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J. Roy, J. Mikolajczyk, and S. Romanov (Nanosyn, Raleigh-Durham, NC)
We introducing a new drug discovery technology for screening antiviral inhibitors: Luminescent Polymerase Activity (LPA) assay. The assay operates in real-time and has high-information yield capabilities for rapid and cost-effective identification of inhibition mechanisms, such as competitive, non-competitive and un-competitive inhibition of viral polymerases. This information allows the identification of target enzyme binding sites, i.e., catalytic vs. allosteric sites, and may be used for a compound’s structure optimization through the implementation of rational drug design strategies. The proposed platform addresses the drawbacks of the existing methods for high-throughput screening of viral inhibitors. It has an additional unique capability to screen weak inhibitors for implementing Fragment-Based Drug Discovery (FBDD) strategies, and provides a viable alternative for the use of NMR and X-ray crystallography in FBDD.