Author: ["Ralph Hoessel","Sophie Leclerc","Jane A. Endicott","Martin E. M. Nobel","Alison Lawrie","Paul Tunnah","Maryse Leost","Eve Damiens","Dominique Marie","Doris Marko","Ellen Niederberger","Weici Tang","Gerhard Eisenbrand","Laurent Meijer"]
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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.Cite this article
Hoessel, R., Leclerc, S., Endicott, J. et al. Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases. Nat Cell Biol 1, 60–67 (1999). https://doi.org/10.1038/9035 