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Identification of a trichothecene production inhibitor by chemical array and library screening using trichodiene synthase as a target protein
http://hdl.handle.net/2237/00028584
http://hdl.handle.net/2237/00028584479d837a-f62a-4a66-a439-41b4c24e968e
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
Identification_of_a_trichothecene_production_inhibitor (1.6 MB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||
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| 公開日 | 2018-09-27 | |||||
| タイトル | ||||||
| タイトル | Identification of a trichothecene production inhibitor by chemical array and library screening using trichodiene synthase as a target protein | |||||
| 言語 | en | |||||
| 著者 |
Maeda, Kazuyuki
× Maeda, Kazuyuki× Nakajima, Yuichi× Motoyama, Takayuki× Kondoh, Yasumitsu× Kawamura, Tatsuro× Kanamaru, Kyoko× Ohsato, Shuichi× Nishiuchi, Takumi× Yoshida, Minoru× Osada, Hiroyuki× Kobayashi, Tetsuo× Kimura, Makoto |
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| アクセス権 | ||||||
| アクセス権 | open access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_abf2 | |||||
| 権利 | ||||||
| 言語 | en | |||||
| 権利情報 | © 2017. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ | |||||
| キーワード | ||||||
| 主題Scheme | Other | |||||
| 主題 | Chemical array | |||||
| キーワード | ||||||
| 主題Scheme | Other | |||||
| 主題 | Fusarium graminearum | |||||
| キーワード | ||||||
| 主題Scheme | Other | |||||
| 主題 | Gonane skeleton | |||||
| キーワード | ||||||
| 主題Scheme | Other | |||||
| 主題 | Mixed-type inhibition | |||||
| キーワード | ||||||
| 主題Scheme | Other | |||||
| 主題 | Trichodiene synthase | |||||
| キーワード | ||||||
| 主題Scheme | Other | |||||
| 主題 | Trichothecene production inhibitor | |||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Trichothecene mycotoxins often accumulate in apparently normal grains of cereal crops. In an effort to develop an agricultural chemical to reduce trichothecene contamination, we screened trichothecene production inhibitors from the compounds on the chemical arrays. By using the trichodiene (TDN) synthase tagged with hexahistidine (rTRI5) as a target protein, 32 hit compounds were obtained from chemical library of the RIKEN Natural Product Depository (NPDepo) by chemical array screening. At 10 μg mL^− 1, none of the 32 chemicals inhibited trichothecene production by Fusarium graminearum in liquid culture. Against the purified rTRI5 enzyme, however, NPD10133 [progesterone 3-(O-carboxymethyl)oxime amide-bonded to phenylalanine] showed weak inhibitory activity at 10 μg mL^− 1 (18.7 μM). For the screening of chemicals inhibiting trichothecene accumulation in liquid culture, 20 analogs of NPD10133 selected from the NPDepo chemical library were assayed. At 10 μM, only NPD352 [testosterone 3-(O-carboxymethyl)oxime amide-bonded to phenylalanine methyl ester] inhibited rTRI5 activity and trichothecene production. Kinetic analysis suggested that the enzyme inhibition was of a mixed-type. The identification of NPD352 as a TDN synthase inhibitor lays the foundation for the development of a more potent inhibitor via systematic introduction of wide structural diversity on the gonane skeleton and amino acid residues. | |||||
| 言語 | en | |||||
| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| 言語 | en | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| 出版タイプ | ||||||
| 出版タイプ | AM | |||||
| 出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
| DOI | ||||||
| 関連タイプ | isVersionOf | |||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | https://doi.org/10.1016/j.pestbp.2017.03.006 | |||||
| ISSN（print） | ||||||
| 収録物識別子タイプ | PISSN | |||||
| 収録物識別子 | 0048-3575 | |||||
| 書誌情報 |
en : Pesticide Biochemistry and Physiology 巻 138, p. 1-7, 発行日 2017-05 |
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| 著者版フラグ | ||||||
| 値 | author | |||||
