1u6q

Substituted 2-Naphthamadine inhibitors of Urokinase

spinqualitylabelsall models 1u6q, resolution 2.02Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 1u6q 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. Method: X-ray diffraction, Resolution 2.02Å Ligands: 745 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Disease UROK_HUMAN Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:601709. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins. Function UROK_HUMAN Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin. Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors. Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.,Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. PMID:15582418 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Urokinase 3D Structures

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