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PDB: 42 件
6GQK
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BU of 6gqk by Molmil
Crystal structure of human c-KIT kinase domain in complex with AZD3229-analogue (compound 23)
分子名称: Mast/stem cell growth factor receptor Kit, ~{N}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide
著者Schimpl, M, Hardy, C.J, Ogg, D.J, Overman, R.C, Packer, M.J, Kettle, J.G, Anjum, R, Barry, E, Bhavsar, D, Brown, C, Campbell, A, Goldberg, K, Grondine, M, Guichard, S, Hunt, T, Jones, O, Li, X, Moleva, O, Pearson, S, Shao, W, Smith, A, Smith, J, Stead, D, Stokes, S, Tucker, M, Ye, Y.
登録日2018-06-07
公開日2018-09-19
最終更新日2024-05-15
実験手法X-RAY DIFFRACTION (2.31 Å)
主引用文献Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
J. Med. Chem., 61, 2018
6GQJ
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Crystal structure of human c-KIT kinase domain in complex with AZD3229-analogue (compound 18)
分子名称: 2-[4-(6,7-dimethoxyquinazolin-4-yl)oxy-2-methoxy-phenyl]-~{N}-(1-propan-2-ylpyrazol-4-yl)ethanamide, Mast/stem cell growth factor receptor Kit
著者Schimpl, M, Hardy, C.J, Ogg, D.J, Overman, R.C, Packer, M.J, Kettle, J.G, Anjum, R, Barry, E, Bhavsar, D, Brown, C, Campbell, A, Goldberg, K, Grondine, M, Guichard, S, Hunt, T, Jones, O, Li, X, Moleva, O, Pearson, S, Shao, W, Smith, A, Smith, J, Stead, D, Stokes, S, Tucker, M, Ye, Y.
登録日2018-06-07
公開日2018-09-19
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.33 Å)
主引用文献Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
J. Med. Chem., 61, 2018
7KHK
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Crystal structure of KIT kinase domain with a small molecule inhibitor, PLX9486 (bezuclastinib) in the DFG-in state
分子名称: 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide, Mast/stem cell growth factor receptor Kit
著者Zhang, Y.
登録日2020-10-21
公開日2021-07-07
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.34 Å)
主引用文献Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial.
Jama Oncol, 7, 2021
4K94
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BU of 4k94 by Molmil
Crystal structure of KIT D4D5 fragment in complex with anti-Kit antibody Fab19
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, Fab19 heavy chain, Fab19 light chain, ...
著者Resheynyak, A.V, Boggon, T.J, Lax, I, Schlessinger, J.
登録日2013-04-19
公開日2013-10-16
最終更新日2020-07-29
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structural basis for KIT receptor tyrosine kinase inhibition by antibodies targeting the D4 membrane-proximal region.
Proc.Natl.Acad.Sci.USA, 110, 2013
8PQG
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c-KIT T670I mutated kinase domain in complex with avapritinib
分子名称: (1~{S})-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine, Mast/stem cell growth factor receptor Kit
著者Teuber, A, Mueller, M.P, Rauh, D.
登録日2023-07-11
公開日2023-12-27
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA.
Nat Commun, 15, 2024
4PGZ
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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
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, COBALT (II) ION, Mast/stem cell growth factor receptor Kit
著者Reshetnyak, A.V, Boggon, T.J, Lax, I, Schlessinger, J.
登録日2014-05-03
公開日2015-03-18
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献The strength and cooperativity of KIT ectodomain contacts determine normal ligand-dependent stimulation or oncogenic activation in cancer.
Mol.Cell, 57, 2015
3G0F
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KIT kinase domain mutant D816H in complex with sunitinib
分子名称: Mast/stem cell growth factor receptor, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo xamide, SULFATE ION
著者Gajiwala, K.S, Wu, J.C, Lunney, E.A, Demetri, G.D.
登録日2009-01-27
公開日2009-02-24
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.
Proc.Natl.Acad.Sci.USA, 106, 2009
4K9E
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BU of 4k9e by Molmil
Crystal structure of KIT D4D5 fragment in complex with anti-Kit antibodies Fab79D
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, Mast/stem cell growth factor receptor Kit, heavy chain, ...
著者Resheynyak, A.V, Boggon, T.J, Lax, I, Schlessinger, J.
登録日2013-04-19
公開日2013-10-16
最終更新日2020-07-29
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Structural basis for KIT receptor tyrosine kinase inhibition by antibodies targeting the D4 membrane-proximal region.
Proc.Natl.Acad.Sci.USA, 110, 2013
7KHJ
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BU of 7khj by Molmil
Crystal structure of KIT kinase domain with a small molecule inhibitor, PLX8512 in the DFG-in state
分子名称: 2-phenyl-5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine, Mast/stem cell growth factor receptor Kit
著者Zhang, Y.
登録日2020-10-21
公開日2021-07-07
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial.
Jama Oncol, 7, 2021
1PKG
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BU of 1pkg by Molmil
Structure of a c-Kit Kinase Product Complex
分子名称: ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, c-kit protein
著者Mol, C.D, Lim, K.B, Sridhar, V, Zou, H, Chien, E.Y.T, Sang, B.-C, Nowakowski, J, Kassel, D.B, Cronin, C.N, McRee, D.E.
登録日2003-06-05
公開日2003-08-12
最終更新日2017-08-09
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Structure of a c-Kit Product Complex Reveals the Basis for Kinase Transactivation.
J.Biol.Chem., 278, 2003
2EC8
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BU of 2ec8 by Molmil
Crystal structure of the exctracellular domain of the receptor tyrosine kinase, Kit
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, Mast/stem cell growth factor receptor
著者Yuzawa, S, Opatowsky, Y, Zhang, Z, Mandiyan, V, Lax, I, Schlessinger, J.
登録日2007-02-11
公開日2007-08-07
最終更新日2020-07-29
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献Structural Basis for Activation of the Receptor Tyrosine Kinase KIT by Stem Cell Factor
Cell(Cambridge,Mass.), 130, 2007
7ZY6
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BU of 7zy6 by Molmil
Identification of M4205 a highly selective inhibitor of cKIT mutations for unresectable metastatic or recurrent GIST
分子名称: 5-imidazo[1,2-a]pyridin-3-yl-~{N}-[(1~{R})-1-(6-pyrrolidin-1-ylpyridin-3-yl)ethyl]pyridin-3-amine, HUMAN PROTO-ONCOGENE C-KIT
著者Graedler, U, Lammens, A.
登録日2022-05-24
公開日2023-02-22
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (3.09 Å)
主引用文献Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors.
J.Med.Chem., 66, 2023
8DFP
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BU of 8dfp by Molmil
Ectodomain of full-length KIT(DupA502,Y503)-SCF dimers
分子名称: 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, ...
著者Bertoletti, N, Krimmer, S.G, Mi, W, Schlessinger, J.
登録日2022-06-22
公開日2023-03-29
最終更新日2023-04-05
実験手法ELECTRON MICROSCOPY (3.17 Å)
主引用文献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
6XV9
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BU of 6xv9 by Molmil
Crystal structure of the kinase domain of human c-KIT in complex with a type-II inhibitor
分子名称: Mast/stem cell growth factor receptor Kit,Mast/stem cell growth factor receptor Kit, ~{N}-[3-[(dimethylamino)methyl]-5-methyl-phenyl]-2-[3-methoxy-5-(7-methoxyquinolin-4-yl)oxy-pyridin-2-yl]ethanamide
著者Ogg, D.J, Howard, T, McAuley, K, Hoyt, E.A, Thomas, M, Bodnarchuk, M.S, Lewis, H.J, Barratt, D, Deery, M.J, Bernardes, G.J.L, Ward, R.A, Kettle, J.G, Waring, M.J.
登録日2020-01-21
公開日2020-05-27
最終更新日2024-05-01
実験手法X-RAY DIFFRACTION (3.38 Å)
主引用文献Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors.
J.Am.Chem.Soc., 142, 2020
8DFM
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BU of 8dfm by Molmil
Ectodomain of full-length wild-type KIT-SCF dimers
分子名称: 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, ...
著者Krimmer, S.G, Bertoletti, N, Mi, W, Schlessinger, J.
登録日2022-06-22
公開日2023-03-29
最終更新日2023-04-05
実験手法ELECTRON MICROSCOPY (3.45 Å)
主引用文献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
2E9W
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BU of 2e9w by Molmil
Crystal structure of the extracellular domain of Kit in complex with stem cell factor (SCF)
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, Kit ligand, Mast/stem cell growth factor receptor
著者Yuzawa, S, Opatowsky, Y, Zhang, Z, Mandiyan, V, Lax, I, Schlessinger, J.
登録日2007-01-27
公開日2007-08-07
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (3.5 Å)
主引用文献Structural Basis for Activation of the Receptor Tyrosine Kinase KIT by Stem Cell Factor
Cell(Cambridge,Mass.), 130, 2007
8DFQ
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Ectodomain of full-length KIT(T417I,delta418-419)-SCF dimers
分子名称: 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, ...
著者Krimmer, S.G, Bertoletti, N, Mi, W, Schlessinger, J.
登録日2022-06-22
公開日2023-03-29
最終更新日2023-04-05
実験手法ELECTRON MICROSCOPY (3.96 Å)
主引用文献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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