5A6R
| Crystal structure of the BTB domain of human KCTD17 | Descriptor: | BTB/POZ DOMAIN-CONTAINING PROTEIN KCTD17 | Authors: | Pinkas, D.M, Sorrell, F, Sanvitale, C.E, Goubin, S, Williams, E, Newman, J.A, Pearce, N.M, Neshich, I, Pike, A.C.W, MacKenzie, A, Quigley, A, Faust, B, Carpenter, E.P, Tallant, C, Kopec, J, Chalk, R, Krojer, T, Burgess-Brown, N.A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2015-06-30 | Release date: | 2015-11-04 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.85 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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4AW6
| Crystal structure of the human nuclear membrane zinc metalloprotease ZMPSTE24 (FACE1) | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, CAAX PRENYL PROTEASE 1 HOMOLOG, ZINC ION | Authors: | Pike, A.C.W, Dong, Y.Y, Quigley, A, Dong, L, Cooper, C.D.O, Chaikuad, A, Goubin, S, Shrestha, L, Li, Q, Mukhopadhyay, S, Yang, J, Xia, X, Shintre, C.A, Barr, A.J, Berridge, G, Chalk, R, Bray, J.E, von Delft, F, Bullock, A, Bountra, C, Arrowsmith, C.H, Edwards, A, Burgess-Brown, N, Carpenter, E.P. | Deposit date: | 2012-05-31 | Release date: | 2012-07-25 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (3.4 Å) | Cite: | The Structural Basis of Zmpste24-Dependent Laminopathies. Science, 339, 2013
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2C3I
| CRYSTAL STRUCTURE OF HUMAN PIM1 IN COMPLEX WITH IMIDAZOPYRIDAZIN I | Descriptor: | 1-(3-{6-[(CYCLOPROPYLMETHYL)AMINO]IMIDAZO[1,2-B]PYRIDAZIN-3-YL}PHENYL)ETHANONE, PIMTIDE, PROTO-ONCOGENE SERINE THREONINE PROTEIN KINASE PIM1 | Authors: | Philippakopoulos, P, Knapp, S, Debreczeni, J, Bullock, A, von Delft, F, Sundstrom, M, Arrowsmith, C, Edwards, A, Guo, K, Weigelt, J. | Deposit date: | 2005-10-07 | Release date: | 2005-11-01 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structural Analysis Identifies Imidazo[1,2- B]Pyridazines as Pim Kinase Inhibitors with in Vitro Antileukemic Activity. Cancer Res., 67, 2007
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6YMQ
| TREM2 extracellular domain (19-131) in complex with single-chain variable 4 (scFv-4) | Descriptor: | (4S)-2-METHYL-2,4-PENTANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, Single-chain variable 4, ... | Authors: | Szykowska, A, Preger, C, Scacioc, A, Mukhopadhyay, S.M.M, McKinley, G, Graslund, S, Wigren, E, Persson, H, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Di Daniel, E, Davis, J.B, Burgess-Brown, N, Bullock, A. | Deposit date: | 2020-04-09 | Release date: | 2021-02-17 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.07 Å) | Cite: | Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain. Structure, 29, 2021
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6Y6C
| TREM2 extracellular domain (19-174) in complex with single-chain variable fragment (scFv-4) | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Single chain variable, Triggering receptor expressed on myeloid cells 2 | Authors: | Szykowska, A, Preger, C, Williams, E, Mukhopadhyay, S.M.M, McKinley, G, Gruslund, S, Wigren, E, Persson, H, Arrowsmith, C.H, Edwards, A, von Delft, F, Bountra, C, Davis, J.B, Di Daniel, E, Burgess-Brown, N, Bullock, A. | Deposit date: | 2020-02-26 | Release date: | 2021-02-17 | Last modified: | 2024-10-16 | Method: | X-RAY DIFFRACTION (2.26 Å) | Cite: | Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain. Structure, 29, 2021
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3II7
| Crystal structure of the kelch domain of human KLHL7 | Descriptor: | 1,2-ETHANEDIOL, Kelch-like protein 7 | Authors: | Chaikuad, A, Thangaratnarajah, C, Cooper, C.D.O, Ugochukwu, E, Muniz, J.R.C, Krojer, T, Sethi, R, Pike, A.C.W, Filippakopoulos, P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2009-07-31 | Release date: | 2009-08-25 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.63 Å) | Cite: | Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases. J.Biol.Chem., 288, 2013
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6YYE
| TREM2 extracellular domain (19-131) in complex with single-chain variable fragment (scFv-2) | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, TREM2 Single chain variable 2, Triggering receptor expressed on myeloid cells 2 | Authors: | Szykowska, A, Preger, C, Krojer, T, Mukhopadhyay, S.M.M, McKinley, G, Graslund, S, Wigren, E, Persson, H, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Di Daniel, E, Burgess-Brown, N, Bullock, A. | Deposit date: | 2020-05-04 | Release date: | 2021-02-17 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.36 Å) | Cite: | Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain. Structure, 29, 2021
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7OOX
| Crystal structure of PIM1 in complex with ARC-3126 | Descriptor: | 1,2-ETHANEDIOL, Inhibitor ARC-3126, PHOSPHATE ION, ... | Authors: | Chaikuad, A, Dixon-Clarke, S.E, Nonga, O.E, Uri, A, Bullock, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2021-05-28 | Release date: | 2021-08-04 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.97 Å) | Cite: | Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules, 26, 2021
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7OOV
| Crystal structure of PIM1 in complex with ARC-1411 | Descriptor: | 1,2-ETHANEDIOL, Inhibitor ARC-1411, SULFATE ION, ... | Authors: | Chaikuad, A, Dixon-Clarke, S.E, Nonga, O.E, Uri, A, Bullock, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2021-05-28 | Release date: | 2021-08-04 | Last modified: | 2024-04-10 | Method: | X-RAY DIFFRACTION (1.96 Å) | Cite: | Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules, 26, 2021
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7OOW
| Crystal structure of PIM1 in complex with ARC-1415 | Descriptor: | 1,2-ETHANEDIOL, INHIBITOR ARC-1415, MAGNESIUM ION, ... | Authors: | Chaikuad, A, Dixon-Clarke, S.E, Nonga, O.E, Uri, A, Bullock, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2021-05-28 | Release date: | 2021-08-04 | Last modified: | 2024-04-10 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules, 26, 2021
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5NLB
| Crystal structure of human CUL3 N-terminal domain bound to KEAP1 BTB and 3-box | Descriptor: | Cullin-3, Kelch-like ECH-associated protein 1 | Authors: | Adamson, R, Krojer, T, Pinkas, D.M, Bartual, S.G, Burgess-Brown, N.A, Borkowska, O, Chalk, R, Newman, J.A, Kopec, J, Dixon-Clarke, S.E, Mathea, S, Sethi, R, Velupillai, S, Mackinnon, S, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2017-04-04 | Release date: | 2017-04-19 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (3.45 Å) | Cite: | Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly. Free Radic Biol Med, 204, 2023
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3F2O
| Crystal Structure of human splA/ryanodine receptor domain and SOCS box containing 1 (SPSB1) in complex with a 20-residue VASA peptide | Descriptor: | 20-mer peptide from ATP-dependent RNA helicase vasa, SPRY domain-containing SOCS box protein 1 | Authors: | Filippakopoulos, P, Sharpe, T, Keates, T, Murray, J.W, Savitsky, P, Roos, A, Pike, A.C.W, Von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2008-10-30 | Release date: | 2008-12-09 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4. J.Mol.Biol., 401, 2010
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3G2F
| Crystal structure of the kinase domain of bone morphogenetic protein receptor type II (BMPR2) at 2.35 A resolution | Descriptor: | 1,2-ETHANEDIOL, ADENOSINE-5'-DIPHOSPHATE, Bone morphogenetic protein receptor type-2, ... | Authors: | Chaikuad, A, Thangaratnarajah, C, Roos, A.K, Filippakopoulos, P, Salah, E, Phillips, C, Keates, T, Fedorov, O, Chalk, R, Petrie, K, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2009-01-31 | Release date: | 2009-02-17 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension. Sci Rep, 9, 2019
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3H9R
| Crystal structure of the kinase domain of type I activin receptor (ACVR1) in complex with FKBP12 and dorsomorphin | Descriptor: | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine, Activin receptor type-1, Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | Authors: | Chaikuad, A, Alfano, I, Shrestha, B, Muniz, J.R.C, Petrie, K, Fedorov, O, Phillips, C, Bishop, S, Mahajan, P, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2009-04-30 | Release date: | 2009-06-02 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Structure of the Bone Morphogenetic Protein Receptor ALK2 and Implications for Fibrodysplasia Ossificans Progressiva. J.Biol.Chem., 287, 2012
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3EMW
| Crystal Structure of human splA/ryanodine receptor domain and SOCS box containing 2 (SPSB2) in complex with a 20-residue VASA peptide | Descriptor: | 1,2-ETHANEDIOL, Peptide (VASA), SPRY domain-containing SOCS box protein 2 | Authors: | Filippakopoulos, P, Sharpe, T, Keates, T, Murray, J.W, Savitsky, P, Roos, A.K, Pike, A.C.W, Von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2008-09-25 | Release date: | 2008-10-28 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4. J.Mol.Biol., 401, 2010
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5FTA
| Crystal structure of the N-terminal BTB domain of human KCTD10 | Descriptor: | BTB/POZ DOMAIN-CONTAINING ADAPTER FOR CUL3-MEDIATED RHOA DEGRADATION PROTEIN 3, MERCURY (II) ION | Authors: | Pinkas, D.M, Sanvitale, C.E, Solcan, N, Goubin, S, Tallant, C, Newman, J.A, Kopec, J, Fitzpatrick, F, Talon, R, Collins, P, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2016-01-12 | Release date: | 2016-02-17 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.64 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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5FDP
| Structure of DDR1 receptor tyrosine kinase in complex with D2099 inhibitor at 2.25 Angstroms resolution. | Descriptor: | (4~{S})-4-methyl-~{N}-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-2-pyrimidin-5-yl-3,4-dihydro-1~{H}-isoquinoline-7-carboxamide, 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, ... | Authors: | Bartual, S.G, Pinkas, D.M, Wang, Z, Ding, K, Mahajan, P, Kupinska, K, Mukhopadhyay, S, Strain-Damerell, C, Borkowska, O, Talon, R, Kopec, J, Williams, E, Tallant, C, Chaikuad, A, Sorell, F, Newman, J, Burgess-Brown, N, Arrowsmith, C.H, von Delft, F, Edwards, A.M, Bountra, C, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2015-12-16 | Release date: | 2016-06-08 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.25 Å) | Cite: | Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J.Med.Chem., 59, 2016
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5G6V
| Crystal structure of the PCTAIRE1 kinase in complex with inhibitor | Descriptor: | 1,2-ETHANEDIOL, 4-[4-({[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, CYCLIN-DEPENDENT KINASE 16 | Authors: | Dixon-Clarke, S.E, Galan Bartual, S, Elkins, J, Savitsky, P, Kopec, J, Mackenzie, A, Tallant, C, Heroven, C, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2016-08-16 | Release date: | 2016-11-23 | Last modified: | 2024-06-19 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16. Biochem.J., 474, 2017
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5A15
| Crystal structure of the BTB domain of human KCTD16 | Descriptor: | BTB/POZ DOMAIN-CONTAINING PROTEIN KCTD16 | Authors: | Pinkas, D.M, Sanvitale, C.E, Solcan, N, Goubin, S, Canning, P, Dixon Clarke, S.E, Talon, R, Wiggers, H.J, Fitzpatrick, F, Tallant, C, Kopec, J, Chalk, R, Doutch, J, Krojer, T, Burgess-Brown, N.A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2015-04-28 | Release date: | 2015-11-04 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.76 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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5ACB
| Crystal Structure of the Human Cdk12-Cyclink Complex | Descriptor: | CYCLIN-DEPENDENT KINASE 12, CYCLIN-K, N-[4-[(3R)-3-[[5-chloranyl-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]carbonylphenyl]-4-(dimethylamino)butanamide | Authors: | Dixon Clarke, S.E, Elkins, J.M, Pike, A.C.W, Mackenzie, A, Goubin, S, Strain-Damerell, C, Mahajan, P, Tallant, C, Chalk, R, Wiggers, H, Kopec, J, Fitzpatrick, F, Burgess-Brown, N, Carpenter, E.P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2015-08-14 | Release date: | 2016-06-15 | Last modified: | 2016-10-05 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Covalent Targeting of Remote Cysteine Residues to Develop Cdk12 and Cdk13 Inhibitors. Nat.Chem.Biol., 12, 2016
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4CH9
| Crystal structure of the human KLHL3 Kelch domain in complex with a WNK4 peptide | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, KELCH-LIKE PROTEIN 3, ... | Authors: | Sorrell, F.J, Schumacher, F.R, Kurz, T, Alessi, D.R, Newman, J, Goubin, S, Chalk, R, Kopec, J, Tallant, C, Williams, E, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2013-11-29 | Release date: | 2014-01-08 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (1.84 Å) | Cite: | Structural and Biochemical Characterisation of the Klhl3-Wnk Kinase Interaction Important in Blood Pressure Regulation. Biochem.J., 460, 2014
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4CKR
| Crystal structure of the human DDR1 kinase domain in complex with DDR1-IN-1 | Descriptor: | 1,2-ETHANEDIOL, 4-[(4-ethylpiperazin-1-yl)methyl]-n-{4-methyl-3-[(2-oxo-2,3-dihydro-1h-indol-5-yl)oxy]phenyl}-3-(trifluoromethyl)benzamide, EPITHELIAL DISCOIDIN DOMAIN-CONTAINING RECEPTOR 1 | Authors: | Canning, P, Elkins, J.M, Goubin, S, Mahajan, P, Krojer, T, Newman, J.A, Dixon-Clarke, S, Chaikuad, A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2014-01-07 | Release date: | 2014-01-15 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Discovery of a Potent and Selective Ddr1 Receptor Tyrosine Kinase Inhibitor. Acs Chem.Biol., 8, 2013
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4CRH
| Crystal structure of the BTB-T1 domain of human SHKBP1 | Descriptor: | SH3KBP1-BINDING PROTEIN 1 | Authors: | Pinkas, D.M, Solcan, N, Krojer, T, Goubin, S, Williams, E.P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2014-02-26 | Release date: | 2014-03-12 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (1.72 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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4CXA
| Crystal structure of the human CDK12-cyclin K complex bound to AMPPNP | Descriptor: | CYCLIN-DEPENDENT KINASE 12, CYCLIN-K, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | Authors: | Dixon Clarke, S.E, Elkins, J.M, Pike, A.C.W, Nowak, R, Goubin, S, Mahajan, R.P, Kopec, J, Froese, S, Tallant, C, Carpenter, E.P, Mackenzie, A, Faust, B, Burgess-Brown, N, von Delft, F, Arrowsmith, C, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2014-04-04 | Release date: | 2014-05-21 | Last modified: | 2024-10-16 | Method: | X-RAY DIFFRACTION (3.15 Å) | Cite: | Structures of the Cdk12/Cyck Complex with AMP-Pnp Reveal a Flexible C-Terminal Kinase Extension Important for ATP Binding. Sci.Rep., 5, 2015
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4CHB
| Crystal structure of the human KLHL2 Kelch domain in complex with a WNK4 peptide | Descriptor: | 1,2-ETHANEDIOL, DODECAETHYLENE GLYCOL, KELCH-LIKE PROTEIN 2, ... | Authors: | Sorrell, F.J, Schumacher, F.R, Kurz, T, Alessi, D.R, Newman, J, Cooper, C.D.O, Canning, P, Kopec, J, Williams, E, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2013-11-29 | Release date: | 2014-01-08 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (1.56 Å) | Cite: | Structural and Biochemical Characterisation of the Klhl3-Wnk Kinase Interaction Important in Blood Pressure Regulation. Biochem.J., 460, 2014
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