首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Anion inhibition studies of the Zn(II)-bound ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii
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Anion inhibition studies of the Zn(II)-bound ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii

机译:来自革兰氏阴性菌Burkholderia Territorii的Zn(II)Zn(II)Znount-Carbonic Anhydrase的阴离子抑制研究

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Burkholderia territorii , a Gram-negative bacterium, encodes for the ι-class carbonic anhydrase (CA, EC 4.2.1.1) BteCAι, which was recently characterised. It acts as a good catalyst for the hydration of CO 2 to bicarbonate and protons, with a k cat value of 3.0?×?10 5 ?s ?1 and k cat /K M value of 3.9?×?10 7 ?M ?1 s ?1 . No inhibition data on this new class of enzymes are available to date. We report here an anion and small molecules inhibition study of BteCAι, which we prove to be a zinc(II)- and not manganese(II)-containing enzyme, as reported for diatom ι-CAs. The best inhibitors were sulphamic acid, stannate, phenylarsonic acid, phenylboronic acid and sulfamide (K I values of 6.2–94?μM), whereas diethyldithiocarbamate, tellurate, selenate, bicarbonate and cyanate were submillimolar inhibitors (K I values of 0.71–0.94?mM). The halides (except iodide), thiocyanate, nitrite, nitrate, carbonate, bisulphite, sulphate, hydrogensulfide, peroxydisulfate, selenocyanate, fluorosulfonate and trithiocarbonate showed K I values in the range of 3.1–9.3?mM.
机译:Burkholderia Territorii,一种革兰氏阴性细菌,用于最近表征的BTECA1的ι级碳酸酐酶(CA,EC 4.2.1.1)编码。它用作碳酸二氧化合物和质子的水合的良好催化剂,Ak猫值为3.0?×10 5?S?1和K猫/ km值为3.9?×10 7?m?1 s ?1。没有关于这类新类酶的抑制数据可用于迄今为止。我们在此报告了BTECA1的阴离子和小分子抑制研究,我们证明是锌(II) - 而不是硅藻土(II)致硅藻酶,如硅藻ι-CA。最佳抑制剂是硫酸盐,纵象,苯甲酸,苯基硼酸和磺酰胺(Ki值为6.2-94Ω·μm),而二乙基硫代氨基甲酸酯,碲化物,硒酸盐,碳酸氢盐和氰酸酯是亚乳醛氧化抑制剂(ki值0.71-0.94Ω·mm) 。卤化物(碘化物除外),硫氰酸酯,亚硝酸盐,硝酸盐,碳酸盐,亚硫酸氢盐,硫酸盐,氢硫化物,过氧磺酸氢盐,氟烷基酯,氟磺酸盐和三碳酸酯,显示为3.1-9.3ΩΩmm的k i值。

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