1FQ9
 
 | | CRYSTAL STRUCTURE OF A TERNARY FGF2-FGFR1-HEPARIN COMPLEX | | Descriptor: | 4-deoxy-2-O-sulfo-alpha-L-threo-hex-4-enopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose, 4-deoxy-2-O-sulfo-alpha-L-threo-hex-4-enopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose-(1-4)-2-O-sulfo-beta-L-altropyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose, FIBROBLAST GROWTH FACTOR 2, ... | | Authors: | Schlessinger, J, Plotnikov, A.N, Ibrahimi, O.A, Eliseenkova, A.V, Yeh, B.K, Yayon, A, Linhardt, R.J, Mohammadi, M. | | Deposit date: | 2000-09-04 | | Release date: | 2000-09-27 | | Last modified: | 2021-11-03 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Crystal structure of a ternary FGF-FGFR-heparin complex reveals a dual role for heparin in FGFR binding and dimerization.
Mol.Cell, 6, 2000
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1MAI
 | | STRUCTURE OF THE PLECKSTRIN HOMOLOGY DOMAIN FROM PHOSPHOLIPASE C DELTA IN COMPLEX WITH INOSITOL TRISPHOSPHATE | | Descriptor: | D-MYO-INOSITOL-1,4,5-TRIPHOSPHATE, PHOSPHOLIPASE C DELTA-1 | | Authors: | Ferguson, K.M, Lemmon, M.A, Schlessinger, J, Sigler, P.B. | | Deposit date: | 1996-05-23 | | Release date: | 1996-11-08 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structure of the high affinity complex of inositol trisphosphate with a phospholipase C pleckstrin homology domain.
Cell(Cambridge,Mass.), 83, 1995
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6DRW
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6NFJ
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8DFM
 | | Ectodomain of full-length wild-type KIT-SCF dimers | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Isoform 2 of Mast/stem cell growth factor receptor Kit, ... | | Authors: | Krimmer, S.G, Bertoletti, N, Mi, W, Schlessinger, J. | | Deposit date: | 2022-06-22 | | Release date: | 2023-03-29 | | Last modified: | 2023-04-05 | | Method: | ELECTRON MICROSCOPY (3.45 Å) | | Cite: | Cryo-EM analyses of KIT and oncogenic mutants reveal structural oncogenic plasticity and a target for therapeutic intervention.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8DFP
 | | Ectodomain of full-length KIT(DupA502,Y503)-SCF dimers | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Isoform 2 of Mast/stem cell growth factor receptor Kit, ... | | Authors: | Bertoletti, N, Krimmer, S.G, Mi, W, Schlessinger, J. | | Deposit date: | 2022-06-22 | | Release date: | 2023-03-29 | | Last modified: | 2023-04-05 | | Method: | ELECTRON MICROSCOPY (3.17 Å) | | Cite: | Cryo-EM analyses of KIT and oncogenic mutants reveal structural oncogenic plasticity and a target for therapeutic intervention.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8DFQ
 | | Ectodomain of full-length KIT(T417I,delta418-419)-SCF dimers | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Isoform 2 of Mast/stem cell growth factor receptor Kit, ... | | Authors: | Krimmer, S.G, Bertoletti, N, Mi, W, Schlessinger, J. | | Deposit date: | 2022-06-22 | | Release date: | 2023-03-29 | | Last modified: | 2023-04-05 | | Method: | ELECTRON MICROSCOPY (3.96 Å) | | Cite: | Cryo-EM analyses of KIT and oncogenic mutants reveal structural oncogenic plasticity and a target for therapeutic intervention.
Proc.Natl.Acad.Sci.USA, 120, 2023
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3KVQ
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3KXX
 | | Structure of the mutant Fibroblast Growth Factor receptor 1 | | Descriptor: | Basic fibroblast growth factor receptor 1 | | Authors: | Bae, J.H, Boggon, T.J, Tome, F, Mandiyan, V, Lax, I, Schlessinger, J. | | Deposit date: | 2009-12-04 | | Release date: | 2010-03-02 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells.
Proc.Natl.Acad.Sci.USA, 107, 2010
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3KY2
 | | Crystal structure of Fibroblast Growth Factor Receptor 1 kinase domain | | Descriptor: | Basic fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Bae, J.H, Boggon, T.J, Tome, F, Mandiyan, V, Lax, I, Schlessinger, J. | | Deposit date: | 2009-12-04 | | Release date: | 2010-03-02 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells.
Proc.Natl.Acad.Sci.USA, 107, 2010
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5CUS
 | | Crystal Structure of sErbB3-Fab3379 Complex | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Fab LC region of KTN3379, IgG H chain, ... | | Authors: | Lee, S, Schlessinger, J. | | Deposit date: | 2015-07-25 | | Release date: | 2015-10-14 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Inhibition of ErbB3 by a monoclonal antibody that locks the extracellular domain in an inactive configuration.
Proc.Natl.Acad.Sci.USA, 112, 2015
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4PGZ
 | | Structural basis of KIT activation by oncogenic mutations in the extracellular region reveals a zipper-like mechanism for ligand-dependent or oncogenic receptor tyrosine kinase activation | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, COBALT (II) ION, Mast/stem cell growth factor receptor Kit | | Authors: | Reshetnyak, A.V, Boggon, T.J, Lax, I, Schlessinger, J. | | Deposit date: | 2014-05-03 | | Release date: | 2015-03-18 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | The strength and cooperativity of KIT ectodomain contacts determine normal ligand-dependent stimulation or oncogenic activation in cancer.
Mol.Cell, 57, 2015
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6OBL
 | | JAK2 JH2 in complex with JAK168 | | Descriptor: | Tyrosine-protein kinase JAK2, [4-({5-amino-3-[(4-cyanophenyl)amino]-1H-1,2,4-triazole-1-carbonyl}amino)phenoxy]acetic acid | | Authors: | Krimmer, S.G, Liosi, M.E, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2019-03-21 | | Release date: | 2020-03-25 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.061 Å) | | Cite: | Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
J.Med.Chem., 63, 2020
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6OBF
 | | JAK2 JH2 in complex with JAK179 | | Descriptor: | GLYCEROL, Tyrosine-protein kinase JAK2, [4-({5-amino-3-[(4-sulfamoylphenyl)amino]-1H-1,2,4-triazole-1-carbonyl}amino)phenoxy]acetic acid | | Authors: | Krimmer, S.G, Liosi, M.E, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2019-03-20 | | Release date: | 2020-03-25 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.71 Å) | | Cite: | Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
J.Med.Chem., 63, 2020
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6OCC
 | | JAK2 JH2 in complex with JAK190 | | Descriptor: | 2-[4-({5-amino-3-[(4-sulfamoylphenyl)amino]-1H-1,2,4-triazole-1-carbonyl}amino)phenyl]-1,3-oxazole-4-carboxylic acid, GLYCEROL, Tyrosine-protein kinase JAK2 | | Authors: | Krimmer, S.G, Liosi, M.E, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2019-03-22 | | Release date: | 2020-03-25 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.03 Å) | | Cite: | Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
J.Med.Chem., 63, 2020
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2FGI
 | | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074 | | Descriptor: | 1-TERT-BUTYL-3-[6-(3,5-DIMETHOXY-PHENYL)-2-(4-DIETHYLAMINO-BUTYLAMINO)-PYRIDO[2,3-D]PYRIMIDIN-7-YL]-UREA, PROTEIN (FIBROBLAST GROWTH FACTOR (FGF) RECEPTOR 1) | | Authors: | Mohammadi, M, Froum, S, Hamby, J.M, Schroeder, M, Panek, R.L, Lu, G.H, Eliseenkova, A.V, Green, D, Schlessinger, J, Hubbard, S.R. | | Deposit date: | 1998-09-15 | | Release date: | 1999-09-13 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain.
EMBO J., 17, 1998
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7T0P
 | | JAK2 JH2 IN COMPLEX WITH JAK315 | | Descriptor: | 4'-{[5-amino-3-(4-sulfamoylanilino)-1H-1,2,4-triazole-1-carbonyl]amino}-4-(benzyloxy)[1,1'-biphenyl]-3-carboxylic acid, GLYCEROL, Tyrosine-protein kinase JAK2 | | Authors: | Ippolito, J.A, Liosi, M.-E, Krimmer, S.G, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2021-11-30 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.04 Å) | | Cite: | Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
J.Med.Chem., 65, 2022
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7JYO
 | | JAK2 JH2 in complex with JAK064 | | Descriptor: | 3-({4-amino-6-[(4-cyanophenyl)amino]-1,3,5-triazin-2-yl}oxy)benzoic acid, GLYCEROL, Tyrosine-protein kinase JAK2 | | Authors: | Puleo, D.E, Krimmer, S.G, Newton, A.S, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2020-08-31 | | Release date: | 2021-07-14 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.16127229 Å) | | Cite: | Indoloxytriazines as binding molecules for the JAK2 JH2 pseudokinase domain and its V617F variant
Tetrahedron Lett., 77, 2021
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7JYQ
 | | JAK2 JH2 in complex with JAK020 | | Descriptor: | GLYCEROL, N~2~-(4-fluorophenyl)-6-{[(5-{[(oxolan-2-yl)methyl]amino}-1,3,4-thiadiazol-2-yl)sulfanyl]methyl}-1,3,5-triazine-2,4-diamine, Tyrosine-protein kinase JAK2 | | Authors: | Puleo, D.E, Krimmer, S.G, Newton, A.S, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2020-08-31 | | Release date: | 2021-07-14 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.85941613 Å) | | Cite: | Indoloxytriazines as binding molecules for the JAK2 JH2 pseudokinase domain and its V617F variant
Tetrahedron Lett., 77, 2021
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3B2T
 | | Structure of phosphotransferase | | Descriptor: | 5'-O-[(S)-hydroxy{[(S)-hydroxy(methyl)phosphoryl]oxy}phosphoryl]adenosine, Fibroblast growth factor receptor 2, PHOSPHATE ION | | Authors: | Lew, E.D, Bae, J.H, Rohmann, E, Wollnik, B, Schlessinger, J. | | Deposit date: | 2007-10-19 | | Release date: | 2008-02-26 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structural basis for reduced FGFR2 activity in LADD syndrome: Implications for FGFR autoinhibition and activation.
Proc.Natl.Acad.Sci.Usa, 104, 2007
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4K9E
 | | Crystal structure of KIT D4D5 fragment in complex with anti-Kit antibodies Fab79D | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Mast/stem cell growth factor receptor Kit, heavy chain, ... | | Authors: | Resheynyak, A.V, Boggon, T.J, Lax, I, Schlessinger, J. | | Deposit date: | 2013-04-19 | | Release date: | 2013-10-16 | | Last modified: | 2020-07-29 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structural basis for KIT receptor tyrosine kinase inhibition by antibodies targeting the D4 membrane-proximal region.
Proc.Natl.Acad.Sci.USA, 110, 2013
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6BRW
 | | JAK2 JH2 in complex with XMU-MP-1 | | Descriptor: | 4-[(5,10-dimethyl-6-oxo-6,10-dihydro-5H-pyrimido[5,4-b]thieno[3,2-e][1,4]diazepin-2-yl)amino]benzenesulfonamide, ACETATE ION, GLYCEROL, ... | | Authors: | Puleo, D.E, Schlessinger, J. | | Deposit date: | 2017-12-01 | | Release date: | 2018-08-15 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.031 Å) | | Cite: | JAK2 JH2 Binders
To Be Published
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6BS0
 | | JAK2 JH2 in complex with 63552444 | | Descriptor: | 4-(5-aminopyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridin-6-amine, GLYCEROL, Tyrosine-protein kinase JAK2 | | Authors: | Puleo, D.E, Schlessinger, J. | | Deposit date: | 2017-12-01 | | Release date: | 2018-08-22 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.541 Å) | | Cite: | JAK2 JH2 Binders
To Be Published
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6BSS
 | | JAK2 JH2 in complex with NU6102 | | Descriptor: | GLYCEROL, O6-CYCLOHEXYLMETHOXY-2-(4'-SULPHAMOYLANILINO) PURINE, Tyrosine-protein kinase JAK2 | | Authors: | Puleo, D.E, Schlessinger, J. | | Deposit date: | 2017-12-04 | | Release date: | 2018-08-15 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | JAK2 JH2 Binders
To Be Published
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1FGI
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