This paper presents the production and kinetic and inhibitory characterisation of β-carbonic anhydrase from the opportunistic bacterium Staphylococcus aureus (SauBCA). From the eight different carbonic anhydrase (CA) families known to date, humans have only the α-form, whereas many clinically relevant pathogens have β- and/or γ-form(s). Based on this discovery, β- and γ-CAs have been introduced as promising new anti-infective targets. The results of this study revealed that recombinant SauBCA possesses significant CO₂ hydration activity with a k_cat of 1.46 × 10⁵ s⁻¹ and a k_cat/K_M of 2.56 × 10⁷ s^{− 1}M⁻¹. Its enzymatic function was inhibited by various sulphonamides in the nanomolar − micromolar range, and the K_i of acetazolamide was 628 nM. The best inhibitor was the clinically used sulfamide agent famotidine (K_i of 71 nM). The least efficient inhibitors were zonisamide and dorzolamide. Our work encourages further investigations of SauBCA in an attempt to discover novel drugs against staphylococcal infections.

本文介绍了机会细菌金黄色葡萄球菌（SauBCA）的β-碳酸酐酶的产生，动力学和抑制特性。从迄今已知的八个不同的碳酸酐酶（CA）家族中，人类仅具有α-形式，而许多临床相关的病原体具有β-和/或γ-形式。基于此发现，β-和γ-CAs被引入作为有希望的新抗感染靶标。研究结果表明重组SauBCA具有显着的CO ₂水合活性，k _cat 为1.46×10 ⁵  s ^-1，k _cat / K _M 为2.56×10 ⁷  s。^{− 1} M ^-1。它的酶功能受到纳摩尔-微摩尔范围内各种磺酰胺的抑制，乙酰唑胺的K _i 为628 nM。最好抑制剂临床上使用的磺酰胺剂法莫替丁（ķ_我 的71纳米）。最无效的抑制剂是唑尼沙胺和多佐胺。我们的工作鼓励对SauBCA进行进一步研究，以期发现针对葡萄球菌感染的新药。