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PDB: 155 件
7VM6
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Crystal structure of uPA in complex with 6-amidino-2-naphthol
分子名称: 6-oxidanylnaphthalene-2-carboximidamide, SULFATE ION, TRIETHYLENE GLYCOL, ...
著者Jiang, L.G, Huang, M.D.
登録日2021-10-07
公開日2022-10-12
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (1.79 Å)
主引用文献Structural study of the uPA-nafamostat complex reveals a covalent inhibitory mechanism of nafamostat.
Biophys.J., 121, 2022
1GI7
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BU of 1gi7 by Molmil
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
4X1N
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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
4FUG
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BU of 4fug by Molmil
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
1F5K
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BU of 1f5k by Molmil
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
4MNV
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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
7ZRT
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BU of 7zrt by Molmil
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
1GJ9
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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
1EJN
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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
2VIO
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BU of 2vio by Molmil
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
1GI9
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BU of 1gi9 by Molmil
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
1O3P
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BU of 1o3p by Molmil
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
3IG6
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BU of 3ig6 by Molmil
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
1SQO
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BU of 1sqo by Molmil
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
4ZKS
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BU of 4zks by Molmil
The crystal structure of upain-1-W3A in complex with inactive uPA (uPA-S195A) at pH7.4
分子名称: Urokinase-type plasminogen activator, upain-1-W3A
著者Jiang, L, Andreasen, P.A, Huang, M.
登録日2015-04-30
公開日2016-05-18
実験手法X-RAY DIFFRACTION (1.85 Å)
主引用文献The crystal structure of mupain-1-IG in complex with murinised human uPA at pH7.4
To Be Published
1O5B
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BU of 1o5b by Molmil
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
1C5Z
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BU of 1c5z by Molmil
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
4MNX
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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
2O8W
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BU of 2o8w by Molmil
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
7VM7
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BU of 7vm7 by Molmil
Crystal structure of inactive uPA in complex with nafamostat
分子名称: (6-carbamimidoylnaphthalen-2-yl) 4-carbamimidamidobenzoate, Urokinase-type plasminogen activator chain B
著者Jiang, L.G, Huang, M.D.
登録日2021-10-07
公開日2022-11-23
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (1.87 Å)
主引用文献Structural study of the uPA-nafamostat complex reveals a covalent inhibitory mechanism of nafamostat.
Biophys.J., 121, 2022
3QN7
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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
6AG7
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BU of 6ag7 by Molmil
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
4X1S
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BU of 4x1s by Molmil
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
4ZHM
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BU of 4zhm by Molmil
The crystal structure of mupain-1--16-IG in complex with murinised human uPA at pH7.4
分子名称: Urokinase-type plasminogen activator, mupain-1-16-IG, piperidine-1-carboximidamide
著者Jiang, L, Andreasen, P.A, Huang, M.
登録日2015-04-25
公開日2015-09-16
最終更新日2015-10-14
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Selection of High-Affinity Peptidic Serine Protease Inhibitors with Increased Binding Entropy from a Back-Flip Library of Peptide-Protease Fusions.
J.Mol.Biol., 427, 2015
2VIN
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BU of 2vin by Molmil
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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