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Babesia bovis dihydroorotate dehydrogenase (BboDHODH) is a novel molecular target of drug for bovine babesiosis.
- Source :
-
The Journal of veterinary medical science [J Vet Med Sci] 2014 Mar; Vol. 76 (3), pp. 323-30. Date of Electronic Publication: 2013 Nov 01. - Publication Year :
- 2014
-
Abstract
- The emergence of drug resistance and adverse side effects of current bovine babesiosis treatment suggest that the search of new drug targets and development of safer and effective compounds are required. This study focuses on dihydroorotate dehydrogenase (DHODH), the fourth enzyme of pyrimidine biosynthesis pathway as a potential drug target for bovine babesiosis. Recombinant Babesia bovis DHODH protein (rBboDHODH) was produced in Escherichia coli and used for characterization and measurement of enzymatic activity. Furthermore, the effects of DHODH inhibitors were evaluated in vitro. The recombinant B. bovis DHODH histidine fusion protein (rBboDHODH) had 42.4-kDa molecular weight and exhibited a specific activity of 475.7 ± 245 Unit/mg, a Km = 276.2 µM for L-dihydroorotate and a Km= 94.41 µM for decylubiquinone. A 44-kDa band of native BboDHODH was detected by Western blot analysis and found in parasites mitochondria using a confocal microscope. Among DHODH inhibitors, atovaquone (ATV) and leflunomide (LFN) significantly inhibited the activity of rBboDHODH as well as the growth of B. bovis in vitro. The half maximal inhibitory concentration (IC50) of ATV and LFN was 2.38 ± 0.53 nM and 52.41 ± 11.47 µM, respectively. These results suggest that BboDHODH might be a novel target for development of new drug for treatment of B. bovis infection.
- Subjects :
- Amino Acid Sequence
Animals
Babesiosis metabolism
Blotting, Western
Cattle
Cloning, Molecular
Computational Biology
DNA Primers genetics
Dihydroorotate Dehydrogenase
Drug Delivery Systems
Drug Discovery
Escherichia coli
Microscopy, Confocal
Molecular Sequence Data
Oxidoreductases Acting on CH-CH Group Donors genetics
Phylogeny
Recombinant Fusion Proteins genetics
Recombinant Fusion Proteins metabolism
Babesia bovis enzymology
Babesiosis drug therapy
Cattle Diseases drug therapy
Cattle Diseases parasitology
Enzyme Inhibitors metabolism
Oxidoreductases Acting on CH-CH Group Donors metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1347-7439
- Volume :
- 76
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- The Journal of veterinary medical science
- Publication Type :
- Academic Journal
- Accession number :
- 24189582
- Full Text :
- https://doi.org/10.1292/jvms.13-0419