Feray Kockar
Balikesir University, Molecular biology-Genetic, Faculty Member
Streptococcus mutans, the oral pathogenic bacterium provoking dental caries formation, encodes for a β-class carbonic anhydrase (CA, EC 4.2.1.1), SmuCA. This enzyme was cloned, characterized and investigated for its inhibition profile... more
Streptococcus mutans, the oral pathogenic bacterium provoking dental caries formation, encodes for a β-class carbonic anhydrase (CA, EC 4.2.1.1), SmuCA. This enzyme was cloned, characterized and investigated for its inhibition profile with the major class of CA inhibitors, the primary sulfonamides. SmuCA has a good catalytic activity for the CO2 hydration reaction, with a kcat of 4.2×10(5)s(-1) and kcat/Km of 5.8×10(7)M(-1)×s(-1), and is efficiently inhibited by most sulfonamides (KIs of 246nM-13.5μM). The best SmuCA inhibitors were bromosulfanilamide, deacetylated acetazolamide, 4-hydroxymethylbenzenesulfonamide, a pyrimidine-substituted sulfanilamide derivative, aminobenzolamide and compounds structurally similar to it, as well as acetazolamide, methazolamide, indisulam and valdecoxib. These compounds showed inhibition constants ranging between 246 and 468nM. Identification of effective inhibitors of this enzyme may lead to pharmacological tools useful for understanding the role o...
Research Interests:
The inhibition of the ??-carbonic anhydrases (CAs, EC 4.2. 1.1) from the pathogenic fungi Cryptococcus neoformans (Can2) and Candida albicans (Nce103) with carboxylates such as the C1???C5 aliphatic carboxylates, oxalate, malonate,... more
The inhibition of the ??-carbonic anhydrases (CAs, EC 4.2. 1.1) from the pathogenic fungi Cryptococcus neoformans (Can2) and Candida albicans (Nce103) with carboxylates such as the C1???C5 aliphatic carboxylates, oxalate, malonate, maleate, malate, pyruvate, lactate ...