Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Journal of Medicinal Chemistry Année : 2010

Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis.

Résumé

A beta-carbonic anhydrase (CA, EC 4.2.1.1) from the bacterial pathogen Brucella suis, bsCA 1, 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 beta-CA. All types of activities have been detected, with K(I)s in the range of 17 nM to 5.87 microM. 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.

Domaines

Bactériologie
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Dates et versions

hal-00509065 , version 1 (10-08-2010)

Identifiants

Citer

Pascale Joseph, François Turtaut, Safia Ouahrani-Bettache, Jean-Louis Montero, Isao Nishimori, et al.. Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis.. Journal of Medicinal Chemistry, 2010, 53 (5), pp.2277-85. ⟨10.1021/jm901855h⟩. ⟨hal-00509065⟩
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