Isolation of a novel substrate-competitive tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis

Hideaki Kakeya, Masaya Imoto, Yuji Tabata, Junko Iwami, Haruhiko Matsumoto, Kazuo Nakamura, Takashi Koyano, Kin ichi Tadano, Kazuo Umezawa

研究成果: Article査読

32 被引用数 (Scopus)

抄録

In the course of a screening program for tyrosine kinase inhibitors, the chloroform extract of a tropical plant, Desmos chinensis, strongly inhibited the enzyme activity. The active substance was purified by silica gel, gel filtration, and finally crystallized. The structure was elucidated by mass spectrometry and X-ray crystallography to be 8-formyl-2,5,7-trihydroxy-6-methylflavanone, and we named it desmal. Desmal competed with peptide substrate and non-competed with ATP. It inhibited tyrosine kinase in situ in epidermal growth factor (EGF) receptor-overexpressing NIH3T3 (ER 12) cells. It also inhibited EGF-induced inositol phosphate formation and morphological changes.

本文言語English
ページ(範囲)169-172
ページ数4
ジャーナルFEBS Letters
320
2
DOI
出版ステータスPublished - 1993 4 5

ASJC Scopus subject areas

  • 生物理学
  • 構造生物学
  • 生化学
  • 分子生物学
  • 遺伝学
  • 細胞生物学

フィンガープリント

「Isolation of a novel substrate-competitive tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル