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刚果锥虫鸟苷5'-单磷酸还原酶作为药物靶点的鉴定与表征

Identification and characterization of guanosine 5'-monophosphate reductase of Trypanosoma congolense as a drug target.

作者信息

Sarwono Albertus Eka Yudistira, Suganuma Keisuke, Mitsuhashi Shinya, Okada Tadashi, Musinguzi Simon Peter, Shigetomi Kengo, Inoue Noboru, Ubukata Makoto

机构信息

Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Kita-ku, Sapporo, Hokkaido 060-8589, Japan.

National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Inada, Obihiro, Hokkaido 080-8555, Japan; Research Center for Global Agromedicine, Obihiro University of Agriculture and Veterinary Medicine, Inada, Obihiro, Hokkaido 080-8555, Japan.

出版信息

Parasitol Int. 2017 Oct;66(5):537-544. doi: 10.1016/j.parint.2017.03.006. Epub 2017 Mar 31.

Abstract

Trypanosoma congolense is one of the most prevalent pathogens which causes trypanosomosis in African animals, resulting in a significant economic loss. In its life cycle, T. congolense is incapable of synthesizing purine nucleotides via a de novo pathway, and thus relies on a salvage pathway to survive. In this study, we identified a gene from T. congolense, TcIL3000_5_1940, as a guanosine 5'-monophosphate reductase (GMPR), an enzyme that modulates the concentration of intracellular guanosine in the pathogen. The recombinant protein was expressed in Escherichia coli, and the gene product was enzymatically confirmed as a unique GMPR, designated as rTcGMPR. This enzyme was constitutively expressed in glycosomes at all of the parasite's developmental stages similar to other purine nucleotide metabolic enzymes. Mycophenolic acid (MPA) was found to inhibit rTcGMPR activity. Hence, it is a potential lead compound for the design of trypanocidal agents, specifically GMPR inhibitor.

摘要

刚果锥虫是导致非洲动物锥虫病的最常见病原体之一,会造成重大经济损失。在其生命周期中,刚果锥虫无法通过从头合成途径合成嘌呤核苷酸,因此依赖补救途径生存。在本研究中,我们从刚果锥虫中鉴定出一个基因TcIL3000_5_1940,它是一种鸟苷5'-单磷酸还原酶(GMPR),该酶可调节病原体细胞内鸟苷的浓度。重组蛋白在大肠杆菌中表达,经酶学鉴定该基因产物为一种独特的GMPR,命名为rTcGMPR。与其他嘌呤核苷酸代谢酶类似,这种酶在寄生虫的所有发育阶段均在糖体中组成性表达。发现霉酚酸(MPA)可抑制rTcGMPR的活性。因此,它是设计杀锥虫剂(特别是GMPR抑制剂)的潜在先导化合物。

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