induction studies. Here we present the CYP2B6 luminogenic assay characterization and demonstrate its utility for measuring time dependent CYP2B6 inhibition, and for measuring CYP2B6 induction in cultured primary human hepatocytes with normalization to viable cell count.
|Predicting Regioselectivityand Labilityof Cytochrome P450 Metabolism using Quantum Mechanical Simulations|
Tyzack, Nicholas Foster, Peter Hunt, Matthew Segall
Predicting Regioselectivity and Lability of Cytochrome P450 Metabolism using Quantum Mechanical Simulations
|An HTS-Compatible Plate For Highly Miniaturized Cultures Of Primary Human Bronchial Epithelial Cells At Air-Liquid Interface|
Elizabeth Vu1, Eric Sorscher2, Robert Lowery1, Steven Hayes1
Primary human bronchial epithelial cells (HBE) cultured at air liquid interface (ALI) exhibit striking similarity to the in vivo situation, including both tissue architecture and ion channel functionality. Cultures of this type serve as a gold standard for predicting therapeutic activity in airway diseases such as cystic fibrosis.
|The Prestwick Chemical Library (R), A Valuable Tool for Screening|
Jean-Marie Contreras1, Christophe Morice1, Jean-Marc Simon1, Bruno Didier2, Marie-Louise Jung1 and Thierry Langer3
The Prestwick Chemical Library® (PCL) is Prestwick’s flagship product dedicated to screening. It is a collection of 1280 molecules comprising 100% approved drugs (FDA, EMEA and other agencies) selected for their high chemical and pharmacological diversity. The PCL was designed to reduce the risk of "low quality" hits and therefore the cost of the initial screening, and appears to be an efficient smart library for hit discovery. The PCL comes with an extended fully-annotated database.
|Building a Diverse and Experimentally-Curated Fragment Library|
Andrew Lowerson, Steven LaPlante, Patrick McCarren, and Michael Serrano-Wu
Presenting a new fragment collection with experimentally-determined aqueous solubility that will address a major source of false positives and attrition in fragment screening
|Polymer Microarrays for Biomaterial Development|
Simmonte, M.J.1, Dhaliwal, K.2, Cuschieri, K.3, Graham, S.V.4, Bradley, M.1
The application of polymer microarrays in the discovery of biocompatible and bioactive substrates. Progress towards biomaterial development for the treatment of SIRS (systemic inflammatory response syndrome), and improving cervical cytology.
|DETERMINATION OF THE QUALITY OF ACTIVE INGREDIENTS IN PAIN KILLERS USING GC-MS|
Elizabeth N.M Murago1, Nathan Oyaro1, Anthony N. Gachanja, Onditi O. Anam, Felix M. Mawili, Steve Lancaster
From this study, the pain killers sampled were found to have large error bars suggesting that there exist counterfeit drugs in the market. The brands mostly affected for analysis of acetaminophen were panadol, action, P500, P5500, elymol and neladol. The error bars for caffeine analysis were quite low indicating that all tablets either counterfeit or original maintained the same amount of this active ingredient.
|Human iPSC-derived hepatocytes and cardiomyocytes for drug toxicity testing|
AnnandRR; Vardaro R; Hamilton B; Akakira R; Tamura K; Yoshida S; Lin YC; Toyoda D; Kogami H; Okuda Y; Watanabe T; Inamura M
Human iPS-derived hepatocytes (ReproHepato™) and cardiomyocytes (ReproCardio 2™) are useful for in vitro toxicity assays.