6FJT
 
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6BX8
 | | Human Mesotrypsin (PRSS3) Complexed with Tissue Factor Pathway Inhibitor Variant (TFPI1-KD1-K15R-I17C-I34C) | | 分子名称: | SULFATE ION, Tissue factor pathway inhibitor, Trypsin-3 | | 著者 | Coban, M, Sankaran, B, Cohen, I, Hockla, A, Papo, N, Radisky, E.S. | | 登録日 | 2017-12-18 | | 公開日 | 2019-02-06 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.98 Å) | | 主引用文献 | Disulfide engineering of human Kunitz-type serine protease inhibitors enhances proteolytic stability and target affinity toward mesotrypsin.
J. Biol. Chem., 294, 2019
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6DWU
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6DWH
 | | Crystal structure of complex of BBKI and Bovine Trypsin | | 分子名称: | CHLORIDE ION, Cationic trypsin, Kunitz-type inihibitor, ... | | 著者 | Li, M, Wlodawer, A. | | 登録日 | 2018-06-26 | | 公開日 | 2019-01-30 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Crystal structures of the complex of a kallikrein inhibitor from Bauhinia bauhinioides with trypsin and modeling of kallikrein complexes.
Acta Crystallogr D Struct Biol, 75, 2019
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6DWF
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6D3Z
 | | Protease SFTI complex | | 分子名称: | Plasminogen, Trypsin inhibitor 1 | | 著者 | Law, R.H.P, Wu, G. | | 登録日 | 2018-04-17 | | 公開日 | 2019-01-23 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.
J. Med. Chem., 62, 2019
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6DI8
 | | Crystal structure of bovine alpha-chymotrypsin in space group P65 | | 分子名称: | Chymotrypsin A chain A, Chymotrypsin A chain B, Chymotrypsin A chain C, ... | | 著者 | Marshall, A.C, Keiller, B.G, Bruning, J.B. | | 登録日 | 2018-05-23 | | 公開日 | 2019-01-23 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (1.859 Å) | | 主引用文献 | Crystal Structure of Bovine Alpha-Chymotrypsin in Space Group P65
Crystals, 8, 2018
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6D40
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6D3Y
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6D3X
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6AHS
 | | Mouse Kallikrein 7 in complex with imidazolinylindole derivative | | 分子名称: | 1-[(2-chlorophenyl)sulfonyl]-5-methyl-3-[(4R)-2-methyl-4,5-dihydro-1H-imidazol-4-yl]-1H-indole, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, CHLORIDE ION, ... | | 著者 | Sugawara, H. | | 登録日 | 2018-08-20 | | 公開日 | 2019-01-02 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Discovery and structure-activity relationship of imidazolinylindole derivatives as kallikrein 7 inhibitors.
Bioorg. Med. Chem. Lett., 29, 2019
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5Z1C
 | | The crystal structure of uPA in complex with 4-Iodobenzylamine at pH7.4 | | 分子名称: | 1-(4-iodophenyl)methanamine, Urokinase-type plasminogen activator | | 著者 | Jiang, L.G, Zhang, X, Luo, Z.P, Huang, M.D. | | 登録日 | 2017-12-25 | | 公開日 | 2018-12-26 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.45 Å) | | 主引用文献 | Halogen bonding for the design of inhibitors by targeting the S1 pocket of serine proteases
Rsc Adv, 49, 2018
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5ZAJ
 | | uPA-31F | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-07 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | 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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5ZAG
 | | uPA-BB2-94F | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-pyrimidin-5-yl-pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-07 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | 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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5ZA8
 | | uPA-BB2-27F | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(1-methylpyrazol-4-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-06 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | 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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5ZAF
 | | uPA-BB2-28F | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-3-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-07 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | 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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5ZA7
 | | uPA-HMA | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-[bis(azanyl)methylidene]-6-chloranyl-pyrazine-2-carboxamide, SULFATE ION, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-06 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | 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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5ZAE
 | | uPA-6F-HMA | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-2-yl)pyrazine-2-carboxamide, SULFATE ION, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-07 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.73 Å) | | 主引用文献 | 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 | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(4-fluoranyl-1-benzofuran-2-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Jiang, L.G, Buckley, B.J, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-15 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | 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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5ZAH
 | | uPA-BB2-30F | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2-methoxypyrimidin-5-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-07 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.98 Å) | | 主引用文献 | 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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5ZA9
 | | uPA-BB2-50F | | 分子名称: | 3-azanyl-5-(azepan-1-yl)-6-(1-benzofuran-2-yl)-Ncarbamimidoyl-pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 著者 | Buckley, B.J, Jiang, L.G, Huang, M.D, Kelso, M.J, Ranson, M. | | 登録日 | 2018-02-07 | | 公開日 | 2018-12-19 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.62 Å) | | 主引用文献 | 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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6BVH
 | | Trypsin complexed with a modified sunflower trypsin inhibitor, SFTI-TCTR(N12,N14) | | 分子名称: | CALCIUM ION, Cationic trypsin, GLYCEROL, ... | | 著者 | Riley, B.T, Chen, X. | | 登録日 | 2017-12-13 | | 公開日 | 2018-12-19 | | 最終更新日 | 2019-01-30 | | 実験手法 | X-RAY DIFFRACTION (1.927 Å) | | 主引用文献 | Potent, multi-target serine protease inhibition achieved by a simplified beta-sheet motif.
PLoS ONE, 14, 2019
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6BQM
 | | Secreted serine protease VesC from Vibrio cholerae | | 分子名称: | serine protease VesC | | 著者 | Park, Y.J, Korotkov, K.V, Delarosa, J.R, Turley, S, DiMaio, F, Hol, W.G.J. | | 登録日 | 2017-11-28 | | 公開日 | 2018-11-28 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Suppressor Mutations in Type II Secretion Mutants of Vibrio cholerae: Inactivation of the VesC Protease.
Msphere, 5, 2020
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6BFP
 | | Bovine trypsin bound to potent inhibitor | | 分子名称: | 3-{2-[(4-carbamimidoylphenyl)carbamoyl]-4-ethenyl-5-methoxyphenyl}-6-[(cyclopropylmethyl)carbamoyl]pyridine-2-carboxylic acid, CALCIUM ION, Cationic trypsin | | 著者 | Partridge, J.R, Choy, R.M. | | 登録日 | 2017-10-26 | | 公開日 | 2018-10-31 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.292 Å) | | 主引用文献 | Structures of full-length plasma kallikrein bound to highly specific inhibitors describe a new mode of targeted inhibition.
J.Struct.Biol., 206, 2019
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6EVV
 | | X-ray structure of the complex between human alpha thrombin and NU172, a duplex/quadruplex 26-mer DNA aptamer, in the presence of potassium ions. | | 分子名称: | D-phenylalanyl-N-[(2S,3S)-6-{[amino(iminio)methyl]amino}-1-chloro-2-hydroxyhexan-3-yl]-L-prolinamide, GLYCEROL, N-acetyl-alpha-neuraminic acid-(2-6)-beta-D-galactopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-6)-[alpha-D-mannopyranose-(1-3)]beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Troisi, R, Russo Krauss, I, Sica, F. | | 登録日 | 2017-11-02 | | 公開日 | 2018-10-24 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Several structural motifs cooperate in determining the highly effective anti-thrombin activity of NU172 aptamer.
Nucleic Acids Res., 46, 2018
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