Kinase inhibitors are an important class of anticancer and anti-inflammatory compounds. Pharmaceutical companies rely on structure activity-genotoxicity evaluations to evaluate off target action of novel drugs (such Ames or other in vitro genotoxicity screens). Effective drugs should be highly targeted and not pleiotropic. Researchers at AstraZeneca have recently shown that promising compounds (that hit the desired target and appear to be non-genotoxic) may target topoisomerases in vivo or show other DNA reactive characteristics. Off target drug action is extremely important to assess and we can help. TopoGEN has numerous tools to help researchers rule in or rule out off target action. Since topoisomerase targeting, DNA adduct formation and genotoxicity/intercalation are mechanistically valid actions of many chemotypes, it is essential to employ cutting edge tools to reveal these events.
Contact us to learn more about how we can help you attain your research goals.