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Sulfonamide Inhibition Studies of the β-Class Carbonic Anhydrase CAS3 from the Filamentous Ascomycete Sordaria macrospora .

التفاصيل البيبلوغرافية
العنوان: Sulfonamide Inhibition Studies of the β-Class Carbonic Anhydrase CAS3 from the Filamentous Ascomycete Sordaria macrospora .
المؤلفون: Vullo D; Dipartimento di Chimica Ugo Schiff, Università degli Studi di Firenze, 50019 Sesto Fiorentino (Florence), Italy., Lehneck R; Institute of Microbiology and Genetics, Department of Genetics of Eukaryotic Microorganisms, Georg-August-University, 37077 Gottingen, Germany., Donald WA; University of New South Wales, School of Chemistry, Sydney, NSW 2052, Australia., Pöggeler S; Institute of Microbiology and Genetics, Department of Genetics of Eukaryotic Microorganisms, Georg-August-University, 37077 Gottingen, Germany., Supuran CT; University of New South Wales, School of Chemistry, Sydney, NSW 2052, Australia.; Neurofarba Dept., Section of Pharmaceutical and Nutriceutical Sciences, Università degli Studi di Firenze, 50019 Sesto Fiorentino (Florence), Italy.
المصدر: Molecules (Basel, Switzerland) [Molecules] 2020 Feb 25; Vol. 25 (5). Date of Electronic Publication: 2020 Feb 25.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, c1995-
مواضيع طبية MeSH: Structure-Activity Relationship*, Carbonic Anhydrase Inhibitors/*chemistry , Carbonic Anhydrases/*chemistry , Sordariales/*enzymology, Acetazolamide/chemistry ; Amino Acid Sequence/genetics ; Benzolamide/chemistry ; Carbonic Anhydrase Inhibitors/classification ; Carbonic Anhydrase Inhibitors/pharmacology ; Carbonic Anhydrases/genetics ; Carbonic Anhydrases/isolation & purification ; Ethoxzolamide/chemistry ; Humans ; Kinetics ; Methazolamide/chemistry ; Sulfanilamide/chemistry ; Sulfonamides/chemistry ; Thiazines/chemistry
مستخلص: A new β-class carbonic anhydrase was cloned and purified from the filamentous ascomycete Sordaria macrospora, CAS3. This enzyme has a higher catalytic activity compared to the other two such enzymes from this fungus, CAS1 and CAS2, which were reported earlier, with the following kinetic parameters: k cat of (7.9 ± 0.2) × 10 5 s -1 , and k cat /K m of (9.5 ± 0.12) × 10 7 M -1 ∙s -1 . An inhibition study with a panel of sulfonamides and one sulfamate was also performed. The most effective CAS3 inhibitors were benzolamide, brinzolamide, dichlorophnamide, methazolamide, acetazolamide, ethoxzolamide, sulfanilamide, methanilamide, and benzene-1,3-disulfonamide, with K I s in the range of 54-95 nM. CAS3 generally shows a higher affinity for this class of inhibitors compared to CAS1 and CAS2. As S. macrospora is a model organism for the study of fruiting body development in fungi, these data may be useful for developing antifungal compounds based on CA inhibition.
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فهرسة مساهمة: Keywords: Sordaria macrospora; antifungals; carbonic anhydrase; fungus; kinetics; sulfonamide
المشرفين على المادة: 0 (Carbonic Anhydrase Inhibitors)
0 (Sulfonamides)
0 (Thiazines)
21240MF57M (Sulfanilamide)
9451Z89515 (brinzolamide)
EC 4.2.1.1 (Carbonic Anhydrases)
FC5AAH89R5 (Benzolamide)
O3FX965V0I (Acetazolamide)
W733B0S9SD (Methazolamide)
Z52H4811WX (Ethoxzolamide)
تواريخ الأحداث: Date Created: 20200229 Date Completed: 20201201 Latest Revision: 20201201
رمز التحديث: 20231215
مُعرف محوري في PubMed: PMC7179226
DOI: 10.3390/molecules25051036
PMID: 32106611
قاعدة البيانات: MEDLINE
الوصف
تدمد:1420-3049
DOI:10.3390/molecules25051036