1. Academic Validation
  2. Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases

Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases

  • Nat Cell Biol. 1999 May;1(1):60-7. doi: 10.1038/9035.
R Hoessel 1 S Leclerc J A Endicott M E Nobel A Lawrie P Tunnah M Leost E Damiens D Marie D Marko E Niederberger W Tang G Eisenbrand L Meijer
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Kaiserslautern, Germany.
PMID: 10559866 DOI: 10.1038/9035
Abstract

Indirubin is the active ingredient of Danggui Longhui Wan, a mixture of Plants that is used in traditional Chinese medicine to treat chronic diseases. Here we identify indirubin and its analogues as potent inhibitors of cyclin-dependent kinases (CDKs). The crystal structure of CDK2 in complex with indirubin derivatives shows that indirubin interacts with the kinase's ATP-binding site through van der Waals interactions and three hydrogen bonds. Indirubin-3'-monoxime inhibits the proliferation of a large range of cells, mainly through arresting the cells in the G2/M phase of the cell cycle. These results have implications for therapeutic optimization of indigoids.

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