8T59
| Crystal structure of Para.09 bound to TREM2 | 分子名称: | DI(HYDROXYETHYL)ETHER, GLYCEROL, Para.09 heavy chain, ... | 著者 | Wallweber, H, Hsu, P.L. | 登録日 | 2023-06-12 | 公開日 | 2024-07-31 | 最終更新日 | 2024-10-09 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Rapid affinity optimization of an anti-TREM2 clinical lead antibody by cross-lineage immune repertoire mining. Nat Commun, 15, 2024
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6W3B
| Structure of apo unphosphorylated IRE1 | 分子名称: | Serine/threonine-protein kinase/endoribonuclease IRE1 | 著者 | Wallweber, H, Mortara, K, Ferri, E, Rudolph, J, Wang, W. | 登録日 | 2020-03-09 | 公開日 | 2020-12-09 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.57 Å) | 主引用文献 | Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands. Nat Commun, 11, 2020
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6W3C
| Structure of phosphorylated apo IRE1 | 分子名称: | Serine/threonine-protein kinase/endoribonuclease IRE1 | 著者 | Wallweber, H, Mortara, K, Ferri, E, Wang, W, Rudolph, J. | 登録日 | 2020-03-09 | 公開日 | 2020-12-09 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | 主引用文献 | Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands. Nat Commun, 11, 2020
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6XDD
| Crystal structure of IRE1 in complex with G-3053 | 分子名称: | 4-[(trans-4-aminocyclohexyl)amino]-N-(6-chloro-3-{[(2,5-difluorophenyl)sulfonyl]amino}-2-fluorophenyl)thieno[3,2-d]pyrimidine-7-carboxamide, Serine/threonine-protein kinase/endoribonuclease IRE1 | 著者 | Ackerly-Wallweber, H, Wang, W. | 登録日 | 2020-06-10 | 公開日 | 2021-04-21 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1 alpha Inhibitory Activity. Acs Med.Chem.Lett., 11, 2020
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4K1B
| Structure of PIM-1 kinase bound to N-(5-(2-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-((((3R,4R)-3-fluoropiperidin-4-yl)methyl)amino)pyrazolo[1,5-a]pyrimidine-3-carboxamide | 分子名称: | N-[5-(2-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-5-({[(3R,4R)-3-fluoropiperidin-4-yl]methyl}amino)pyrazolo[1,5-a]pyrimidine-3-carboxamide, PHOSPHATE ION, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H, Steffek, M. | 登録日 | 2013-04-04 | 公開日 | 2013-05-15 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (2.082 Å) | 主引用文献 | Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design. Bioorg.Med.Chem.Lett., 23, 2013
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4K18
| Structure of PIM-1 kinase bound to 5-(4-cyanobenzyl)-N-(4-fluorophenyl)-7-hydroxypyrazolo[1,5-a]pyrimidine-3-carboxamide | 分子名称: | 5-(4-cyanobenzyl)-N-(4-fluorophenyl)-7-hydroxypyrazolo[1,5-a]pyrimidine-3-carboxamide, PHOSPHATE ION, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H, Steffek, M. | 登録日 | 2013-04-04 | 公開日 | 2013-05-15 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (2.051 Å) | 主引用文献 | Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design. Bioorg.Med.Chem.Lett., 23, 2013
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4K0Y
| Structure of PIM-1 kinase bound to N-(4-fluorophenyl)-7-hydroxy-5-(piperidin-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | 分子名称: | N-(4-fluorophenyl)-7-hydroxy-5-(piperidin-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide, PHOSPHATE ION, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H, Steffek, M. | 登録日 | 2013-04-04 | 公開日 | 2013-05-15 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.954 Å) | 主引用文献 | Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design. Bioorg.Med.Chem.Lett., 23, 2013
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4OLI
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5DGZ
| Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors | 分子名称: | (2S)-1-(1H-INDOL-3-YL)-3-{[5-(3-METHYL-1H-INDAZOL-5-YL)PYRIDIN-3-YL]OXY}PROPAN-2-AMINE, PHOSPHATE ION, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H, Steffek, M. | 登録日 | 2015-08-29 | 公開日 | 2015-10-28 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (2.502 Å) | 主引用文献 | Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors. Bioorg.Med.Chem.Lett., 25, 2015
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5DHJ
| PIM1 in complex with Cpd4 (3-methyl-5-(pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridine) | 分子名称: | 3-methyl-5-(pyridin-3-yl)-2H-pyrazolo[3,4-c]pyridine, PHOSPHATE ION, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H. | 登録日 | 2015-08-31 | 公開日 | 2015-10-28 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (2.457 Å) | 主引用文献 | Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors. Bioorg.Med.Chem.Lett., 25, 2015
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5DIA
| PIM1 in complex with Cpd36 ((1S,3S)-N1-(6-(5-(pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridin-3-yl)pyridin-2-yl)cyclohexane-1,3-diamine) | 分子名称: | (1S,3S)-N-{6-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridin-3-yl]pyridin-2-yl}cyclohexane-1,3-diamine, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H. | 登録日 | 2015-08-31 | 公開日 | 2015-10-28 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (1.964 Å) | 主引用文献 | Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors. Bioorg.Med.Chem.Lett., 25, 2015
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5V80
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8T51
| Crystal structure of Fab 3.10C2 bound to TREM2 | 分子名称: | 3.10C2 Fab heavy chain, 3.10C2 Fab light chain, ACETATE ION, ... | 著者 | Hsu, P.L, Wallweber, H. | 登録日 | 2023-06-12 | 公開日 | 2024-06-19 | 最終更新日 | 2024-10-09 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Rapid affinity optimization of an anti-TREM2 clinical lead antibody by cross-lineage immune repertoire mining. Nat Commun, 15, 2024
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5V82
| PIM1 kinase in complex with Cpd17 (1-(6-(4,4-difluoropiperidin-3-yl)pyridin-2-yl)-6-(6-methylpyrazin-2-yl)-1H-pyrazolo[4,3-c]pyridine) | 分子名称: | 1-{6-[(3R)-4,4-difluoropiperidin-3-yl]pyridin-2-yl}-6-(6-methylpyrazin-2-yl)-1H-pyrazolo[4,3-c]pyridine, Serine/threonine-protein kinase pim-1 | 著者 | Murray, J.M, Wallweber, H. | 登録日 | 2017-03-21 | 公開日 | 2017-05-10 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (1.888 Å) | 主引用文献 | Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. J. Med. Chem., 60, 2017
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3T6P
| IAP antagonist-induced conformational change in cIAP1 promotes E3 ligase activation via dimerization | 分子名称: | Baculoviral IAP repeat-containing protein 2, ZINC ION | 著者 | Dueber, E.C, Schoeffler, A.J, Lingel, A, Elliott, M, Fedorova, A.V, Giannetti, A.M, Zobel, K, Maurer, B, Varfolomeev, E, Wu, P, Wallweber, H, Hymowitz, S, Deshayes, K, Vucic, D, Fairbrother, W.J. | 登録日 | 2011-07-28 | 公開日 | 2011-11-02 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.897 Å) | 主引用文献 | Antagonists induce a conformational change in cIAP1 that promotes autoubiquitination. Science, 334, 2011
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