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Lookup NU author(s): Professor Jane Endicott,
Professor Martin Noble
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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.
Author(s): Hoessel R, Leclerc S, Endicott JA, Noble MEM, Lawrie A, Tunnah P, Leost M, Damiens E, Marie D, Marko D, Niederberger E, Tang WC, Eisenbrand G, Meijer L
Publication type: Article
Publication status: Published
Journal: Nature cell biology
Print publication date: 01/05/1999
ISSN (print): 1465-7392
ISSN (electronic): 1476-4679
Publisher: Nature Publishing Group
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