1SQT
 
 | | Substituted 2-Naphthamidine Inhibitors of Urokinase | | Descriptor: | 7-METHOXY-8-[1-(METHYLSULFONYL)-1H-PYRAZOL-4-YL]NAPHTHALENE-2-CARBOXIMIDAMIDE, Urokinase-type plasminogen activator | | Authors: | Wendt, M.D, Geyer, A, McClellan, W.J, Rockway, T.W, Weitzberg, M, Zhang, X, Mantei, R, Stewart, K, Nienaber, V, Klinghofer, V, Giranda, V.L. | | Deposit date: | 2004-03-19 | | Release date: | 2004-04-27 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Interaction with the S1beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Bioorg.Med.Chem.Lett., 14, 2004
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2I9A
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4FUB
 | | Crystal Structure of the Urokinase | | Descriptor: | 6-[(2S,3S)-3-phenyloxiran-2-yl]naphthalene-2-carboximidamide, ACETATE ION, GLYCEROL, ... | | Authors: | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | | Deposit date: | 2012-06-28 | | Release date: | 2012-08-22 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystal Structure of the Urokinase
to be published
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5ZA8
 | | uPA-BB2-27F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(1-methylpyrazol-4-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | Authors: | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | Deposit date: | 2018-02-06 | | Release date: | 2018-12-19 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | 6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
J. Med. Chem., 61, 2018
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5ZC5
 | | uPA-NU-09F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(4-fluoranyl-1-benzofuran-2-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | Authors: | Jiang, L.G, Buckley, B.J, Huang, M.D, Kelso, M.J, Ranson, M. | | Deposit date: | 2018-02-15 | | Release date: | 2018-12-19 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | 6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
J. Med. Chem., 61, 2018
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2FD6
 | | Structure of Human Urokinase Plasminogen Activator in Complex with Urokinase Receptor and an anti-upar antibody at 1.9 A | | Descriptor: | 1,2-ETHANEDIOL, 2-ETHOXYETHANOL, 2-acetamido-2-deoxy-alpha-D-glucopyranose, ... | | Authors: | Huang, M, Huai, Q, Li, Y. | | Deposit date: | 2005-12-13 | | Release date: | 2006-02-21 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structure of human urokinase plasminogen activator in complex with its receptor
Science, 311, 2006
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1GJB
 | | ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS | | Descriptor: | 2-(2-HYDROXY-BIPHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE, CITRIC ACID, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | | Authors: | Katz, B.A, Sprengeler, P.A, Luong, C, Verner, E, Spencer, J.R, Breitenbucher, J.G, Hui, H, McGee, D, Allen, D, Martelli, A, Mackman, R.L. | | Deposit date: | 2001-04-27 | | Release date: | 2002-04-27 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.
Chem.Biol., 8, 2001
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1W0Z
 | | Urokinase type plasminogen activator | | Descriptor: | N-(BUTYLSULFONYL)-D-SERYL-N-{4-[AMINO(IMINO)METHYL]BENZYL}-L-ALANINAMIDE, SULFATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | | Authors: | Jacob, U. | | Deposit date: | 2004-06-15 | | Release date: | 2008-05-20 | | Last modified: | 2019-09-18 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors.
J.Mol.Biol., 328, 2003
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1C5W
 | | STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR | | Descriptor: | 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE, CITRATE ANION, PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR) | | Authors: | Katz, B.A, Mackman, R, Luong, C, Radika, K, Martelli, A, Sprengeler, P.A, Wang, J, Chan, H, Wong, L. | | Deposit date: | 1999-12-22 | | Release date: | 2000-12-22 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.
Chem.Biol., 7, 2000
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4DVA
 | | The crystal structure of human urokinase-type plasminogen activator catalytic domain | | Descriptor: | HEXAETHYLENE GLYCOL, SULFATE ION, Urokinase-type plasminogen activator | | Authors: | Jiang, L, Botkjaer, K.A, Andersen, L.M, Yuan, C, Andreasen, P.A, Huang, M. | | Deposit date: | 2012-02-23 | | Release date: | 2013-01-16 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Rezymogenation of active urokinase induced by an inhibitory antibody
Biochem.J., 449, 2013
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5ZAG
 | | uPA-BB2-94F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-pyrimidin-5-yl-pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | Authors: | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | Deposit date: | 2018-02-07 | | Release date: | 2018-12-19 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | 6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
J. Med. Chem., 61, 2018
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5HGG
 | | Crystal structure of uPA in complex with a camelid-derived antibody fragment | | Descriptor: | (3S)-3-[(2S,3S,4R)-3,4-DIMETHYLTETRAHYDROFURAN-2-YL]BUTYL LAURATE, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Camelid Derived Antibody Fragment, ... | | Authors: | Yung, K.W.Y, Kromann-Hansen, T, Andreasen, P.A, Ngo, J.C.K. | | Deposit date: | 2016-01-08 | | Release date: | 2016-06-01 | | Last modified: | 2016-08-10 | | Method: | X-RAY DIFFRACTION (1.97 Å) | | Cite: | A Camelid-derived Antibody Fragment Targeting the Active Site of a Serine Protease Balances between Inhibitor and Substrate Behavior
J.Biol.Chem., 291, 2016
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7VM5
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4FUF
 | | Crystal Structure of the Urokinase | | Descriptor: | 8-(3-bromopropoxy)-7-methoxynaphthalene-2-carboximidamide, ACETATE ION, GLYCEROL, ... | | Authors: | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | | Deposit date: | 2012-06-28 | | Release date: | 2012-08-22 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal Structure of the Urokinase
to be published
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1W10
 | | Urokinase type plasminogen activator | | Descriptor: | N-(ISOBUTOXYCARBONYL)-D-SERYL-N-((1S)-4-{[AMINO(IMINO)METHYL]AMINO}-1-FORMYLBUTYL)-L-ALANINAMIDE, SULFATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | | Authors: | Jacob, U. | | Deposit date: | 2004-06-15 | | Release date: | 2008-05-20 | | Last modified: | 2019-09-18 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors.
J.Mol.Biol., 328, 2003
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1W11
 | | UROKINASE TYPE PLASMINOGEN ACTIVATOR | | Descriptor: | N-(BENZYLSULFONYL)-D-SERYL-N-{4-[AMINO(IMINO)METHYL]BENZYL}-L-ALANINAMIDE, SULFATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | | Authors: | Jacob, U. | | Deposit date: | 2004-06-15 | | Release date: | 2008-05-20 | | Last modified: | 2019-10-09 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystals of Urokinase Type Plasminogen Activator Complexes Reveal the Binding Mode of Peptidomimetic Inhibitors.
J.Mol.Biol., 328, 2003
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1W13
 | | UROKINASE TYPE PLASMINOGEN ACTIVATOR | | Descriptor: | N-(BENZYLSULFONYL)-D-SERYL-N-(4-{[AMINO(IMINO)METHYL]AMINO}BENZYL)-L-ALANINAMIDE, SULFATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | | Authors: | Jacob, U. | | Deposit date: | 2004-06-15 | | Release date: | 2008-05-20 | | Last modified: | 2019-05-22 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystals of Urokinase Type Plasminogen Activator Complexes Reveal the Binding Mode of Peptidomimetic Inhibitors.
J.Mol.Biol., 328, 2003
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4OS4
 | | Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK603 (bicyclic 1) | | Descriptor: | ACETATE ION, CHLORIDE ION, GLYCEROL, ... | | Authors: | Chen, S, Pojer, F, Heinis, C. | | Deposit date: | 2014-02-12 | | Release date: | 2014-09-24 | | Last modified: | 2021-06-02 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides.
Nat Chem, 6, 2014
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4FUI
 | | Crystal Structure of the Urokinase | | Descriptor: | 7-METHOXY-8-[1-(METHYLSULFONYL)-1H-PYRAZOL-4-YL]NAPHTHALENE-2-CARBOXIMIDAMIDE, GLYCEROL, SODIUM ION, ... | | Authors: | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | | Deposit date: | 2012-06-28 | | Release date: | 2012-08-22 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal Structure of the Urokinase
to be published
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4FUD
 | | Crystal Structure of the Urokinase | | Descriptor: | 8-aminonaphthalene-2-carboximidamide, SODIUM ION, SUCCINIC ACID, ... | | Authors: | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | | Deposit date: | 2012-06-28 | | Release date: | 2012-08-22 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal Structure of the Urokinase
to be published
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4OS7
 | | Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK607 (bicyclic) | | Descriptor: | ACETATE ION, GLYCEROL, SULFATE ION, ... | | Authors: | Chen, S, Pojer, F, Heinis, C. | | Deposit date: | 2014-02-12 | | Release date: | 2014-09-24 | | Last modified: | 2021-06-02 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides.
Nat Chem, 6, 2014
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4FU7
 | | Crystal Structure of the Urokinase | | Descriptor: | 2-[(7-carbamimidoyl-2-methoxynaphthalen-1-yl)oxy]acetamide, ACETATE ION, SULFATE ION, ... | | Authors: | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | | Deposit date: | 2012-06-28 | | Release date: | 2012-08-22 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal Structure of the Urokinase
to be published
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4FUE
 | | Crystal Structure of the Urokinase | | Descriptor: | 6-(1,2,3,4-tetrahydroisoquinolin-6-ylethynyl)naphthalene-2-carboximidamide, ACETATE ION, GLYCEROL, ... | | Authors: | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | | Deposit date: | 2012-06-28 | | Release date: | 2012-08-22 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal Structure of the Urokinase
to be published
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5YC7
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2VIQ
 | | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | | Descriptor: | 4-(2-aminoethoxy)-N-(2,5-diethoxyphenyl)-3,5-dimethylbenzamide, ACETATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR CHAIN B | | Authors: | Frederickson, M, Callaghan, O, Chessari, G, Congreve, M, Cowan, S.R, Matthews, J.E, McMenamin, R, Smith, D, Vinkovic, M, Wallis, N.G. | | Deposit date: | 2007-12-05 | | Release date: | 2008-01-22 | | Last modified: | 2017-07-05 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator.
J.Med.Chem., 51, 2008
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