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PDB: 52 results
4J95
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Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K659N Mutation Responsible for an Unclassified Craniosynostosis Syndrome in Space Group C2.
Descriptor: Fibroblast growth factor receptor 2, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, SULFATE ION
Authors:Chen, H, Mohammadi, M.
Deposit date:2013-02-15
Release date:2013-08-07
Last modified:2023-09-20
Method:X-RAY DIFFRACTION (2.3767 Å)
Cite:Cracking the Molecular Origin of Intrinsic Tyrosine Kinase Activity through Analysis of Pathogenic Gain-of-Function Mutations.
Cell Rep, 4, 2013
1DJS
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BU of 1djs by Molmil
LIGAND-BINDING PORTION OF FIBROBLAST GROWTH FACTOR RECEPTOR 2 IN COMPLEX WITH FGF1
Descriptor: PROTEIN (FIBROBLAST GROWTH FACTOR 1), PROTEIN (FIBROBLAST GROWTH FACTOR RECEPTOR 2), SULFATE ION
Authors:Stauber, D.J, Digabriele, A.D, Hendrickson, W.A.
Deposit date:1999-12-03
Release date:2000-01-12
Last modified:2022-12-21
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:Structural interactions of fibroblast growth factor receptor with its ligands.
Proc.Natl.Acad.Sci.USA, 97, 2000
1OEC
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FGFr2 kinase domain
Descriptor: 4-ARYL-2-PHENYLAMINO PYRIMIDINE, FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION
Authors:Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J.
Deposit date:2003-03-24
Release date:2004-10-27
Last modified:2023-12-13
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:The Crystal Structure of the Fgfr2 Tyrosine Kinase Domain in Complex with 4-Aryl-2-Phenylamino Pyrimidine Angiogenesis Inhibitors
To be Published
2PWL
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BU of 2pwl by Molmil
Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic N549H Mutation Responsible for Crouzon Syndrome.
Descriptor: Fibroblast growth factor receptor 2, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, SULFATE ION
Authors:Chen, H, Mohammadi, M.
Deposit date:2007-05-11
Release date:2007-09-25
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.
Mol.Cell, 27, 2007
1GJO
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BU of 1gjo by Molmil
The FGFr2 tyrosine kinase domain
Descriptor: FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION
Authors:Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J.
Deposit date:2001-07-31
Release date:2003-08-15
Last modified:2023-12-13
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:The Fgfr2 Tyrosine Kinase Domain
To be Published
2PZ5
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Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic N549T Mutation Responsible for Pfeiffer Syndrome
Descriptor: Fibroblast growth factor receptor 2, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ...
Authors:Chen, H, Mohammadi, M.
Deposit date:2007-05-17
Release date:2007-09-25
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.
Mol.Cell, 27, 2007
2PSQ
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BU of 2psq by Molmil
Crystal Structure of Unphosphorylated Unactivated Wild Type FGF Receptor 2 (FGFR2) Kinase Domain
Descriptor: Fibroblast growth factor receptor 2, SULFATE ION
Authors:Chen, H, Mohammadi, M.
Deposit date:2007-05-07
Release date:2007-09-25
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.
Mol.Cell, 27, 2007
2PZP
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BU of 2pzp by Molmil
Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K526E Mutation Responsible for Crouzon Syndrome
Descriptor: Fibroblast growth factor receptor 2, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ...
Authors:Chen, H, Mohammadi, M.
Deposit date:2007-05-18
Release date:2007-09-25
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.
Mol.Cell, 27, 2007
6V6Q
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BU of 6v6q by Molmil
Crystal Structure of Monophosphorylated FGF Receptor 2 isoform IIIb with PTR657
Descriptor: Fibroblast growth factor receptor 2, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER
Authors:Lin, C.-C, Wieteska, L, Poncet-Montange, G, Suen, K.M, Arold, S.T, Ahmed, Z, Ladbury, J.E.
Deposit date:2019-12-05
Release date:2020-11-11
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.46 Å)
Cite:The combined action of the intracellular regions regulates FGFR2 kinase activity
Commun Biol, 6, 2023
7KIE
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BU of 7kie by Molmil
Crystal structure of FGFR2 kinase domain gatekeeper mutant V564F in complex with covalent compound 3
Descriptor: CITRATE ANION, Fibroblast growth factor receptor 2, GLYCEROL, ...
Authors:Ke, J, Wibowo, A.S, Carter, J.J, Larsen, N.A.
Deposit date:2020-10-23
Release date:2021-02-10
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.47 Å)
Cite:Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.
Acs Med.Chem.Lett., 12, 2021
4J97
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BU of 4j97 by Molmil
Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic Gain-of-Function K659E Mutation Identified in Endometrial Cancer.
Descriptor: Fibroblast growth factor receptor 2, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, SULFATE ION
Authors:Chen, H, Mohammadi, M.
Deposit date:2013-02-15
Release date:2013-08-07
Last modified:2023-09-20
Method:X-RAY DIFFRACTION (2.5482 Å)
Cite:Cracking the Molecular Origin of Intrinsic Tyrosine Kinase Activity through Analysis of Pathogenic Gain-of-Function Mutations.
Cell Rep, 4, 2013
3CU1
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Crystal Structure of 2:2:2 FGFR2D2:FGF1:SOS complex
Descriptor: 1,3,4,6-tetra-O-sulfo-beta-D-fructofuranose-(2-1)-2,3,4,6-tetra-O-sulfonato-alpha-D-glucopyranose, Fibroblast growth factor receptor 2, Heparin-binding growth factor 1
Authors:Guo, F, Dakshinamurthy, R, Thallapuranam, S.K.K, Sakon, J.
Deposit date:2008-04-15
Release date:2009-04-21
Last modified:2020-07-29
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Crystal structure of 2:2:2 FGFR2D2:FGF1:SOS complex
To be Published
5EG3
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BU of 5eg3 by Molmil
Crystal Structure of the Activated FGF Receptor 2 (FGFR2) Kinase Domain in complex with the cSH2 domain of Phospholipase C gamma (PLCgamma)
Descriptor: 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, Fibroblast growth factor receptor 2, MAGNESIUM ION, ...
Authors:Huang, Z, Li, X, Mohammadi, M.
Deposit date:2015-10-26
Release date:2016-02-03
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.606 Å)
Cite:Two FGF Receptor Kinase Molecules Act in Concert to Recruit and Transphosphorylate Phospholipase C gamma.
Mol.Cell, 61, 2016
8E1X
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BU of 8e1x by Molmil
FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29)
Descriptor: (5M)-N-methyl-5-{(6M,8S)-5-{[(3S)-oxolan-3-yl]amino}-6-[1-(propan-2-yl)-1H-pyrazol-3-yl]pyrazolo[1,5-a]pyrimidin-3-yl}pyridine-3-carboxamide, Fibroblast growth factor receptor 2
Authors:Lei, H.-T, Epling, L.B, Deller, M.C.
Deposit date:2022-08-11
Release date:2022-11-23
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.68 Å)
Cite:Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
J.Med.Chem., 65, 2022
1II4
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BU of 1ii4 by Molmil
CRYSTAL STRUCTURE OF SER252TRP APERT MUTANT FGF RECEPTOR 2 (FGFR2) IN COMPLEX WITH FGF2
Descriptor: FIBROBLAST GROWTH FACTOR RECEPTOR 2, HEPARIN-BINDING GROWTH FACTOR 2
Authors:Ibrahimi, O.A, Eliseenkova, A.V, Plotnikov, A.N, Ornitz, D.M, Mohammadi, M.
Deposit date:2001-04-20
Release date:2001-05-09
Last modified:2023-08-16
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Structural basis for fibroblast growth factor receptor 2 activation in Apert syndrome.
Proc.Natl.Acad.Sci.USA, 98, 2001
1E0O
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BU of 1e0o by Molmil
CRYSTAL STRUCTURE OF A TERNARY FGF1-FGFR2-HEPARIN COMPLEX
Descriptor: 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-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-alpha-L-idopyranuronic acid-(1-4)-2-deoxy-6-O-sulfo-2-(sulfoamino)-alpha-D-glucopyranose, FIBROBLAST GROWTH FACTOR 1, FIBROBLAST GROWTH FACTOR RECEPTOR 2, ...
Authors:Pellegrini, L, Burke, D.F, von Delft, F, Mulloy, B, Blundell, T.L.
Deposit date:2000-04-03
Release date:2000-10-23
Last modified:2020-07-29
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Crystal Structure of Fibroblast Growth Factor Receptor Ectodomain Bound to Ligand and Heparin
Nature, 407, 2000
1NUN
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BU of 1nun by Molmil
Crystal Structure Analysis of the FGF10-FGFR2b Complex
Descriptor: Fibroblast growth factor-10, POLYETHYLENE GLYCOL (N=34), SULFATE ION, ...
Authors:Yeh, B.K, Igarashi, M, Eliseenkova, A.V, Plotnikov, A.N, Sher, I, Ron, D, Aaronson, S.A, Mohammadi, M.
Deposit date:2003-01-31
Release date:2003-02-11
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:Structural basis by which alternative splicing confers specificity in fibroblast growth factor receptors.
Proc.Natl.Acad.Sci.USA, 100, 2003
2Q0B
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BU of 2q0b by Molmil
Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic E565A Mutation Responsible for Pfeiffer Syndrome
Descriptor: Fibroblast growth factor receptor 2, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, SULFATE ION
Authors:Chen, H, Mohammadi, M.
Deposit date:2007-05-21
Release date:2007-09-25
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.
Mol.Cell, 27, 2007
5UHN
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BU of 5uhn by Molmil
Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 2 harboring a N549H/E565A Double Gain-of-Function Mutation
Descriptor: Fibroblast growth factor receptor 2, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ...
Authors:Mohammadi, M, Chen, H.
Deposit date:2017-01-11
Release date:2017-02-22
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (2.909 Å)
Cite:Elucidation of a four-site allosteric network in fibroblast growth factor receptor tyrosine kinases.
Elife, 6, 2017
6AGX
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The cocrystal structure of FGFR2 bound with compound 14 harboring 5H-pyrrolo[2,3-b]pyrazine scaffold
Descriptor: Fibroblast growth factor receptor 2, ethyl [4-({3-[2-(3,5-dimethoxyphenyl)ethyl]-5H-pyrrolo[2,3-b]pyrazin-5-yl}sulfonyl)-1H-imidazol-1-yl]acetate
Authors:Xiong, B.
Deposit date:2018-08-15
Release date:2019-08-21
Last modified:2023-11-22
Method:X-RAY DIFFRACTION (2.95 Å)
Cite:The cocrystal structure of FGFR2 bound with compound 14 harboring 5H-pyrrolo[2,3-b]pyrazine scaffold
To be published
6LVL
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Crystal structure of FGFR2 in complex with 1,3,5-triazine derivative
Descriptor: Fibroblast growth factor receptor 2, N-ethyl-2-[[4-[[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-1,3,5-triazin-2-yl]amino]benzenesulfonamide, SULFATE ION
Authors:Echizen, Y, Tateishi, Y, Amano, Y.
Deposit date:2020-02-04
Release date:2020-04-08
Last modified:2023-11-29
Method:X-RAY DIFFRACTION (2.98 Å)
Cite:Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.
Bioorg.Med.Chem., 28, 2020
2PZR
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BU of 2pzr by Molmil
Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic K641R Mutation Responsible for Pfeiffer Syndrome
Descriptor: Fibroblast growth factor receptor 2, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, SULFATE ION
Authors:Chen, H, Mohammadi, M.
Deposit date:2007-05-18
Release date:2007-09-25
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (3 Å)
Cite:A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.
Mol.Cell, 27, 2007
8U1F
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BU of 8u1f by Molmil
FGFR2 Kinase Domain Bound to Irreversible Inhibitor Cmpd 10
Descriptor: Fibroblast growth factor receptor 2, GLYCEROL, N-[4-(4-amino-7-methyl-5-{4-[(4-methylpyrimidin-2-yl)oxy]phenyl}-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenyl]-2-methylpropanamide, ...
Authors:Valverde, R, Foster, L.
Deposit date:2023-08-31
Release date:2024-02-14
Method:X-RAY DIFFRACTION (3.33 Å)
Cite:Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.
Proc.Natl.Acad.Sci.USA, 121, 2024
8H75
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BU of 8h75 by Molmil
FGFR2 in complex with YJ001
Descriptor: CHLORIDE ION, Fibroblast growth factor receptor 2, Tinengotinib
Authors:Yan, X.E, Yun, C.H.
Deposit date:2022-10-19
Release date:2023-10-25
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (3.75 Å)
Cite:FGFR2 in complex with YJ001
To Be Published
8STG
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Discovery and clinical validation of RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Descriptor: Fibroblast growth factor receptor 2, N-{4-[(5P)-4-amino-5-{3-fluoro-4-[(4-methylpyrimidin-2-yl)oxy]phenyl}-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl}-2-methylpropanamide
Authors:Valverde, R, Foster, L.
Deposit date:2023-05-10
Release date:2023-06-07
Last modified:2023-10-25
Method:X-RAY DIFFRACTION (3.79 Å)
Cite:RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.
Cancer Discov, 13, 2023

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