3qbn | pdb_00003qbn

Structure of Human Aurora A in Complex with a diaminopyrimidine

spinqualitylabelsall models 3qbn, resolution 3.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3qbn is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: E9Z Gene: AURKA, AIK, ARK1, AURA, BTAK, STK15, STK6 (Homo sapiens) Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Infestation of crops by pathogenic fungi has continued to have a major impact by reducing yield and quality, emphasizing the need to identify new targets and develop new agents to improve methods of crop protection. Here we present Aurora kinase from the phytopathogenic fungus Ustilago maydis as a novel target for N-substituted diaminopyrimidines, a class of small-molecule kinase inhibitors. We show that Aurora kinase is essential in U. maydis and that diaminopyrimidines inhibit its activity in vitro. Furthermore, we observed an overall good correlation between in vitro inhibition of Aurora kinase and growth inhibition of diverse fungi in vivo. In vitro inhibition assays with Ustilago and human Aurora kinases indicate that some compounds of the N-substituted diaminopyrimidine class show specificity for the Ustilago enzyme, thus revealing their potential as selective fungicides. Identification of Ustilago maydis Aurora kinase as a novel antifungal target.,Tuckmantel S, Greul JN, Janning P, Brockmeyer A, Grutter C, Simard JR, Gutbrod O, Beck ME, Tietjen K, Rauh D, Schreier PH ACS Chem Biol. 2011 Sep 16;6(9):926-33. Epub 2011 Jun 20. PMID:21671622 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Serine/threonine protein kinase

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