6HRL
 
 | | Crystal structure of the Kelch domain of human KLHL17 | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, Kelch-like protein 17, ... | | 著者 | Chen, Z, Williams, E, Sorrell, F.J, Newman, J.A, Shrestha, L, Burgess-Brown, N, von Delft, F, Arrowsmith, F, Edwards, C.H, Bountra, C, Bullock, A.N. | | 登録日 | 2018-09-27 | | 公開日 | 2018-10-17 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal structure of the Kelch domain of human KLHL17
To Be Published
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6GY5
 | | Crystal structure of the kelch domain of human KLHL20 in complex with DAPK1 peptide | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, Death-associated protein kinase 1, ... | | 著者 | Chen, Z, Hozjan, V, Strain-Damerell, C, Williams, E, Wang, D, Cooper, C.D.O, Sanvitale, C.E, Fairhead, M, Carpenter, E.P, Pike, A.C.W, Krojer, T, Srikannathasan, V, Sorrell, F, Johansson, C, Mathea, S, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A.N. | | 登録日 | 2018-06-28 | | 公開日 | 2018-08-08 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.086 Å) | | 主引用文献 | Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase.
Structure, 27, 2019
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6FMQ
 | | Keap1 - peptide complex | | 分子名称: | 1,2-ETHANEDIOL, ACETATE ION, ACY-SC1-GLU-THR-GLY-GLU-LEU, ... | | 著者 | Talapatra, S.K, Kozielski, F, Wells, G, Georgakopoulos, N.D. | | 登録日 | 2018-02-02 | | 公開日 | 2018-08-08 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Modified Peptide Inhibitors of the Keap1-Nrf2 Protein-Protein Interaction Incorporating Unnatural Amino Acids.
Chembiochem, 19, 2018
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6FMP
 | | Keap1 - peptide complex | | 分子名称: | 1,2-ETHANEDIOL, ACETATE ION, ACY-ASP-GLU-GLU-THR-GLY-GLU-PHE, ... | | 著者 | Talapatra, S.K, Kozielski, F, Wells, G, Georgakopoulos, N.D. | | 登録日 | 2018-02-01 | | 公開日 | 2018-08-08 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.92 Å) | | 主引用文献 | Modified Peptide Inhibitors of the Keap1-Nrf2 Protein-Protein Interaction Incorporating Unnatural Amino Acids.
Chembiochem, 19, 2018
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5YY8
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5YQ4
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5X54
 | | Crystal structure of the Keap1 Kelch domain in complex with a tetrapeptide | | 分子名称: | ACE-GLU-TRP-TRP-TRP, ACETATE ION, Kelch-like ECH-associated protein 1 | | 著者 | Sogabe, S, Kadotani, A, Lane, W, Snell, G. | | 登録日 | 2017-02-14 | | 公開日 | 2017-03-29 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Discovery of a Kelch-like ECH-associated protein 1-inhibitory tetrapeptide and its structural characterization
Biochem. Biophys. Res. Commun., 486, 2017
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5WIY
 | | Kelch domain of human Keap1 bound to small molecule inhibitor fragment: 4-amino-1,7-dihydro-6H-pyrazolo[3,4-d]pyrimidine-6-thione | | 分子名称: | 4-amino-1,7-dihydro-6H-pyrazolo[3,4-d]pyrimidine-6-thione, Kelch-like ECH-associated protein 1, SULFATE ION | | 著者 | Carolan, J.P, Lynch, A.J, Allen, K.N. | | 登録日 | 2017-07-20 | | 公開日 | 2018-09-26 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.23 Å) | | 主引用文献 | Interaction Energetics and Druggability of the Protein-Protein Interaction between Kelch-like ECH-Associated Protein 1 (KEAP1) and Nuclear Factor Erythroid 2 Like 2 (Nrf2).
Biochemistry, 59, 2020
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5WHO
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5WHL
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5WG1
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5WFV
 | | Kelch domain of human Keap1 bound to Nrf2 ETGE peptide | | 分子名称: | Kelch-like ECH-associated protein 1, Nrf2 ETGE peptide, SULFATE ION | | 著者 | Carolan, J.P, Lynch, A.J, Allen, K.N. | | 登録日 | 2017-07-12 | | 公開日 | 2018-09-19 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.91 Å) | | 主引用文献 | Interaction Energetics and Druggability of the Protein-Protein Interaction between Kelch-like ECH-Associated Protein 1 (KEAP1) and Nuclear Factor Erythroid 2 Like 2 (Nrf2).
Biochemistry, 59, 2020
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5WFL
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5NKP
 | | Crystal structure of the human KLHL3 Kelch domain in complex with a WNK3 peptide | | 分子名称: | CHLORIDE ION, CITRIC ACID, Kelch-like protein 3, ... | | 著者 | Chen, Z, Sorrell, F.J, Pinkas, D.M, Williams, E, Mathea, S, Goubin, S, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Burgess-Brown, N, Bountra, C, Bullock, A. | | 登録日 | 2017-03-31 | | 公開日 | 2017-05-03 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Crystal structure of the human KLHL3 Kelch domain in complex with a WNK3 peptide
To Be Published
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5GQT
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5GQ0
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5FZN
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | KELCH-LIKE ECH-ASSOCIATED PROTEIN 1, SULFATE ION, benzenesulfonamide | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2016-03-15 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.97 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5FZJ
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | 2,6-DIMETHYL-4H-PYRANO[3,4-D][1,3]OXAZOL-4-ONE, KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2016-03-14 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5FNU
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | (3S)-3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(4-methyl-3-(((R)-4-methyl-1,1-dioxido-3,4-dihydro-2H-benzo[b][1,4,5]oxathiazepin-2-yl)methyl)phenyl)propanoic acid, CHLORIDE ION, KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2015-11-16 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.78 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5FNT
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | (3S)-3-{4-Chloro-3-[(N-methylbenzenesulfonamido) methyl]phenyl}-3-(1-methyl-1H-1,2,3-benzotriazol-5-yl)propanoic acid, CHLORIDE ION, KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2015-11-16 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5FNS
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | (3s)-{4-Chloro-3-[(N-methylmethanesulfonamido) methyl]phenyl}-3-(1-methyl-1H-1,2,3-benzotriazol-5-yl) propanoic acid, CHLORIDE ION, KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2015-11-16 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5FNR
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | (3S)-3-(4-chlorophenyl)-3-(1-methylbenzotriazol-5-yl)propanoic acid, KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2015-11-16 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5FNQ
 | | Structure of the Keap1 Kelch domain in complex with a small molecule inhibitor. | | 分子名称: | 3-(4-CHLOROPHENYL)PROPANOIC ACID, KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 | | 著者 | Davies, T.G, Wixted, W.E, Coyle, J.E, Griffiths-Jones, C, Hearn, K, McMenamin, R, Norton, D, Rich, S.J, Richardson, C, Saxty, G, Willems, H.M.G, Woolford, A.J, Cottom, J.E, Kou, J, Yonchuk, J.G, Feldser, H.G, Sanchez, Y, Foley, J.P, Bolognese, B.J, Logan, G, Podolin, P.L, Yan, H, Callahan, J.F, Heightman, T.D, Kerns, J.K. | | 登録日 | 2015-11-16 | | 公開日 | 2016-04-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.91 Å) | | 主引用文献 | Mono-Acidic Inhibitors of the Kelch-Like Ech-Associated Protein 1 : Nuclear Factor Erythroid 2-Related Factor 2 (Keap1:Nrf2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
J.Med.Chem., 59, 2016
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5F72
 | | De novo design and crystallographic validation of antibodies targeting a pre-selected epitope | | 分子名称: | Kelch-like ECH-associated protein 1, Single chain Fv from a Fab | | 著者 | Liu, X, Taylor, R.D, Griffin, L, Coker, S, Adams, R, Ceska, T, Shi, J, Lawson, A.D.G, Baker, T. | | 登録日 | 2015-12-07 | | 公開日 | 2016-12-14 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | De novo design and crystallographic validation of antibodies targeting a pre-selected epitope
To Be Published
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5CGJ
 | | Crystal structure of murine Keap1 in complex with RA839, a non-covalent small-molecule binder to Keap1 and selective activator of Nrf2 signalling. | | 分子名称: | (3S)-1-(4-{[(2,3,5,6-tetramethylphenyl)sulfonyl]amino}naphthalen-1-yl)pyrrolidine-3-carboxylic acid, Kelch-like ECH-associated protein 1, SULFATE ION | | 著者 | Schimanski-Breves, S, Loenze, P, Engel, C.K. | | 登録日 | 2015-07-09 | | 公開日 | 2015-10-21 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.36 Å) | | 主引用文献 | Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling.
J.Biol.Chem., 290, 2015
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