Fungal metabolite, epoxyquinol B, crosslinks proteins by epoxy-thiol conjugation

Hiroshi Kamiyama, Takeo Usui, Masakazu Uramoto, Hiroshi Takagi, Mitsuru Shoji, Yujiro Hayashi, Hideaki Kakeya, Hiroyuki Osada

研究成果: Article査読

11 被引用数 (Scopus)

抄録

Epoxyquinol B (EPQB) is a fungal metabolite, containing two α,/β-epoxy ketones. We previously showed that EPQB inhibited the signal transduction involved in angiogenesis through the binding to cysteine residues of receptor kinases. However, the inhibitory mechanism was undefined. In this report, we found that one EPQB molecule is covalently bound to two X-cysteine molecules through two epoxide residues on EPQB. Furthermore, EPQB crosslinked binding proteins through the cysteine residues. These results suggest that EPQB inhibits receptor kinases by crosslinking with other protein or by intramolecular crosslinking.

本文言語English
ページ(範囲)94-97
ページ数4
ジャーナルJournal of Antibiotics
61
2
DOI
出版ステータスPublished - 2008 2

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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