Centre d'Etudes d'Agents Pathogenes et Biotechnologies pour la Sante, UMR 5236 CNRS-UM1-UM2, Universite Montpellier II, cc100, Place E Bataillon, 34095 Montpellier, France.
J Med Chem. 2010 Mar 11;53(5):2277-85. doi: 10.1021/jm901855h.
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.
从细菌病原体猪布鲁氏菌中克隆、纯化并在动力学上表征了一种β-碳酸酐酶（CA，EC 4.2.1.1），bsCA1。bsCA1 作为 CO2 水合为碳酸氢盐的催化剂具有相当的活性，kcat 为 6.4 x 10(5) s(-1)，kcat/Km 为 3.9 x 10(7) M(-1).s(-1)。研究了 38 种磺胺类药物和一种磺胺酸盐对这种新型β-CA 的抑制作用。已检测到所有类型的活性，K（I）值在 17 nM 至 5.87 μM 范围内。bsCA1 的最佳抑制剂是乙氧唑胺（17 nM）、塞来昔布（18 nM）、多佐胺（21 nM）、伐地考昔和舒必利（19 nM）。bsCA1 抑制剂是否可能应用于对抗布鲁氏菌病（一种地方性疾病和主要的动物细菌性传染病，导致人类和动物衰弱性感染），这值得进一步研究。
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