Design, Synthesis, and in-vitro Protease Inhibition Assay of Linear Pentapeptides as Potential Dengue Virus NS۲B/NS۳ Protease Inhibitors
محل انتشار: مجله آرشیو رازی، دوره: 77، شماره: 2
سال انتشار: 1401
نوع سند: مقاله ژورنالی
زبان: انگلیسی
مشاهده: 26
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شناسه ملی سند علمی:
JR_ARCHRAZI-77-2_041
تاریخ نمایه سازی: 6 دی 1402
چکیده مقاله:
Nowadays dengue virus infection (DENV) is one of the major health complications in the world. Although DENV is an old and common disease, unfortunately, until now, there are no specific relevant treatments available for it. This study, therefore, aimed to design, as well as synthesize selective peptide inhibitors, and investigate their activity by in-vitro NS۲B/NS۳ protease inhibition assay. The design of the peptide ligands was based on studying the interactions with the dengue NS۲B/NS۳ protease using the computational docking technique in the MOE and AutoDock (version ۴.۲) software. To this end, the researchers designed ۲۶ linear pentapeptides based on previous studies. It was revealed that two linear pentapeptides (i.e., GKRRK and KRRRK) are the best potential inhibitors. Furthermore, based on the findings of the two independent docking programs, the peptide GKRRK was synthesized by solid-phase peptide synthesis and its structure was confirmed. The in-vitro protease inhibitor study was conducted for these two peptides to examine their activity against the dengue virus using a protin in as a control. It was found that the designed potential peptides possess interesting inhibition against the NS۲B/NS۳ protease. Additionally, the findings showed that the peptide GKRRK had the highest percentage of inhibition (۷۱.۱۱%) at ۱۰۰ µM with the IC۵۰of۴۸.۸۷ µM; therefore, this linear peptide could serve as a good inhibitor for the DENV.
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نویسندگان
N Abdalsatar Abdalrazaq
Discipline of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, University of Science, Malaysia (USM), ۱۱۸۰۰, Penang, Malaysia
E Ezleen Binti Kamarulzaman
Discipline of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, University of Science, Malaysia (USM), ۱۱۸۰۰, Penang, Malaysia
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