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5ZA7
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UPA-HMA
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-[bis(azanyl)methylidene]-6-chloranyl-pyrazine-2-carboxamide, SULFATE ION
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
Method:X-RAY DIFFRACTION (1.7 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
5ZA8
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UPA-BB2-27F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(1-methylpyrazol-4-yl)pyrazine-2-carboxamide
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
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
5ZA9
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UPA-BB2-50F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-6-(1-benzofuran-2-yl)-Ncarbamimidoyl-pyrazine-2-carboxamide
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
Method:X-RAY DIFFRACTION (1.62 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
5ZAE
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UPA-6F-HMA
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-2-yl)pyrazine-2-carboxamide, SULFATE ION
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
Method:X-RAY DIFFRACTION (1.73 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
5ZAF
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UPA-BB2-28F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-3-yl)pyrazine-2-carboxamide
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
Method:X-RAY DIFFRACTION (1.65 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
5ZAG
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UPA-BB2-94F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-pyrimidin-5-yl-pyrazine-2-carboxamide
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
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
5ZAH
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UPA-BB2-30F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2-methoxypyrimidin-5-yl)pyrazine-2-carboxamide
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
Method:X-RAY DIFFRACTION (2.98 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
5ZAJ
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UPA-31F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide
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
Method:X-RAY DIFFRACTION (1.65 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
5ZC5
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UPA-NU-09F
Descriptor:Urokinase-type plasminogen activator chain B, 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(4-fluoranyl-1-benzofuran-2-yl)pyrazine-2-carboxamide
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
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
6AG7
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THE CRYSTAL STRUCTURE OF UPA IN COMPLEX WITH HMA-55F
Descriptor:Urokinase-type plasminogen activator, 3,5-diamino-N-carbamimidoyl-6-(1-methyl-1H-pyrazol-4-yl)pyrazine-2-carboxamide
Authors:Buckley, B., Jiang, L.G., Majed, H., Huang, M.D., Kelso, M., Ranson, M.
Deposit date:2018-08-09
Release date:2019-08-14
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:uPA-HMA
To Be Published
1JRR
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HUMAN PLASMINOGEN ACTIVATOR INHIBITOR-2.[LOOP (66-98) DELETIONMUTANT] COMPLEXED WITH PEPTIDE MIMICKING THE REACTIVE CENTER LOOP
Descriptor:PLASMINOGEN ACTIVATOR INHIBITOR-2, BETA-MERCAPTOETHANOL
Authors:Jankova, L., Harrop, S.J., Saunders, D.N., Andrews, J.L., Bertram, K.C., Gould, A.R., Baker, M.S., Curmi, P.M.G.
Deposit date:2001-08-15
Release date:2001-09-26
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.6 Å)
Cite:CRYSTAL STRUCTURE OF THE COMPLEX OF PLASMINOGEN ACTIVATOR INHIBITOR 2 WITH A PEPTIDE MIMICKING THE REACTIVE CENTER LOOP
J.Biol.Chem., 276, 2001