Development of a NS2B/NS3 protease inhibition assay using AlphaScreen® beads for screening of anti-dengue activities

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

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Official URL: https://doi.org/10.1016/j.heliyon.2018.e01023

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
Uncontrolled Keywords: Bioinformatics; Biotechnology
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
R Medicine
Divisions: Faculty of Medicine
Faculty of Science > Dept 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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