Innocenti, A. and Muhlschlegel, F.A. and Hall, R.A. and Steegborn, C. and Scozzafava, A. and Supuran, C.T. (2008) Carbonic anhydrase inhibitors: Inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions. Bioorganic & Medicinal Chemistry Letters, 18 (18). pp. 5066-5070. ISSN 0960-894X.
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The catalytic activity and inhibition of the beta-carbonic anhydrases (CAs, EC 18.104.22.168) 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 CO2 hydrase activity (k(cat) in the range of (3.9-8.0) x 10(5) s (1), and k(cat)/K-m in the range of (4.3-9.7) x 10(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 mu M), 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.
|Uncontrolled keywords:||beta-carbonic anhydrases; anions; Candida albicans; Nce103; Cryptococcus neoformans; Can2; fungal pathogens|
|Depositing User:||Jane Griffiths|
|Date Deposited:||22 Apr 2009 11:03|
|Last Modified:||28 Mar 2012 10:48|
|Resource URI:||http://kar.kent.ac.uk/id/eprint/15708 (The current URI for this page, for reference purposes)|
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