a Neurofarba Department, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Sesto Fiorentino , Italy.
b Istituto di Bioscienze e Biorisorse , CNR , Napoli , Italy.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):1178-1185. doi: 10.1080/14756366.2019.1630617.
The activation of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacteria and with amine and amino acids was investigated. BsuCA 1 was sensitive to activation with amino acids and amines, whereas FtuCA was not. The most effective BsuCA 1 activators were L-adrenaline and D-Tyr (Ks of 0.70-0.95 µM). L-His, L-/D-Phe, L-/D-DOPA, L-Trp, L-Tyr, 4-amino-L-Phe, dopamine, 2-pyridyl-methylamine, D-Glu and L-Gln showed activation constants in the range of 0.70-3.21 µM. FtuCA was sensitive to activation with L-Glu (K of 9.13 µM). Most of the investigated compounds showed a weak activating effect against FtuCA (Ks of 30.5-78.3 µM). Many of the investigated amino acid and amines are present in high concentrations in many tissues in vertebrates, and their role in the pathogenicity of the two bacteria is poorly understood. Our study may bring insights in processes connected with invasion and pathogenic effects of intracellular bacteria.
研究了细菌 和 的β 类碳酸酐酶（CAs，EC 4.2.1.1）与胺和氨基酸的相互作用。BsuCA1 对氨基酸和胺的激活敏感，而 FtuCA 则不敏感。最有效的 BsuCA1 激活剂是 L-肾上腺素和 D-Tyr（Ks 值为 0.70-0.95μM）。L-His、L-/D-Phe、L-/D-DOPA、L-Trp、L-Tyr、4-氨基-L-Phe、多巴胺、2-吡啶基甲胺、D-Glu 和 L-Gln 的激活常数在 0.70-3.21μM 范围内。FtuCA 对 L-Glu（K 值为 9.13μM）的激活敏感。大多数被研究的化合物对 FtuCA 表现出较弱的激活作用（Ks 值为 30.5-78.3μM）。许多被研究的氨基酸和胺在脊椎动物的许多组织中浓度很高，它们在这两种细菌的致病性中的作用还不清楚。我们的研究可能会深入了解与细胞内细菌的入侵和致病作用有关的过程。
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