The γ-class carbonic anhydrase (CAs, EC 4.2.1.1) from the pathogenic bacterium Vibrio cholerae, VchCAγ, was investigated for its activation with a panel of natural and non-natural amino acids and amines. The enzyme was effectively activated by l-tryptophan, 1-(2-minoethyl)-piperazine and 4-(2-aminoethyl)-morpholine, in the low nanomolar range (K_As 8–71 nM). In contrast, l-/d-Phe, l-/d-DOPA, d-Trp, l-/d-Tyr, 4-amino-l-Phe, histamine, dopamine, serotonin, some pyridyl-alkylamines, as well as l-adrenaline were submicromolar activators (K_As between 0.10 and 0.73 µM). l- and d-His were the least effective VchCAγ activators (K_As of 1.01–14.2 µM). The activation of CAs from bacteria have not been considered to date for possible biomedical applications. It would be of interest to study in more details the role of CA activators in processes connected with the virulence and colonization of the host by pathogenic bacteria, such as Vibrio cholerae, which is highly dependent on the concentration of bicarbonate in tissues.

研究了来自致病性霍乱弧菌VchCAγ的γ-类碳酸酐酶（CAs，EC 4.2.1.1）是否被一组天然和非天然氨基酸和胺激活。将酶有效地激活升色氨酸，1-（2- minoethyl） -哌嗪和4-（2-氨基乙基） -吗啉，在低纳摩尔范围内（K_甲小号8-71纳米）。与此相反，升- / d -Phe，升- / d -DOPA，d -Trp，升- / d -Tyr，4-氨基升-Phe，组胺，多巴胺，血清素，一些吡啶基-烷基胺，以及升-肾上腺素是亚微摩尔激活剂（K _A s在0.10和0.73 µM之间）。l-和d -His是最不有效的VchCAγ激活剂（K _A s为1.01-14.2 µM）。迄今为止，尚未针对可能的生物医学应用考虑从细菌激活CA。有趣的是，将更详细地研究CA活化剂在与致病菌（例如霍乱弧菌）的宿主的毒力和定殖有关的过程中的作用，而致病菌高度依赖于组织中碳酸氢盐的浓度。