A FRET-based assay for the discovery of West Nile Virus NS2B-NS3 protease inhibitors |
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Authors: | Rebecca N Adamek Roxanne V Maniquis Sabaha Khakoo Michael D Bridges Nicholas T Salzameda |
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Institution: | Department of Chemistry and Biochemistry, California State University, 800 N. State College, Fullerton, CA 92834, United States |
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Abstract: | The West Nile Virus (WNV) has been a worldwide epidemic since the early 1990s. Currently there are no therapeutic treatments for WNV infections. One particular avenue of treatment is inhibition of the NS2B-NS3 protease, an enzyme that is crucial for WNV replication. In our effort to increase the number of NS2B-NS3 protease inhibitors, we report a novel FRET-based high throughput assay for the discovery of WNV NS2B-NS3 protease inhibitors. For this assay, a FRET-based peptide substrate was synthesized and kinetically characterized with the NS2B-NS3 protease. The new substrate exhibits a Km of 3.35 ± 0.31 μM, a kcat of 0.0717 ± 0.0016 s?1 and a kcat/Km of 21,400 ± 2000 M?1 s?1. |
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Keywords: | West Nile Virus NS2B-NS3 protease Inhibitor assay FRET |
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