Fluorescence Assay for Type IB DNA Topoisomerases for Use in High-Throughput Screening of Small Molecule Libraries

This invention describes the first continuous spectroscopic assay for DNA topoisomerase IB that allows monitoring of the reaction under multiple turnover conditions. As these enzymes are established targets for anticancer and antiviral drug therapies, this assay allows the rapid screening of chemical libraries for new lead compounds for cancer and viral infectious disease. The assay is especially robust and economical for high-throughput screening applications because sensitive molecular beacon technology is utilized, and the topoisomerase is released during the reaction to allow turnover of multiple substrate molecules by a single enzyme molecule. The utility of the assay has been validated by screening a small molecule library from which several novel lead compounds have already been identified. Description (Set) Proposed Use (Set) Type I DNA topoisomerases are established anticancer, antiviral, antibacterial, and antimalarial drug targets. The invention has the potential to accelerate the identification of new lead compounds for the development of new drugs. The assay may be marketed as a kit for laboratory researchers and as a clinical diagnostic assay.

Inventor(s): Stivers, James T.

Type of Offer: Licensing

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