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

11 引文 (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

指紋

Proto-Oncogene Proteins c-pim-1
flavone
Proto-Oncogenes
Quercetin
Hinges
Hydrogen Bonding
Structure-Activity Relationship
Bioactivity
Flavonoids
Protein Kinases
Libraries
Hydrogen bonds
Phosphotransferases
hispidulin

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Pharmaceutical Science
  • Analytical Chemistry
  • Organic Chemistry
  • Molecular Medicine
  • Complementary and alternative medicine

引用此文

Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1. / Chao, Shi Wei; Su, Ming Yuan; Chiou, Lih Chu; Chen, Liang Chieh; Chang, Chung I.; Huang, Wei Jan.

於: Journal of Natural Products, 卷 78, 編號 8, 28.08.2015, p. 1969-1976.

研究成果: 雜誌貢獻文章

Chao, Shi Wei ; Su, Ming Yuan ; Chiou, Lih Chu ; Chen, Liang Chieh ; Chang, Chung I. ; Huang, Wei Jan. / Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1. 於: Journal of Natural Products. 2015 ; 卷 78, 編號 8. 頁 1969-1976.
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