The first activation study of a η-class carbonic anhydrase (CAs, EC 4.2.1.1) is reported. A panel of 24 natural and non-natural amino acids and amines was used to explore the activation profile of Plasmodium falciparum CA (PfACA). The most effective activators belonged to the amino acid chemotype, with d-Glu, l-Asp, l-/d-Phe and l-/d-DOPA possessing activation constant in the range of 82 nM–0.75 µM, whereas l-/d-His, l-Tyr, 4-amino-l-Phe and l-Gln were slightly less effective (K_A in the range of 1.00–2.51 µM. The only amine with submicromolar activating properties was 1-(2-aminoethyl-piperazine) with a K_A of 0.71 µM, whereas histamine, dopamine and serotonin showed K_A ranging between 7.18 and 9.97 µM. As CA activators have scarcely been investigated for their interaction with protozoan CAs, this study may be relevant for an improved understanding of the role of this enzyme in the life cycle of the malaria producing organisms belonging to the genus Plasmodium.

首次报道了η级碳酸酐酶（CAs，EC 4.2.1.1）的活化研究。使用一组24种天然和非天然氨基酸和胺来探索恶性疟原虫CA（PfACA）的活化特性。最有效的激活剂属于氨基酸化学型，其中d -Glu，l -Asp，l- / d -Phe和l- / d -DOPA具有82 nM–0.75 µM范围内的激活常数，而l- / d -His，升-Tyr，4-氨基升-Phe和升-Gln稍微较不有效（K_甲范围为1.00–2.51 µM。仅有的具有亚微摩尔活化特性的胺是1-（2-氨基乙基-哌嗪），其K _A为0.71 µM，而组胺，多巴胺和5-羟色胺的K _A在7.18至9.97 µM之间。由于很少研究CA激活剂与原生动物CA的相互作用，因此该研究可能与更好地了解这种酶在疟原虫属疟疾生产生物的生命周期中的作用有关。