首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Comparison of the amine/amino acid activation profiles of the β- and γ-carbonic anhydrases from the pathogenic bacterium Burkholderia pseudomallei
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Comparison of the amine/amino acid activation profiles of the β- and γ-carbonic anhydrases from the pathogenic bacterium Burkholderia pseudomallei

机译:致病性细菌伯克霍尔德菌假马来酸β-和γ-碳酸酐酶的胺/氨基酸活化曲线比较

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Abstract The β-class carbonic anhydrase (CA, EC 4.2.1.1) from the pathogenic bacterium Burkholderia pseudomallei, BpsCAβ, that is responsible for the tropical disease melioidosis was investigated for its activation with natural and non-natural amino acids and amines. Previously, the γ-CA from this bacterium has been investigated with the same library of 19 amines/amino acids, which show very potent activating effects on both enzymes. The most effective BpsCAβ activators were L- and D-DOPA, L- and D-Trp, L-Tyr, 4-amino-L-Phe, histamine, dopamine, serotonin, 2-pyridyl-methylamine, 1-(2-aminoethyl)-piperazine and L-adrenaline with KAs of 0.9–27?nM. Less effective activators were D-His, L- and D-Phe, D-Tyr, 2-(2-aminoethyl)pyridine and 4-(2-aminoethyl)-morpholine with KAs of 73?nM–3.42?μM. The activation of CAs from bacteria, such as BpsCAγ/β, has not been considered previously for possible biomedical applications. It would be of interest to perform studies in which bacteria are cultivated in the presence of CA activators, which may contribute to understanding processes connected with the virulence and colonization of the host by pathogenic bacteria.
机译:摘要研究了致病性细菌假苹果伯克霍尔德菌(BpsCAβ)引起热带类鼻li病的β-类碳酸酐酶(CA,EC 4.2.1.1)对其天然和非天然氨基酸和胺的活化作用。以前,已经用相同的19种胺/氨基酸文库对这种细菌的γ-CA进行了研究,它们对两种酶均显示出非常强的激活作用。最有效的BpsCAβ激活剂是L-和D-DOPA,L-和D-Trp,L-Tyr,4-氨基-L-Phe,组胺,多巴胺,5-羟色胺,2-吡啶基甲胺,1-(2-氨基乙基) )-哌嗪和L-肾上腺素,K A s为0.9–27?nM。效果较差的活化剂为D-His,L-和D-Phe,D-Tyr,2-(2-氨基乙基)吡啶和4-(2-氨基乙基)吗啉,K A 为73 ?nM–3.42?μM。对于可能的生物医学应用,以前尚未考虑过从细菌(如BpsCAγ/β)中激活CA。进行在CA激活剂存在下培养细菌的研究可能会引起人们的兴趣,这可能有助于理解与致病菌对宿主的毒力和定殖有关的过程。

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