Title data
Innocenti, Alessio ; Mühlschlegel, Fritz A. ; Hall, Rebecca A. ; Steegborn, Clemens ; Scozzafava, Andrea ; Supuran, Claudiu T.:
Carbonic anhydrase inhibitors: inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions.
In: Bioorganic & Medicinal Chemistry Letters.
Vol. 18
(2008)
Issue 18
.
- pp. 5066-5070.
ISSN 1464-3405
DOI: https://doi.org/10.1016/j.bmcl.2008.07.122
Abstract in another language
The catalytic activity and inhibition of the beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic fungi Candida albicans (Nce103) and Cryptococcus neoformans (Can2) with inorganic anions such as halogenides, pseudohalogenides, bicarbonate, carbonate, nitrate, nitrite, hydrogen sulfide, bisulfite, perchlorate, sulfate were investigated. The two enzymes showed appreciable CO(2) hydrase activity (k(cat) in the range of (3.9-8.0)x10(5)s(-1), and k(cat)/K(m) in the range of (4.3-9.7)x10(7)M(-1)s(-1)). Can2 was weakly inhibited by cyanide and sulfamic acid (K(I)s of 8.22-13.56 mM), while all other anions displayed more potent inhibition. Nce103 was strongly inhibited by cyanide and carbonate (K(I)s of 10-11 microM), and weakly inhibited by sulfate, phenylboronic, and phenyl arsonic acid (K(I)s of 14.15-30.85 mM). These data demonstrate that pathogenic, fungal beta-CAs may be targets for the development of antifungals that have a novel mechanism of action.
Further data
Item Type: | Article in a journal |
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Refereed: | Yes |
Additional notes: | PubMed-ID: 18723348 |
Institutions of the University: | Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry > Chair Biochemistry - Univ.-Prof. Dr. Clemens Steegborn Faculties Faculties > Faculty of Biology, Chemistry and Earth Sciences Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry |
Result of work at the UBT: | No |
DDC Subjects: | 500 Science > 540 Chemistry |
Date Deposited: | 16 Apr 2015 12:09 |
Last Modified: | 25 Apr 2022 12:26 |
URI: | https://eref.uni-bayreuth.de/id/eprint/10306 |