4A6L
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![BU of 4a6l by Molmil](/molmil-images/mine/4a6l) | beta-tryptase inhibitor | 分子名称: | 1-{3-[1-({5-[(2-fluorophenyl)ethynyl]furan-2-yl}carbonyl)piperidin-4-yl]phenyl}methanamine, TRYPTASE ALPHA/BETA-1 | 著者 | Mathieu, M, Maignan, S. | 登録日 | 2011-11-04 | 公開日 | 2012-01-25 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | 主引用文献 | Structure-Based Library Design and the Discovery of a Potent and Selective Mast Cell Beta-Tryptase Inhibitor as an Oral Therapeutic Agent. Bioorg.Med.Chem.Lett., 22, 2012
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4AYY
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![BU of 4ayy by Molmil](/molmil-images/mine/4ayy) | Human thrombin - inhibitor complex | 分子名称: | (R)-1-[(S)-3-[((S)-1-Carbamimidoyl-piperidin-3-ylmethyl)-carbamoyl]-2-(naphthalene-2-sulfonylamino)-propionyl]-4-methyl-piperidine-2-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, HIRUDIN-3A', ... | 著者 | Banner, D.W, D'Arcy, A, Winkler, F.K, Hilpert, K. | 登録日 | 2012-06-22 | 公開日 | 2012-08-15 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors. J.Med.Chem., 37, 1994
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4DGJ
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2A7H
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![BU of 2a7h by Molmil](/molmil-images/mine/2a7h) | On the Routine Use of Soft X-Rays in Macromolecular Crystallography, Part III- The Optimal Data Collection Wavelength | 分子名称: | CALCIUM ION, CHLORIDE ION, Cationic trypsin | 著者 | Mueller-Dieckmann, C, Panjikar, S, Tucker, P.A, Weiss, M.S. | 登録日 | 2005-07-05 | 公開日 | 2005-07-19 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | On the routine use of soft X-rays in macromolecular crystallography. Part III. The optimal data-collection wavelength. Acta Crystallogr.,Sect.D, 61, 2005
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3TJU
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![BU of 3tju by Molmil](/molmil-images/mine/3tju) | Crystal structure of human granzyme H with an inhibitor | 分子名称: | Ac-PTSY-CMK inhibitor, Granzyme H, SULFATE ION | 著者 | Wang, L, Zhang, K, Wu, L, Tong, L, Sun, F, Fan, Z. | 登録日 | 2011-08-25 | 公開日 | 2011-12-28 | 最終更新日 | 2023-12-06 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Structural insights into the substrate specificity of human granzyme H: the functional roles of a novel RKR motif J.Immunol., 188, 2012
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3TK9
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![BU of 3tk9 by Molmil](/molmil-images/mine/3tk9) | Crystal structure of human granzyme H | 分子名称: | Granzyme H, SULFATE ION | 著者 | Wang, L, Zhang, K, Wu, L, Tong, L, Sun, F, Fan, Z. | 登録日 | 2011-08-25 | 公開日 | 2011-12-28 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | Structural insights into the substrate specificity of human granzyme H: the functional roles of a novel RKR motif J.Immunol., 188, 2012
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1YGC
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![BU of 1ygc by Molmil](/molmil-images/mine/1ygc) | Short Factor VIIa with a small molecule inhibitor | 分子名称: | (R)-4-[2-(3-AMINO-BENZENESULFONYLAMINO)-1-(3,5-DIETHOXY-2-FLUOROPHENYL)-2-OXO-ETHYLAMINO]-2-HYDROXY-BENZAMIDINE, CALCIUM ION, Coagulation factor VII, ... | 著者 | Olivero, A.G, Eigenbrot, C, Goldsmith, R, Robarge, K, Artis, D.R, Flygare, J, Rawson, T, Refino, C, Bunting, S, Kirchhofer, D. | 登録日 | 2005-01-04 | 公開日 | 2005-01-18 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo. J.Biol.Chem., 280, 2005
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2ANY
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![BU of 2any by Molmil](/molmil-images/mine/2any) | Expression, Crystallization and the Three-dimensional Structure of the Catalytic Domain of Human Plasma Kallikrein: Implications for Structure-Based Design of Protease Inhibitors | 分子名称: | BENZAMIDINE, PHOSPHATE ION, plasma kallikrein, ... | 著者 | Tang, J, Yu, C.L, Williams, S.R, Springman, E, Jeffery, D, Sprengeler, P.A, Estevez, A, Sampang, J, Shrader, W, Spencer, J.R, Young, W.B, McGrath, M.E, Katz, B.A. | 登録日 | 2005-08-11 | 公開日 | 2005-10-11 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | 主引用文献 | Expression, crystallization, and three-dimensional structure of the catalytic domain of human plasma kallikrein. J.Biol.Chem., 280, 2005
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3TJV
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![BU of 3tjv by Molmil](/molmil-images/mine/3tjv) | Crystal structure of human granzyme H with a peptidyl substrate | 分子名称: | Granzyme H, PTSYAGDDSG, SULFATE ION | 著者 | Wang, L, Zhang, K, Wu, L, Tong, L, Sun, F, Fan, Z. | 登録日 | 2011-08-25 | 公開日 | 2011-12-28 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Structural insights into the substrate specificity of human granzyme H: the functional roles of a novel RKR motif J.Immunol., 188, 2012
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2ANW
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![BU of 2anw by Molmil](/molmil-images/mine/2anw) | Expression, crystallization and three-dimensional structure of the catalytic domain of human plasma kallikrein: Implications for structure-based design of protease inhibitors | 分子名称: | BENZAMIDINE, plasma kallikrein, light chain | 著者 | Tang, J, Yu, C.L, Williams, S.R, Springman, E, Jeffery, D, Sprengeler, P.A, Estevez, A, Sampang, J, Shrader, W, Spencer, J.R, Young, W.B, McGrath, M.E, Katz, B.A. | 登録日 | 2005-08-11 | 公開日 | 2005-10-11 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | 主引用文献 | Expression, crystallization, and three-dimensional structure of the catalytic domain of human plasma kallikrein. J.Biol.Chem., 280, 2005
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1YC0
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![BU of 1yc0 by Molmil](/molmil-images/mine/1yc0) | short form HGFA with first Kunitz domain from HAI-1 | 分子名称: | Hepatocyte growth factor activator, Kunitz-type protease inhibitor 1, PHOSPHATE ION | 著者 | Shia, S, Stamos, J, Kirchhofer, D, Fan, B, Wu, J, Corpuz, R.T, Santell, L, Lazarus, R.A, Eigenbrot, C. | 登録日 | 2004-12-21 | 公開日 | 2005-02-15 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Conformational lability in serine protease active sites: structures of hepatocyte growth factor activator (HGFA) alone and with the inhibitory domain from HGFA inhibitor-1B. J.Mol.Biol., 346, 2005
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3WY8
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![BU of 3wy8 by Molmil](/molmil-images/mine/3wy8) | Crystal Structure of Protease Anisep from Arthrobacter Nicotinovorans | 分子名称: | Serine protease | 著者 | Sone, T, Haraguchi, Y, Kuwahara, A, Ose, T, Takano, M, Abe, A, Tanaka, M, Tanaka, I, Asano, K. | 登録日 | 2014-08-20 | 公開日 | 2015-08-26 | 最終更新日 | 2023-11-08 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | Structural characterization reveals the keratinolytic activity of an arthrobacter nicotinovorans protease. Protein Pept.Lett., 22, 2015
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2SGP
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![BU of 2sgp by Molmil](/molmil-images/mine/2sgp) | PRO 18 VARIANT OF TURKEY OVOMUCOID INHIBITOR THIRD DOMAIN COMPLEXED WITH STREPTOMYCES GRISEUS PROTEINASE B AT PH 6.5 | 分子名称: | OVOMUCOID INHIBITOR, PHOSPHATE ION, PROTEINASE B | 著者 | Huang, K, Lu, W, Anderson, S, Laskowski Jr, M, James, M.N.G. | 登録日 | 1999-03-25 | 公開日 | 2001-01-31 | 最終更新日 | 2023-08-30 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Contribution of peptide bonds to inhibitor-protease binding: crystal structures of the turkey ovomucoid third domain backbone variants OMTKY3-Pro18I and OMTKY3-psi[COO]-Leu18I in complex with Streptomyces griseus proteinase B (SGPB) and the structure of the free inhibitor, OMTKY-3-psi[CH2NH2+]-Asp19I J.Mol.Biol., 305, 2001
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2THF
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![BU of 2thf by Molmil](/molmil-images/mine/2thf) | STRUCTURE OF HUMAN ALPHA-THROMBIN Y225F MUTANT BOUND TO D-PHE-PRO-ARG-CHLOROMETHYLKETONE | 分子名称: | D-phenylalanyl-N-[(2S,3S)-6-{[amino(iminio)methyl]amino}-1-chloro-2-hydroxyhexan-3-yl]-L-prolinamide, SODIUM ION, THROMBIN HEAVY CHAIN, ... | 著者 | Caccia, S, Futterer, K, Di Cera, E, Waksman, G. | 登録日 | 1999-01-26 | 公開日 | 1999-03-07 | 最終更新日 | 2023-08-30 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Unexpected crucial role of residue 225 in serine proteases. Proc.Natl.Acad.Sci.USA, 96, 1999
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3NPS
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3NXP
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![BU of 3nxp by Molmil](/molmil-images/mine/3nxp) | Crystal structure of human prethrombin-1 | 分子名称: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, GLYCEROL, ... | 著者 | Chen, Z, Bush-Pelc, L.A, Di Cera, E. | 登録日 | 2010-07-14 | 公開日 | 2010-11-10 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | Crystal structure of prethrombin-1. Proc.Natl.Acad.Sci.USA, 107, 2010
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3R3G
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![BU of 3r3g by Molmil](/molmil-images/mine/3r3g) | Structure of human thrombin with residues 145-150 of murine thrombin. | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, SODIUM ION, Thrombin Heavy Chain, ... | 著者 | Pozzi, N, Chen, R, Chen, Z, Bah, A, Di Cera, E. | 登録日 | 2011-03-15 | 公開日 | 2011-05-11 | 最終更新日 | 2023-09-13 | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | 主引用文献 | Rigidification of the autolysis loop enhances Na(+) binding to thrombin. Biophys.Chem., 159, 2011
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3SO3
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![BU of 3so3 by Molmil](/molmil-images/mine/3so3) | Structures of Fab-Protease Complexes Reveal a Highly Specific Non-Canonical Mechanism of Inhibition. | 分子名称: | A11 FAB heavy chain, A11 FAB light chain, GLYCEROL, ... | 著者 | Schneider, E.L, Farady, C.J, Egea, P.F, Goetz, D.H, Baharuddin, A, Craik, C.S. | 登録日 | 2011-06-29 | 公開日 | 2012-06-20 | 最終更新日 | 2023-09-13 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | A reverse binding motif that contributes to specific protease inhibition by antibodies. J.Mol.Biol., 415, 2012
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5DAE
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1Z8G
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![BU of 1z8g by Molmil](/molmil-images/mine/1z8g) | Crystal structure of the extracellular region of the transmembrane serine protease hepsin with covalently bound preferred substrate. | 分子名称: | ACE-LYS-GLN-LEU-ARG-Chloromethylketone, Serine protease hepsin | 著者 | Herter, S, Piper, D.E, Aaron, W, Gabriele, T, Cutler, G, Cao, P, Bhatt, A.S, Choe, Y, Craik, C.S, Walker, N, Meininger, D, Hoey, T, Austin, R.J. | 登録日 | 2005-03-30 | 公開日 | 2005-05-03 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | 主引用文献 | Hepatocyte growth factor is a preferred in vitro substrate for human hepsin, a membrane-anchored serine protease implicated in prostate and ovarian cancers Biochem.J., 390, 2005
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2WUC
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![BU of 2wuc by Molmil](/molmil-images/mine/2wuc) | Crystal structure of HGFA in complex with the allosteric non- inhibitory antibody Fab40.deltaTrp and Ac-KQLR-chloromethylketone | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ACE-KQLR-CHLOROMETHYLKETONE INHIBITOR, FAB FRAGMENT FAB40.DELTATRP HEAVY CHAIN, ... | 著者 | Ganesan, R, Eigenbrot, C, Shia, S. | 登録日 | 2009-10-01 | 公開日 | 2009-12-15 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Unraveling the Allosteric Mechanism of Serine Protease Inhibition by an Antibody Structure, 17, 2009
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2WUB
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![BU of 2wub by Molmil](/molmil-images/mine/2wub) | Crystal structure of HGFA in complex with the allosteric non- inhibitory antibody Fab40.deltaTrp | 分子名称: | FAB FRAGMENT FAB40.DELTATRP HEAVY CHAIN, FAB FRAGMENT FAB40.DELTATRP LIGHT CHAIN, HEPATOCYTE GROWTH FACTOR ACTIVATOR LONG CHAIN, ... | 著者 | Ganesan, R, Eigenbrot, C, Shia, S. | 登録日 | 2009-10-01 | 公開日 | 2009-12-15 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Unraveling the Allosteric Mechanism of Serine Protease Inhibition by an Antibody Structure, 17, 2009
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2HNT
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1YBW
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![BU of 1ybw by Molmil](/molmil-images/mine/1ybw) | Protease domain of HGFA with no inhibitor | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Hepatocyte growth factor activator precursor | 著者 | Shia, S, Stamos, J, Kirchhofer, D, Fan, B, Wu, J, Corpuz, R.T, Santell, L, Lazarus, R.A, Eigenbrot, C. | 登録日 | 2004-12-21 | 公開日 | 2005-02-15 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Conformational lability in serine protease active sites: structures of hepatocyte growth factor activator (HGFA) alone and with the inhibitory domain from HGFA inhibitor-1B. J.Mol.Biol., 346, 2005
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4BTI
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![BU of 4bti by Molmil](/molmil-images/mine/4bti) | factor Xa in complex with the dual thrombin-FXa inhibitor 58. | 分子名称: | 5-Chloro-thiophene-2-carboxylic acid [(S)-2-[2-difluoromethoxy-3-(2-oxo-piperidin-1-yl)-benzenesulfonylamino]-3-((S)-3-dimethylamino-pyrrolidin-1-yl)-3-oxo-propyl]-amide, CALCIUM ION, COAGULATION FACTOR X HEAVY CHAIN, ... | 著者 | Meneyrol, J, Follmann, M, Lassalle, G, Wehner, V, Barre, G, Rousseaux, T, Altenburger, J.M, Petit, F, Bocskei, Z, Stehlin-Gaon, C, Schreuder, H, Alet, N, Herault, J.-P, Millet, L, Dol, F, Hasbrand, C, Schaeffer, P, Sadoun, F, Klieber, S, Briot, C, Bono, F, Herbert, J.-M. | 登録日 | 2013-06-18 | 公開日 | 2013-12-25 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | 主引用文献 | 5-Chlorothiophene-2-Carboxylic Acid [(S)-2-[2-Methyl-3-(2-Oxopyrrolidin-1-Yl)Benzenesulfonylamino]-3-(4-Methylpiperazin-1-Yl)-3-Oxopropyl]Amide (Sar107375), a Selective and Potent Orally Active Dual Thrombin and Factor Xa Inhibitor. J.Med.Chem., 56, 2013
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