Naturally occurring FANCF-Hes1 complex inhibitors from Wrightia religiosa

Midori A. Arai, Kenji Uemura, Nozomi Hamahiga, Naoki Ishikawa, Takashi Koyano, Thaworn Kowithayakorn, Tagrid Kaddar, Madeleine Carreau, Masami Ishibashi

研究成果: Article

5 引用 (Scopus)

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The isolation and evaluation of inhibitors of Fanconi F protein (FANCF)-hairy and enhancer of split 1 (Hes1) complex are described. A high-throughput screening assay for small-molecule inhibitors of the FANCF-Hes1 complex was realized. Successful complex formation between fluorophore (Cy3)-labeled human FANCF and immobilized rat or human HES1 on a microplate was established. Screening of our plant extract library using this system resulted in the isolation of eight natural products, including two new flavonoid glycosides (3 and 4), from Wrightia religiosa. Of these compounds, 3, 5, and 7 showed potent inhibition of the FANCF-Hes1 complex formation. Compound 7 disrupted the FANCF-Hes1 complex more efficiently than the Hes1 dimer. This journal is

元の言語English
ページ(範囲)455-460
ページ数6
ジャーナルMedChemComm
6
発行部数3
DOI
出版物ステータスPublished - 2015 3 1

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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    Arai, M. A., Uemura, K., Hamahiga, N., Ishikawa, N., Koyano, T., Kowithayakorn, T., Kaddar, T., Carreau, M., & Ishibashi, M. (2015). Naturally occurring FANCF-Hes1 complex inhibitors from Wrightia religiosa. MedChemComm, 6(3), 455-460. https://doi.org/10.1039/c4md00495g