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  1. B300 農学部/生命農学研究科
  2. B300a 雑誌掲載論文
  3. 学術雑誌

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/2237/00028584
479d837a-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.pdf Identification_of_a_trichothecene_production_inhibitor (1.6 MB)
Item type 学術雑誌論文 / Journal Article(1)
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

WEKO 85382

en Maeda, Kazuyuki

Search repository
Nakajima, Yuichi

× Nakajima, Yuichi

WEKO 85383

en Nakajima, Yuichi

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Motoyama, Takayuki

× Motoyama, Takayuki

WEKO 85384

en Motoyama, Takayuki

Search repository
Kondoh, Yasumitsu

× Kondoh, Yasumitsu

WEKO 85385

en Kondoh, Yasumitsu

Search repository
Kawamura, Tatsuro

× Kawamura, Tatsuro

WEKO 85386

en Kawamura, Tatsuro

Search repository
Kanamaru, Kyoko

× Kanamaru, Kyoko

WEKO 85387

en Kanamaru, Kyoko

Search repository
Ohsato, Shuichi

× Ohsato, Shuichi

WEKO 85388

en Ohsato, Shuichi

Search repository
Nishiuchi, Takumi

× Nishiuchi, Takumi

WEKO 85389

en Nishiuchi, Takumi

Search repository
Yoshida, Minoru

× Yoshida, Minoru

WEKO 85390

en Yoshida, Minoru

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Osada, Hiroyuki

× Osada, Hiroyuki

WEKO 85391

en Osada, Hiroyuki

Search repository
Kobayashi, Tetsuo

× Kobayashi, Tetsuo

WEKO 85392

en Kobayashi, Tetsuo

Search repository
Kimura, Makoto

× Kimura, Makoto

WEKO 85393

en Kimura, Makoto

Search repository
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 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
内容記述タイプ Abstract
出版者
言語 en
出版者 Elsevier
言語
言語 eng
資源タイプ
資源タイプresource http://purl.org/coar/resource_type/c_6501
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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