Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1

Shi Wei Chao, Ming Yuan Su, Lih Chu Chiou, Liang Chieh Chen, Chung I. Chang, Wei Jan Huang

研究成果: 雜誌貢獻文章同行評審

18 引文 斯高帕斯(Scopus)

摘要

(Figure Presented). A new method is applied to synthesize hispidulin, a natural flavone with a broad spectrum of biological activities. Hispidulin exhibits inhibitory activity against the oncogenic protein kinase Pim-1. Crystallographic analysis of Pim-1 bound to hispidulin reveals a binding mode distinct from that of quercetin, suggesting that the binding potency of flavonoids is determined by their hydrogen-bonding interactions with the hinge region of the kinase. Overall, this work may facilitate construction of a library of hispidulin-derived compounds for investigating the structure-activity relationship of flavone-based Pim-1 inhibitors.

原文英語
頁(從 - 到)1969-1976
頁數8
期刊Journal of Natural Products
78
發行號8
DOIs
出版狀態已發佈 - 八月 28 2015

ASJC Scopus subject areas

  • 藥物發現
  • 藥理
  • 藥學科學
  • 分析化學
  • 有機化學
  • 分子醫學
  • 補充和替代醫學

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