作者: Daniela Vullo , Ronny Lehneck , William A Donald , Stefanie Pöggeler , Claudiu T Supuran
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摘要: CAS3 is a newly cloned cytosolic β-class carbonic anhydrase (CA, EC 4.2.1.1) from the filamentous ascomycete Sordaria macrospora. This enzyme has high catalytic activity for physiological CO2 hydration reaction and herein, we report inhibition profile of with anions small molecules. The most effective anions/small molecule inhibitors were diethyl-dithiocarbamate, sulfamide, sulfamate, phenyl boronic arsonic acids, KIs in range 0.89 mM-97 µM. Anions such as iodide, pseudohalides, bicarbonate, carbonate, nitrate, nitrite, hydrogensulfide, stannate, selenate, tellurate, tetraborate, perrhenate, perruthenate, selenocyanide trithiocarbonate low millimolar inhibitors. light halides, sulfate, hydrogensulfite, peroxydisulfate, diphosphate, divanadate, perchlorate, tetrafluoroborate, fluorosulfonate iminodisulfonate did not significantly inhibit this enzyme. These data may be useful developing antifungals based on CA inhibition, considering fact that many reported here used lead molecules and, by incorporating appropriate organic scaffolds, potent nanomolar could developed.