دورية أكاديمية
Coumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum
| العنوان: | Coumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum |
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| المؤلفون: | Simone Giovannuzzi, Viviana De Luca, Alessio Nocentini, Clemente Capasso, Claudiu T. Supuran |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 680-685 (2022) |
| بيانات النشر: | Taylor & Francis Group, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | carbonic anhydrase, inhibitor, coumarins, plasmodium falciparum, anti-protozoal agents, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | Coumarins were discovered to act as inhibitors of α-carbonic anhydrases (CAs, EC 4.2.1.1) after undergoing hydrolysis mediated by the esterase activity of the enzyme to the corresponding 2-hydroxycinnamic acids. Other classes of CAs among the eight currently known do not possess esterase activity or this activity was poorly investigated. Hence, we decided to look at the potential of coumarins as inhibitors of the η-CA from the malaria-producing protozoan Plasmodium falciparum, PfaCA. A panel of simple coumarins incorporating hydroxyl, amino, ketone or carboxylic acid ester moieties in various positions of the ring system acted as low to medium micromolar PfaCA inhibitors, whereas their affinities for the cytosolic off-target human isoforms hCA I and II were in a much higher range. Thus, we confirm that η-CAs possess esterase activity and that coumarins effectively inhibit this enzyme. Elaboration of the simple coumarin scaffolds investigated here may probably lead to more effective PfaCA inhibitors. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1475-6366 1475-6374 14756366 |
| Relation: | https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374 |
| DOI: | 10.1080/14756366.2022.2036986 |
| URL الوصول: | https://doaj.org/article/147989acf6304c66964b6afec2088733 |
| رقم الأكسشن: | edsdoj.147989acf6304c66964b6afec2088733 |
| قاعدة البيانات: | Directory of Open Access Journals |
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Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2022.2036986 |