|A New Dual Luciferase Assay Using NanoLuc® Enables a Second Generation Coincidence Reporter System to Reduce False Hits in HTS Poster|
Christopher Eggers, Samuel Hasson, Brock Binkowski, Matt Robers, James Unch, Braeden Butler, , Keith Wood, James Inglese and Frank Fan
Luciferase-based reporter-gene assays remain a cornerstone of high-throughput screening of compounds because of their high sensitivity and dynamic range. However, a substantial number of non-relevant hits can be generated due to direct interaction of compounds with the luciferase reporter.
|CellTiter-Glo® 2.0: A Novel Luminescent Cell Viability Assay with Greatly Enhanced Storage Stability|
Michael P. Valley, James Unch, Poncho L. Meisenheimer, James J. Cali, and Dan F. Lazar
Here we report on the attributes of a novel ATP detection reagent for cell viability with all of the assay performance of the previous CellTiter-Glo® Reagent, but now with markedly enhanced stability as a single component in a liquid format. These new features provide for much greater ease-of-use in that storage of the reagent at 4°C eliminates the requirement for reagent thawing and minimizes temperature equilibration time.
|Design and Validation of Bioluminescent Assays for 3D Cell Culture Models Poster|
Terry L. Riss, Michael P. Valley, Chad A. Zimprich, Andrew L. Niles, Kevin R. Kupcho and Dan F. Lazar
Cells cultured in 3D model systems often acquire relatively large in vivo-like structures compared to the thickness of a 2D monolayer of cells grown on standard plastic plates.
|iPSC-Derived Cardiomyocytes and Luciferase Reporters: A Robust Reporting Platform for Monitoring Cardioprotection and Pathway Biology in Endogenous Human Tissue Cells|
Fiene, S., Thompson, A., Niles, A., Robers, M., Anson, B.
Pathophysiological conditions, medical interventions, and off-target toxicities can all result in cellular oxidative stress. In cardiac myocytes, prolonged and/or excessive oxidative stress can lead to cardiotoxicity: a primary cause of developmental delays, black-box warnings, and post-launch withdrawal of pharmaceuticals.
|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
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