دورية أكاديمية
Specific Targeting of Plant and Apicomplexa Parasite Tubulin through Differential Screening Using In Silico and Assay-Based Approaches
| العنوان: | Specific Targeting of Plant and Apicomplexa Parasite Tubulin through Differential Screening Using In Silico and Assay-Based Approaches |
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| المؤلفون: | Emmanuelle Soleilhac, Loraine Brillet-Guéguen, Véronique Roussel, Renaud Prudent, Bastien Touquet, Sheena Dass, Samia Aci-Sèche, Vinod Kasam, Caroline Barette, Anne Imberty, Vincent Breton, Marylin Vantard, Dragos Horvath, Cyrille Botté, Isabelle Tardieux, Sylvaine Roy, Eric Maréchal, Laurence Lafanechère |
| المصدر: | International Journal of Molecular Sciences, Vol 19, Iss 10, p 3085 (2018) |
| بيانات النشر: | MDPI AG, 2018. |
| سنة النشر: | 2018 |
| المجموعة: | LCC:Biology (General) LCC:Chemistry |
| مصطلحات موضوعية: | Tubulin, dinitroanilines, plant cells, Toxoplasma gondii, Plasmodium falciparum, virtual screening, small molecules, cell-based assays, Biology (General), QH301-705.5, Chemistry, QD1-999 |
| الوصف: | Dinitroanilines are chemical compounds with high selectivity for plant cell α-tubulin in which they promote microtubule depolymerization. They target α-tubulin regions that have diverged over evolution and show no effect on non-photosynthetic eukaryotes. Hence, they have been used as herbicides over decades. Interestingly, dinitroanilines proved active on microtubules of eukaryotes deriving from photosynthetic ancestors such as Toxoplasma gondii and Plasmodium falciparum, which are responsible for toxoplasmosis and malaria, respectively. By combining differential in silico screening of virtual chemical libraries on Arabidopsis thaliana and mammal tubulin structural models together with cell-based screening of chemical libraries, we have identified dinitroaniline related and non-related compounds. They inhibit plant, but not mammalian tubulin assembly in vitro, and accordingly arrest A. thaliana development. In addition, these compounds exhibit a moderate cytotoxic activity towards T. gondii and P. falciparum. These results highlight the potential of novel herbicidal scaffolds in the design of urgently needed anti-parasitic drugs. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1422-0067 19103085 |
| Relation: | http://www.mdpi.com/1422-0067/19/10/3085; https://doaj.org/toc/1422-0067 |
| DOI: | 10.3390/ijms19103085 |
| URL الوصول: | https://doaj.org/article/789a13bed3834bf68035d3301dfb0715 |
| رقم الأكسشن: | edsdoj.789a13bed3834bf68035d3301dfb0715 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14220067 19103085 |
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| DOI: | 10.3390/ijms19103085 |