6X6C
 
 | | Cryo-EM structure of NLRP1-DPP9-VbP complex | | Descriptor: | Dipeptidyl peptidase 9, NACHT, LRR and PYD domains-containing protein 1, ... | | Authors: | Hollingsworth, L.R, Sharif, H, Griswold, A.R, Fontana, P, Mintseris, J, Dagbay, K.B, Paulo, J.A, Gygi, S.P, Bachovchin, D.A, Wu, H. | | Deposit date: | 2020-05-27 | | Release date: | 2021-03-10 | | Last modified: | 2021-05-12 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | DPP9 sequesters the C terminus of NLRP1 to repress inflammasome activation.
Nature, 592, 2021
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6X6A
 | | Cryo-EM structure of NLRP1-DPP9 complex | | Descriptor: | Dipeptidyl peptidase 9, NACHT, LRR and PYD domains-containing protein 1 | | Authors: | Hollingsworth, L.R, Sharif, H, Griswold, A.R, Fontana, P, Mintseris, J, Dagbay, K.B, Paulo, J.A, Gygi, S.P, Bachovchin, D.A, Wu, H. | | Deposit date: | 2020-05-27 | | Release date: | 2021-03-10 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | DPP9 sequesters the C terminus of NLRP1 to repress inflammasome activation.
Nature, 592, 2021
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5MTF
 | | A modular route to novel potent and selective inhibitors of rhomboid intramembrane proteases | | Descriptor: | CHLORIDE ION, Rhomboid protease GlpG, inhibitor, ... | | Authors: | Ticha, A, Stanchev, S, Vinothkumar, K.R, Mikles, D.C, Pachl, P, Svehlova, K, Nguyen, M.T.N, Verhelst, S.H.L, Johnson, D, Bachovchin, D, Lepsik, M, Majer, P, Strisovsky, K. | | Deposit date: | 2017-01-09 | | Release date: | 2017-11-15 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.79 Å) | | Cite: | General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases.
Cell Chem Biol, 24, 2017
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7MDC
 | | Full-length wildtype ClbP inhibited by hexanoyl-D-asparagine boronic acid | | Descriptor: | (2S)-2,3-dihydroxypropyl (9Z)-hexadec-9-enoate, Beta-lactamase, CHLORIDE ION, ... | | Authors: | Velilla, J.A, Volpe, M.R, Gaudet, R. | | Deposit date: | 2021-04-03 | | Release date: | 2022-09-28 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | A small molecule inhibitor prevents gut bacterial genotoxin production.
Nat.Chem.Biol., 19, 2023
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6XKK
 | | Cryo-EM structure of the NLRP1-CARD filament | | Descriptor: | NACHT, LRR and PYD domains-containing protein 1 | | Authors: | Hollingsworth, L.R, David, L, Li, Y, Sharif, H, Fontana, P, Fu, T, Wu, H. | | Deposit date: | 2020-06-26 | | Release date: | 2020-11-25 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.72 Å) | | Cite: | Mechanism of filament formation in UPA-promoted CARD8 and NLRP1 inflammasomes.
Nat Commun, 12, 2021
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6XKJ
 | | Cryo-EM structure of CARD8-CARD filament | | Descriptor: | Caspase recruitment domain-containing protein 8 | | Authors: | Hollingsworth, L.R, David, L, Li, Y, Sharif, H, Fontana, P, Fu, T, Wu, H. | | Deposit date: | 2020-06-26 | | Release date: | 2020-11-25 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.54 Å) | | Cite: | Mechanism of filament formation in UPA-promoted CARD8 and NLRP1 inflammasomes.
Nat Commun, 12, 2021
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5MT7
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5MT6
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5MT8
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5ZAJ
 | | uPA-31F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZAG
 | | uPA-BB2-94F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-pyrimidin-5-yl-pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZA8
 | | uPA-BB2-27F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(1-methylpyrazol-4-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZAF
 | | uPA-BB2-28F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-3-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZA7
 | | uPA-HMA | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-[bis(azanyl)methylidene]-6-chloranyl-pyrazine-2-carboxamide, SULFATE ION, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZAE
 | | uPA-6F-HMA | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-2-yl)pyrazine-2-carboxamide, SULFATE ION, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZC5
 | | uPA-NU-09F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(4-fluoranyl-1-benzofuran-2-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZAH
 | | uPA-BB2-30F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2-methoxypyrimidin-5-yl)pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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5ZA9
 | | uPA-BB2-50F | | Descriptor: | 3-azanyl-5-(azepan-1-yl)-6-(1-benzofuran-2-yl)-Ncarbamimidoyl-pyrazine-2-carboxamide, Urokinase-type plasminogen activator chain B | | 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 | | Last modified: | 2023-11-22 | | 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
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7JN7
 | | Human DPP9-CARD8 complex | | Descriptor: | Caspase recruitment domain-containing protein 8, Dipeptidyl peptidase 9, [(2~{R})-1-[(2~{R})-2-azanyl-3-methyl-butanoyl]pyrrolidin-2-yl]boronic acid | | Authors: | Sharif, H, Hollingsworth, L.R. | | Deposit date: | 2020-08-04 | | Release date: | 2021-05-19 | | Last modified: | 2021-07-28 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Dipeptidyl peptidase 9 sets a threshold for CARD8 inflammasome formation by sequestering its active C-terminal fragment.
Immunity, 54, 2021
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7JKQ
 | | Human DPP9-CARD8 complex | | Descriptor: | Caspase recruitment domain-containing protein 8, Dipeptidyl peptidase 9 | | Authors: | Sharif, H, Hollingsworth, L.R. | | Deposit date: | 2020-07-28 | | Release date: | 2021-05-26 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Dipeptidyl peptidase 9 sets a threshold for CARD8 inflammasome formation by sequestering its active C-terminal fragment.
Immunity, 54, 2021
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7KEU
 | | Cryo-EM structure of the Caspase-1-CARD:ASC-CARD octamer | | Descriptor: | Apoptosis-associated speck-like protein containing a CARD, Caspase-1 | | Authors: | Hollingsworth, L.R, David, L, Li, Y, Ruan, J, Wu, H. | | Deposit date: | 2020-10-12 | | Release date: | 2020-11-25 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Mechanism of filament formation in UPA-promoted CARD8 and NLRP1 inflammasomes.
Nat Commun, 12, 2021
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