دورية أكاديمية
أعرض في EDS

Cloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke, Schistosoma mansoni .

التفاصيل البيبلوغرافية
العنوان: Cloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke, Schistosoma mansoni .
المؤلفون: Haapanen S; Faculty of Medicine and Health Technology, Tampere University, Tampere, Finland., Angeli A; Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Sesto Fiorentino, Italy., Tolvanen M; Department of Computing, University of Turku, Turku, Finland., Emameh RZ; Department of Energy and Environmental Biotechnology, National Institute of Genetic Engineering and Biotechnology (NIGEB), Tehran, Iran., Supuran CT; Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Sesto Fiorentino, Italy., Parkkila S; Faculty of Medicine and Health Technology, Tampere University, Tampere, Finland.; Fimlab Ltd, Tampere University Hospital, Tampere, Finland.
المصدر: Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2023 Dec; Vol. 38 (1), pp. 2184299.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Taylor & Francis Country of Publication: England NLM ID: 101150203 Publication Model: Print Cited Medium: Internet ISSN: 1475-6374 (Electronic) Linking ISSN: 14756366 NLM ISO Abbreviation: J Enzyme Inhib Med Chem Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basingstoke, UK : Taylor & Francis, c2002-
مواضيع طبية MeSH: Parasites* , Carbonic Anhydrases*, Animals ; Schistosoma mansoni ; Benzolamide ; Cloning, Molecular
مستخلص: Schistosoma mansoni is an intestinal parasite with one β-class carbonic anhydrase, SmaBCA. We report the sequence enhancing, production, catalytic activity, and inhibition results of the recombinant SmaBCA. It showed significant catalytic activity on CO 2 hydration in vitro with k cat 1.38 × 10 5  s -1 and k cat / K m 2.33 × 10 7 M -1  s -1 . Several sulphonamide inhibitors, from which many are clinically used, showed submicromolar or nanomolar inhibitory effects on SmaBCA. The most efficient inhibitor with a K I of 43.8 nM was 4-(2-amino-pyrimidine-4-yl)-benzenesulfonamide. Other effective inhibitors with K I s in the range of 79.4-95.9 nM were benzolamide, brinzolamide, topiramate, dorzolamide, saccharin, epacadostat, celecoxib, and famotidine. The other tested compounds showed at least micromolar range inhibition against SmaBCA. Our results introduce SmaBCA as a novel target for drug development against schistosomiasis, a highly prevalent parasitic disease.
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فهرسة مساهمة: Keywords: Carbonic anhydrase; Schistosoma mansoni; anti-parasitic agents; inhibitor; sulphonamide
المشرفين على المادة: FC5AAH89R5 (Benzolamide)
EC 4.2.1.1 (Carbonic Anhydrases)
تواريخ الأحداث: Date Created: 20230301 Date Completed: 20230302 Latest Revision: 20230304
رمز التحديث: 20231215
مُعرف محوري في PubMed: PMC9980027
DOI: 10.1080/14756366.2023.2184299
PMID: 36856011
قاعدة البيانات: MEDLINE
الوصف
تدمد:1475-6374
DOI:10.1080/14756366.2023.2184299