7VM6
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1GI7
| A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE | 分子名称: | 2-(2-OXO-1,2-DIHYDRO-PYRIDIN-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE, CITRIC ACID, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | 著者 | Katz, B.A, Elrod, K, Luong, C, Rice, M, Mackman, R.L, Sprengeler, P.A, Spencer, J, Hatayte, J, Janc, J, Link, J, Litvak, J, Rai, R, Rice, K, Sideris, S, Verner, E, Young, W. | 登録日 | 2001-01-22 | 公開日 | 2002-01-22 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | 主引用文献 | A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site. J.Mol.Biol., 307, 2001
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4X1N
| The crystal structure of mupain-1-16 in complex with murinised human uPA at pH7.4 | 分子名称: | Urokinase-type plasminogen activator, mupain-1-16, piperidine-1-carboximidamide | 著者 | Jiang, L, Zhao, B, Xu, P, Andreasen, P, Huang, M. | 登録日 | 2014-11-25 | 公開日 | 2015-03-25 | 最終更新日 | 2023-11-08 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | A cyclic peptidic serine protease inhibitor: increasing affinity by increasing peptide flexibility. Plos One, 9, 2014
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4FUG
| Crystal Structure of the Urokinase | 分子名称: | ACETATE ION, GLYCEROL, SULFATE ION, ... | 著者 | Kang, Y.N, Stuckey, J.A, Nienaber, V, Giranda, V. | 登録日 | 2012-06-28 | 公開日 | 2012-08-22 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Crystal Structure of the Urokinase to be published
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1F5K
| UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX | 分子名称: | BENZAMIDINE, SULFATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | 著者 | Zeslawska, E, Schweinitz, A, Karcher, A, Sondermann, P, Sperl, S, Sturzebecher, J, Jacob, U. | 登録日 | 2000-06-15 | 公開日 | 2001-06-15 | 最終更新日 | 2021-11-03 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design. J.Mol.Biol., 301, 2000
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4MNV
| Crystal structure of bicyclic peptide UK729 bound as an acyl-enzyme intermediate to urokinase-type plasminogen activator (uPA) | 分子名称: | 1,3,5-tris(bromomethyl)benzene, ACETATE ION, GLYCEROL, ... | 著者 | Chen, S, Pojer, F, Heinis, C. | 登録日 | 2013-09-11 | 公開日 | 2014-02-05 | 最終更新日 | 2017-11-15 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Peptide ligands stabilized by small molecules. Angew.Chem.Int.Ed.Engl., 53, 2014
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7ZRT
| Crystal structure of human Urokinase-type plasminogen activator in complex with bicycle peptide inhibitor UK970 | 分子名称: | 1,2-ETHANEDIOL, 1,3,5-tris(bromomethyl)benzene, DI(HYDROXYETHYL)ETHER, ... | 著者 | Caregnato, A, Angela, P, Mazzoccato, Y, Frasson, N, Angelini, A, Cendron, L. | 登録日 | 2022-05-05 | 公開日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Crystal structure of human Urokinase-type plasminogen activator in complex with bicycle peptide inhibitor UK970 To Be Published
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1GJ9
| ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS | 分子名称: | 6-FLUORO-2-[2-HYDROXY-3-(2-METHYL-CYCLOHEXYLOXY)-PHENYL]-1H-INDOLE-5-CARBOXAMIDINE, CITRIC ACID, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | 著者 | 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. | 登録日 | 2001-04-30 | 公開日 | 2002-04-27 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets. Chem.Biol., 8, 2001
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1EJN
| UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN INHIBITOR COMPLEX | 分子名称: | N-(1-ADAMANTYL)-N'-(4-GUANIDINOBENZYL)UREA, SULFATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | 著者 | Sperl, S, Jacob, U, Arroyo de Prada, N, Stuerzebecher, J, Wilhelm, O.G, Bode, W, Magdolen, V, Huber, R, Moroder, L. | 登録日 | 2000-04-22 | 公開日 | 2000-05-17 | 最終更新日 | 2021-11-03 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | (4-aminomethyl)phenylguanidine derivatives as nonpeptidic highly selective inhibitors of human urokinase. Proc.Natl.Acad.Sci.USA, 97, 2000
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2VIO
| Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | 分子名称: | 4-(2-aminoethoxy)-3,5-dichlorobenzoic acid, ACETATE ION, UROKINASE-TYPE PLASMINOGEN ACTIVATOR CHAIN B | 著者 | Frederickson, M, Callaghan, O, Chessari, G, Congreve, M, Cowan, S.R, Matthews, J.E, McMenamin, R, Smith, D, Vinkovic, M, Wallis, N.G. | 登録日 | 2007-12-05 | 公開日 | 2008-01-22 | 最終更新日 | 2017-07-05 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator J.Med.Chem., 51, 2008
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1GI9
| A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE | 分子名称: | 2-(2-HYDROXY-5-METHOXY-PHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE, CITRIC ACID, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | 著者 | Katz, B.A, Elrod, K, Luong, C, Rice, M, Mackman, R.L, Sprengeler, P.A, Spencer, J, Hatayte, J, Janc, J, Link, J, Litvak, J, Rai, R, Rice, K, Sideris, S, Verner, E, Young, W. | 登録日 | 2001-01-22 | 公開日 | 2002-01-22 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site. J.Mol.Biol., 307, 2001
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1O3P
| Elaborate Manifold of Short Hydrogen Bond Arrays Mediating Binding of Active Site-Directed Serine Protease Inhibitors | 分子名称: | 2-{5-[AMINO(IMINIO)METHYL]-1H-BENZIMIDAZOL-2-YL}-6-(CYCLOPENTYLOXY)BENZENOLATE, CITRIC ACID, Urokinase-type plasminogen activator | 著者 | Katz, B.A, Elrod, K, Verner, E, Mackman, R.L, Luong, C, Shrader, W.D, Sendzik, M, Spencer, J.R, Sprengeler, P.A, Kolesnikov, A, Tai, V.W, Hui, H.C, Breitenbucher, J.G, Allen, D, Janc, J.W. | 登録日 | 2003-03-06 | 公開日 | 2003-09-02 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.81 Å) | 主引用文献 | Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease
inhibitors. J.Mol.Biol., 329, 2003
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3IG6
| Low molecular weigth human Urokinase type Plasminogen activator 2-[6-(3'-Aminomethyl-biphenyl-3-yloxy)-4-(3-dimethylamino-pyrrolidin-1-yl)-3,5-difluoro-pyridin-2-yloxy]-4-dimethylamino-benzoic acid complex | 分子名称: | 2-[(6-{[3'-(aminomethyl)biphenyl-3-yl]oxy}-4-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-3,5-difluoropyridin-2-yl)oxy]-4-(dimethylamino)benzoic acid, PHOSPHATE ION, Urokinase-type plasminogen activator | 著者 | Adler, M, Whitlow, M. | 登録日 | 2009-07-27 | 公開日 | 2009-10-13 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | 主引用文献 | Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA) Bioorg.Med.Chem.Lett., 19, 2009
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1SQO
| Substituted 2-Naphthamidine Inhibitors of Urokinase | 分子名称: | 8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE, SULFATE ION, Urokinase-type plasminogen activator | 著者 | Wendt, M.D, Geyer, A, McClellan, W.J, Rockway, T.W, Weitzberg, M, Zhao, X, Mantei, R, Stewart, K, Nienaber, V, Klinghofer, V, Giranda, V.L. | 登録日 | 2004-03-19 | 公開日 | 2004-04-27 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (1.84 Å) | 主引用文献 | 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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4ZKS
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1O5B
| Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | 分子名称: | 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE, CITRIC ACID, Urokinase-type plasminogen activator | 著者 | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | 登録日 | 2003-09-09 | 公開日 | 2004-09-21 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | 主引用文献 | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA) J.Mol.Biol., 344, 2004
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1C5Z
| STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR | 分子名称: | BENZAMIDINE, CITRATE ANION, PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR) | 著者 | Katz, B.A, Mackman, R, Luong, C, Radika, K, Martelli, A, Sprengeler, P.A, Wang, J, Chan, H, Wong, L. | 登録日 | 1999-12-22 | 公開日 | 2000-12-22 | 最終更新日 | 2024-04-03 | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | 主引用文献 | 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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4MNX
| Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK811 | 分子名称: | 1,1',1''-(1,3,5-triazinane-1,3,5-triyl)tripropan-1-one, GLYCEROL, SULFATE ION, ... | 著者 | Chen, S, Pojer, F, Heinis, C. | 登録日 | 2013-09-11 | 公開日 | 2014-02-05 | 最終更新日 | 2017-11-15 | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | 主引用文献 | Peptide ligands stabilized by small molecules. Angew.Chem.Int.Ed.Engl., 53, 2014
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2O8W
| Crystal Structure and Binding Epitopes of Urokinase-type Plasminogen Activator (C122A/N145Q/S195A) in complex with Inhibitors | 分子名称: | 1-phenylguanidine, SULFATE ION, TETRAETHYLENE GLYCOL, ... | 著者 | Zhao, G, Yuan, C, Jiang, L, Huang, Z, Huang, M. | 登録日 | 2006-12-12 | 公開日 | 2007-12-25 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.86 Å) | 主引用文献 | Crystal Structure and Binding Epitopes of Urokinase-type Plasminogen Activator (C122A/N145Q/S195A) in complex with Inhibitors To be Published
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7VM7
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3QN7
| Potent and selective bicyclic peptide inhibitor (UK18) of human urokinase-type plasminogen activator(uPA) | 分子名称: | 1,3,5-tris(bromomethyl)benzene, Bicyclic peptide inhibitor, Urokinase-type plasminogen activator | 著者 | Angelini, A, Cendron, L, Touati, J, Winter, G, Zanotti, G, Heinis, C. | 登録日 | 2011-02-08 | 公開日 | 2012-02-15 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Bicyclic peptide inhibitor reveals large contact interface with a protease target Acs Chem.Biol., 7, 2012
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6AG7
| The crystal structure of uPA in complex with HMA-55F | 分子名称: | 3,5-diamino-N-carbamimidoyl-6-(1-methyl-1H-pyrazol-4-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator | 著者 | Buckley, B, Jiang, L.G, Majed, H, Huang, M.D, Kelso, M, Ranson, M. | 登録日 | 2018-08-09 | 公開日 | 2019-08-14 | 最終更新日 | 2023-11-22 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | uPA-HMA To Be Published
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4X1S
| The crystal structure of mupain-1-16-D9A in complex with murinised human uPA at pH7.4 | 分子名称: | Urokinase-type plasminogen activator, mupain-1-16, piperidine-1-carboximidamide | 著者 | Jiang, L, Zhao, B, Xu, P, Andreasen, P, Huang, M. | 登録日 | 2014-11-25 | 公開日 | 2015-10-28 | 最終更新日 | 2023-11-08 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | A cyclic peptidic serine protease inhibitor: increasing affinity by increasing peptide flexibility. Plos One, 9, 2014
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4ZHM
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2VIN
| Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator | 分子名称: | (2R)-1-(2,6-dimethylphenoxy)propan-2-amine, ACETATE ION, SULFATE ION, ... | 著者 | Frederickson, M, Callaghan, O, Chessari, G, Congreve, M, Cowan, S.R, Matthews, J.E, McMenamin, R, Smith, D, Vinkovic, M, Wallis, N.G. | 登録日 | 2007-12-05 | 公開日 | 2008-01-22 | 最終更新日 | 2017-07-05 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator J.Med.Chem., 51, 2008
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