دورية أكاديمية
In-Silico Identified New Natural Sortase A Inhibitors Disrupt S. aureus Biofilm Formation
| العنوان: | In-Silico Identified New Natural Sortase A Inhibitors Disrupt S. aureus Biofilm Formation |
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| المؤلفون: | Kishore Reddy Venkata Thappeta, Li Na Zhao, Choy Eng Nge, Sharon Crasta, Chung Yan Leong, Veronica Ng, Yoganathan Kanagasundaram, Hao Fan, Siew Bee Ng |
| المصدر: | International Journal of Molecular Sciences, Vol 21, Iss 22, p 8601 (2020) |
| بيانات النشر: | MDPI AG, 2020. |
| سنة النشر: | 2020 |
| المجموعة: | LCC:Biology (General) LCC:Chemistry |
| مصطلحات موضوعية: | anti-biofilm activity, sortase A inhibitor, Staphylococcus aureus, MRSA, fibrinogen, molecular docking, Biology (General), QH301-705.5, Chemistry, QD1-999 |
| الوصف: | Sortase A (SrtA) is a membrane-associated enzyme that anchors surface-exposed proteins to the cell wall envelope of Gram-positive bacteria such as Staphylococcus aureus. As SrtA is essential for Gram-positive bacterial pathogenesis but dispensable for microbial growth or viability, SrtA is considered a favorable target for the enhancement of novel anti-infective drugs that aim to interfere with key bacterial virulence mechanisms, such as biofilm formation, without developing drug resistance. Here, we used virtual screening to search an in-house natural compound library and identified two natural compounds, N1287 (Skyrin) and N2576 ((4,5-dichloro-1H-pyrrol-2-yl)-[2,4-dihydroxy-3-(4-methyl-pentyl)-phenyl]-methanone) that inhibited the enzymatic activity of SrtA. These compounds also significantly reduced the growth of S. aureus but possessed moderate mammalian toxicity. Furthermore, S. aureus strains treated with these compounds exhibited reduction in adherence to host fibrinogen, as well as biofilm formation. Hence, these compounds may represent an anti-infective therapy without the side effects of antibiotics. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1422-0067 1661-6596 |
| Relation: | https://www.mdpi.com/1422-0067/21/22/8601; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067 |
| DOI: | 10.3390/ijms21228601 |
| URL الوصول: | https://doaj.org/article/9de240cf4bf74ca78a07f313ac2f55d2 |
| رقم الأكسشن: | edsdoj.9de240cf4bf74ca78a07f313ac2f55d2 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14220067 16616596 |
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| DOI: | 10.3390/ijms21228601 |