Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Polo Scientifico, Università degli Studi di Firenze, Sesto Fiorentino, Firenz, Italy.
J Enzyme Inhib Med Chem. 2011 Oct;26(5):749-53. doi: 10.3109/14756366.2011.570759. Epub 2011 Apr 11.
A carbonic anhydrase (CA, EC 4.2.1.1) from red blood cells of pigeons (Columba livia var. domestica), clCA, was purified to homogeneity. Its kinetic parameters for the CO(2) hydration reaction were measured. With a k(cat)/K(m) of 1.1 × 10(8) M(-1) s(-1), and a k(cat) of 1.3 × 10(6) s(-1), clCA has a high activity, similar to that of the human isoform hCA II. A group of 25 aromatic/heterocyclic sulfonamides incorporating the sulfanilamide, homosulfanilamide, benzene-1,3-disulfonamide, and acetazolamide scaffolds showed variable inhibitory activity against the pigeon enzyme, with K(I)s in the range of 1.9-3460 nM. Red blood cells of pigeons, like those of ostriches, contain thus just one CA isoform, unlike the blood of mammals, which normally contain two isoforms, one of low (CA I-like) and one of very high activity (CA II-like). However, from the sulfonamide inhibition viewpoint, the pigeon enzyme was more similar to hCA II than to the ostrich enzyme.
一种来自鸽子(Columba livia var. domestica)红细胞的碳酸酐酶(CA,EC 4.2.1.1),clCA,被纯化至均质。其 CO(2)水合反应的动力学参数被测量。clCA 的 k(cat)/K(m)为 1.1 × 10(8) M(-1) s(-1),k(cat)为 1.3 × 10(6) s(-1),具有高活性,类似于人类同工酶 hCA II。一组 25 种包含磺胺、磺胺甲噁唑、苯-1,3-二磺酰胺和乙酰唑胺结构的芳族/杂环磺酰胺对鸽子酶表现出可变的抑制活性,K(I)范围为 1.9-3460 nM。像鸵鸟一样,鸽子的红细胞只含有一种 CA 同工酶,与哺乳动物的血液不同,哺乳动物的血液通常含有两种同工酶,一种活性低(类似 CA I),一种活性非常高(类似 CA II)。然而,从磺酰胺抑制的角度来看,鸽子酶与 hCA II 比与鸵鸟酶更相似。