Del Prete Sonia, Vullo Daniela, Fisher Gillian M, Andrews Katherine T, Poulsen Sally-Ann, Capasso Clemente, Supuran Claudiu T
Istituto di Bioscienze e Biorisorse (IBBR)-CNR, via P. Castellino 111, 80131 Napoli, Italy.
Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy.
Bioorg Med Chem Lett. 2014 Sep 15;24(18):4389-4396. doi: 10.1016/j.bmcl.2014.08.015. Epub 2014 Aug 12.
The genome of the protozoan parasite Plasmodium falciparum, the causative agent of the most lethal type of human malaria, contains a single gene annotated as encoding a carbonic anhydrase (CAs, EC 4.2.1.1) thought to belong to the α-class, PfCA. Here we demonstrate the kinetic properties of PfCA for the CO2 hydration reaction, as well as an inhibition study of this enzyme with inorganic and complex anions and other molecules known to interact with zinc proteins, including sulfamide, sulfamic acid, and phenylboronic/arsonic acids, detecting several low micromolar inhibitors. A closer examination of the sequence of this and the CAs from other Plasmodium spp., as well as a phylogenetic analysis, revealed that these protozoa encode for a yet undisclosed, new genetic family of CAs termed the η-CA class. The main features of the η-CAs are described in this report.
恶性疟原虫是人类疟疾最致命类型的病原体,这种原生动物寄生虫的基因组包含一个单一基因,注释为编码一种碳酸酐酶(CAs,EC 4.2.1.1),被认为属于α类,即PfCA。在这里,我们展示了PfCA催化二氧化碳水合反应的动力学特性,以及用无机和复合阴离子以及其他已知与锌蛋白相互作用的分子(包括氨磺酰胺、氨基磺酸和苯基硼酸/胂酸)对该酶进行的抑制研究,检测到了几种低微摩尔浓度的抑制剂。对该碳酸酐酶以及其他疟原虫属碳酸酐酶的序列进行更仔细的研究,以及系统发育分析,揭示这些原生动物编码了一个尚未公开的新的碳酸酐酶基因家族,称为η-CA类。本报告描述了η-CA的主要特征。