Burkholderia pseudomallei γ-carbonic anhydrase is strongly activated by amino acids and amines

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• 作者：Daniela Vullo^a ; Sonia Del Prete^b ; ^c ; Sameh M. Osman^d ; Zeid AlOthman^d ; Clemente Capasso^c ; ^{clemente.capasso@ibbr.cnr.it} ; William A. Donald^e ; Claudiu T. Supuran^b ; ^e ; ^{claudiu.supuran@unifi.it}
• 关键词：Carbonic anhydrase ; Gamma-class enzyme ; Activator ; Amine ; Amino acid ; Burkholderia pseudomallei
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：27
• 期：1
• 页码：77-80
• 全文大小：344 K
• 卷排序：27

文摘

Activation of the γ-class carbonic anhydrase (CAs, EC 4.2.1.1) from the pathogenic bacterium Burkholderia pseudomallei (BpsγCA) with a series of natural and non-natural amino acids and aromatic/heterocyclic amines has been investigated. The best BpsγCA activators were d-His, l-DOPA, d-Trp, 4-amino-l-Phe, dopamine, 2-(2-aminoethyl)pyridine, 2-aminoethyl-piparazine/morpholine and l-adrenaline, which showed activation constants ranging between 9 and 86 nM. The least effective activators were l-His, l-Phe and 2-pyridyl-methylamine, with KAs in the range of 1.73–24.7 μM. As little is known about the role of γ-CAs in the lifecycle and virulence of this saprophytic bacterium, this study may shed some light on such phenomena. This is the first CA activation study of a γ-CA from a pathogenic bacterium, the only other such study being on the enzyme discovered in the archaeon Methanosarcina thermophila, Cam.