Potent Inhibition of Macrophomate Synthase by Reaction Intermediate Analogs.
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- OIKAWA Hideaki
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- YAGI Kenji
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- OHASHI Satoshi
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- WATANABE Kenji
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- MIE Takashi,
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- ICHIHARA Akitami
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- HONMA Mamoru
- Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University
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- KOBAYASHI Kimiko
- Molecular Characterization Division, RIKEN (The Institute of Physical and Chemical Research)
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Abstract
Potent inhibitors for macrophomate synthase, which has recently been found to catalyze a highly unusual five-step chemical transformation, were explored. Among 11 oxalacetate analogs tested, only three analogs had moderate to relatively strong inhibitory activities (I50 1.3-8.1 mM). On the other hand, among 35 bicyclic intermediate analogs synthesized, two diacids were found to be the most potent inhibitors (I50 0.80, 0.84 mM) which had a much higher affinity than that of the natural substrate 2-pyrone. (-)-Enantiomers of the diacids showed 30 times stronger activity (I50 0.34, 0.41 mM) than (+)-ones. The I50/Km values (0.20, 0.24) showed their potent inhibitions. Competitive inhibitions were observed in two representative inhibitors.<br>
Journal
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- Bioscience, Biotechnology, and Biochemistry
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Bioscience, Biotechnology, and Biochemistry 64 (11), 2368-2379, 2000
Japan Society for Bioscience, Biotechnology, and Agrochemistry
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Details 詳細情報について
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- CRID
- 1390001206473587840
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- NII Article ID
- 110002679827
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- NII Book ID
- AA10824164
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- COI
- 1:CAS:528:DC%2BD3cXos1SrtL0%3D
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- ISSN
- 13476947
- 09168451
- http://id.crossref.org/issn/09168451
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- NDL BIB ID
- 5590212
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- PubMed
- 11193404
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed