Cloning, Characterization, and Inhibition Studies of a β-Carbonic Anhydrase from Brucella suis
2010
A β-carbonic anhydrase (CA, EC 4.2.1.1) from the bacterial pathogen Brucella suis, bsCA I, has been cloned, purified, and characterized kinetically. bsCA 1 has appreciable activity as catalyst for the hydration of CO 2 to bicarbonate, with a k cat of 6.4 x 10 5 s ―1 and k cat /K m of 3.9 x 10 7 M ―1 ·s ―1 . A panel of 38 sulfonamides and one sulfamate have been investigated for inhibition of this new β-CA, All types of activities have been detected, with K I s in the range of 17 nM to 5.87 μM. The best bsCA 1 inhibitors were ethoxzolamide (17 nM), celecoxib (18 nM), dorzolamide (21 nM), valdecoxib, and sulpiride (19 nM). Whether bsCA 1 inhibitors may have application in the fight against brucellosis, an endemic disease and the major bacterial zoonosis, producing debilitating infection in humans and animals, warrants further studies.
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