Products, services, reviews and techniques used in lead molecule delivery, formulation and toxicology, using assays and animal models.
Gentronix has launched a new, accurate and fast in vitro mammalian cell genotoxicity assay - GreenScreen HC. The TK6 host cells are p53 competent and familiar to most genetic toxicology laboratories. A patented GFP reporter system exploits the proper regulation of the GADD45a gene. The assay delivers both high specificity and high sensitivity and detects all common mechanistic classes of genotoxin. The 96-well microplate for…
In 2008 Gentronix launches a new S9 protocol to extend the application of the GreenScreen HC assay to include the detection of genotoxic metabolites. Many pharmaceuticals only present a genotoxicity hazard after metabolism and such chemicals are called pro-mutagens or pro-genotoxins. Generally, although not exclusively, the liver is considered responsible for the “metabolic activation” (MA) of promutagens. However, none of t…
BlueScreen HC is based on the fast, accurate GreenScreen HC genotoxicity assay from Gentronix Ltd. BlueScreen HC uses the same human-derived, p53-competent TK6 cells to host a patented reporter system that exploits the proper regulation of the GADD45a gene. However, in place of GFP, BlueScreen HC utilizes a luciferase from the marine copepod Gaussia princeps to generate a luminescent output. The BlueScreen luminescent assa…
BlueScreen HC uses a single cell strain, which permits 8 compounds to be tested across 8 dilutions (2-fold serial), together with untreated and positive controls, in one 96-well microplate. After arraying test compounds and dilutions, growing cells are added to each well. For studies without S9 metabolic activation data are collected after incubation (48h) using a multimode microplate reader. For studies incorporating S9 metab…
The cost of drug discovery continues to rise while the output of new NDAs continues to fall. Consequently it has never been more important to address attrition rates in drug discovery and development. Early indication of toxicity in a molecule or lead family means that discovery resources can be directed either at other chemical series if these are available or towards ‘breeding’ out undesirable properties. Gentronix and Apred…
