Burkholderia pseudomallei is a Gram-negative saprophytic bacterium responsible of melioidosis, an endemic disease of tropical and sub-tropical regions of the world. A recombinant γ-CA (BpsγCA) identified in the genome of this bacterium was cloned and purified. Its catalytic activity and anion inhibition profiles were investigated. The enzyme was an efficient catalyst for the CO₂ hydration showing a k_cat of 5.3x10⁵ s^-1 and k_cat/K_m of 2.5 x10⁷ M^-1 x s^-1. The best BpsγCA inhibitors were sulfamide, sulfamic acid, phenylboronic acid and phenylarsonic acid, which showed K_I in the range of 49 – 83 μM (these inhibitors showed millimolar inhibition constant against hCA II), followed by diethyldithiocarbamate, selenate, tellurate, perrhenate, selenocyanate, trithiocarbonate, tetraborato, pyrophosphate, stannate, carbonate, bicarbonate, azide, cyanide, thiocyanate and cyanate with K_Is in the range of 0.55–9.1 mM. In our laboratories, work is in progress to resolve the X-ray crystal structures of BpsγCA, which may allow the development of small molecule inhibitors with desired properties for targeting and inhibiting specifically the bacterial over the human CAs, considering the fact that B. pseudomallei is involved in a serious bacterial disease.

中文翻译：

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致病性细菌类假单胞菌伯克霍尔德氏菌中γ-碳酸酐酶的负离子抑制谱，该假单胞菌可导致类鼻oid病并对常见抗生素具有高度耐药性

假伯克霍尔德氏菌是革兰氏阴性腐生细菌，可引起类鼻oid病，后者是世界热带和亚热带地区的地方病。克隆并纯化了在该细菌的基因组中鉴定的重组γ-CA（BpsγCA）。研究了其催化活性和阴离子抑制曲线。该酶是用于CO ₂水合的有效催化剂，显示ak _cat为5.3x10 ⁵ s ^-1，k _cat / K _m为2.5 x10 ⁷ M ^-1 xs ^-1。最好的BpsγCA抑制剂是磺酰胺，氨基磺酸，苯硼酸和苯ar酸，显示出K _I在49 – 83μM的范围内（这些抑制剂显示出对hCA II的毫摩尔抑制常数），然后是二乙基二硫代氨基甲酸酯，硒酸盐，碲酸，高per酸盐，硒代氰酸盐，三硫代碳酸盐，四硼酸盐，焦磷酸盐，锡酸盐，碳酸盐，碳酸氢盐，叠氮化物，氰化物，硫氰酸盐K _I s为0.55–9.1 mM的氰酸盐。在我们的实验室中，目前正在进行解决BpsγCA的X射线晶体结构的工作，考虑到假芽孢杆菌（B. pseudomallei）的事实，这可能允许开发具有所需特性的小分子抑制剂，使其具有靶向和抑制人类CA细菌的特性。与严重的细菌性疾病有关。