Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with anions.
The protein encoded by the Nce103 gene of Saccharomyces cerevisiae, a beta-carbonic anhydrase (CA, EC 4.2.1.1) designated as scCA, has been cloned, purified, characterized kinetically, and investigated for its inhibition with a series simple, inorganic anions such as halogenides, pseudohalogenides, bicarbonate, carbonate, nitrate, nitrite, hydrogen sulfide, bisulfite, perchlorate, sulfate, and some of its isosteric species. The enzyme showed high CO(2) hydrase activity, with a k(cat) of 9.4x10(5) s(-1) and k(cat)/K(m) of 9.8x10(7) M(-1) s(-1). scCA was weakly inhibited by metal poisons (cyanide, azide, cyanate, thiocyanate, K(I)s of 16.8-55.6 mM) and strongly inhibited by bromide, iodide, and sulfamide (K(I)s of 8.7-10.8 microM). The other investigated anions showed inhibition constants in the low millimolar range.
Isik
Semra
S
Department of Chemistry, Science and Art Faculty, Balikesir University, Balikesir, Turkey.
Kockar
Feray
F
Arslan
Oktay
O
Guler
Ozen Ozensoy
OO
Innocenti
Alessio
A
Supuran
Claudiu T
CT
D000086:Acetazolamide / Q000737:chemistry; D000595:Amino Acid Sequence; D000838:Anions; D001965:Bromides / Q000737:chemistry; D002176:Candida albicans / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007454:Iodides / Q000737:chemistry; D007527:Isoenzymes / Q000737:chemistry; D007700:Kinetics; D008956:Models, Chemical; D008969:Molecular Sequence Data; D012441:Saccharomyces cerevisiae / Q000201:enzymology* / Q000378:metabolism; D017386:Sequence Homology, Amino Acid; D013440:Sulfides / Q000737:chemistry
D000838:Anions; D001965:Bromides; D002257:Carbonic Anhydrase Inhibitors; D004791:Enzyme Inhibitors; D007454:Iodides; D007527:Isoenzymes; D013440:Sulfides; D000086:Acetazolamide