Abduraman, Muhammad Asyraf and Hariono, Maywan and Yusof, Rohana and Abd Rahman, Noorsaadah and Wahab, Habibah A. and Tan, Mei Lan (2018) Development of a NS2B/NS3 protease inhibition assay using AlphaScreen® beads for screening of anti-dengue activities. Heliyon, 4 (12). e01023. ISSN 2405-8440, DOI https://doi.org/10.1016/j.heliyon.2018.e01023.
Full text not available from this repository.Abstract
Background: Dengue infection is an endemic infectious disease and it can lead to dengue fever, dengue hemorrhagic fever, and/or dengue shock syndromes. Dengue NS2B/NS3 protease complex is essential for viral replication and is a primary target for anti-dengue drug development. In this study, a NS2B/NS3 protease inhibition assay was developed using AlphaScreen ® beads and was used to screen compounds for their protease inhibition activities. Methods: The assay system utilized a known NS2B/NS3 peptide substrate, a recombinant of NS2B/NS3 protease with proprietary StrepTactin ® donor and nickel chelate acceptor beads in 384-well format. Results: The optimized assay to screen for NS2B/NS3 protease inhibitors was demonstrated to be potentially useful with reasonable zʹ factor, coefficient variance and signal to background ratio. However, screening of synthesized thioguanine derivatives using the optimized AlphaScreen ® assay revealed weak NS2B/NS3 inhibition activities. Conclusion: The AlphaScreen ® assay to screen for NS2B/NS3 protease inhibitors is potentially applicable for high throughput screening.
| Item Type: | Article |
|---|---|
| Funders: | Sciencefund Grant from the Ministry of Energy, Science, Technology, Environment and Climate Change, Malaysia (MESTECC) (Grant No 02-05-23-SF0006) |
| Uncontrolled Keywords: | Bioinformatics; Biotechnology |
| Subjects: | Q Science > Q Science (General) Q Science > QD Chemistry R Medicine |
| Divisions: | Faculty of Medicine Faculty of Science > Department of Chemistry |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 14 Oct 2019 03:29 |
| Last Modified: | 14 Oct 2019 03:29 |
| URI: | http://eprints.um.edu.my/id/eprint/22731 |
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