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PDB: 47 件
4JDJ
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Crystal structure of Serine/threonine-protein kinase PAK 4 F461V mutant in complex with Paktide T peptide substrate
分子名称: Paktide T, Serine/threonine-protein kinase PAK 4
著者Ha, B.H, Boggon, T.J.
登録日2013-02-25
公開日2014-01-29
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Identification of a major determinant for serine-threonine kinase phosphoacceptor specificity.
Mol.Cell, 53, 2014
5VED
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PAK4 kinase domain in complex with Staurosporine
分子名称: STAUROSPORINE, Serine/threonine-protein kinase PAK 4
著者Zhang, E.Y, Ha, B.H, Boggon, T.J.
登録日2017-04-04
公開日2017-10-18
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.301 Å)
主引用文献PAK4 crystal structures suggest unusual kinase conformational movements.
Biochim. Biophys. Acta, 1866, 2018
4JDK
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Crystal structure of Serine/threonine-protein kinase PAK 4 F461V mutant in complex with Paktide S peptide substrate
分子名称: Paktide S, Serine/threonine-protein kinase PAK 4
著者Ha, B.H, Boggon, T.J.
登録日2013-02-25
公開日2014-01-29
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Identification of a major determinant for serine-threonine kinase phosphoacceptor specificity.
Mol.Cell, 53, 2014
5UPK
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CDC42 binds PAK4 via an extended GTPase-effector interface - 3 peptide: PAK4cat, PAK4-N45, CDC42
分子名称: Cell division control protein 42 homolog, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ...
著者Ha, B.H, Boggon, T.J.
登録日2017-02-03
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献CDC42 binds PAK4 via an extended GTPase-effector interface.
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
4O0X
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Back pocket flexibility provides group-II PAK selectivity for type 1 kinase inhibitors
分子名称: 1-{[1-(4-amino-1,3,5-triazin-2-yl)-2-methyl-1H-benzimidazol-6-yl]ethynyl}cyclohexanol, Serine/threonine-protein kinase PAK 4
著者Rouge, L, Tam, C, Wang, W.
登録日2013-12-14
公開日2014-02-12
最終更新日2014-11-05
実験手法X-RAY DIFFRACTION (2.483 Å)
主引用文献Back Pocket Flexibility Provides Group II p21-Activated Kinase (PAK) Selectivity for Type I 1/2 Kinase Inhibitors.
J.Med.Chem., 57, 2014
7CP4
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Crystal Structure of PAK4 in complex with inhibitor 55
分子名称: Serine/threonine-protein kinase PAK 4, [1-(2-azanylpyrimidin-4-yl)-6-[2-(1-oxidanylcyclohexyl)ethynyl]indol-3-yl]-[(3S)-3-methylpiperazin-1-yl]methanone
著者Zhao, F, Li, H.
登録日2020-08-06
公開日2021-08-11
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Discovery of 6-ethynyl-1H-indole-3-carboxamide Derivatives as Highly Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors
to be published
5VEE
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PAK4 kinase domain in complex with FRAX486
分子名称: 6-(2,4-dichlorophenyl)-8-ethyl-2-{[3-fluoro-4-(piperazin-1-yl)phenyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one, Serine/threonine-protein kinase PAK 4
著者Zhang, E.Y, Ha, B.H, Boggon, T.J.
登録日2017-04-04
公開日2017-10-18
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献PAK4 crystal structures suggest unusual kinase conformational movements.
Biochim. Biophys. Acta, 1866, 2018
4NJD
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Structure of p21-activated kinase 4 with a novel inhibitor KY-04031
分子名称: N-(1H-indazol-5-yl)-N'-[2-(1H-indol-3-yl)ethyl]-6-methoxy-1,3,5-triazine-2,4-diamine, Serine/threonine-protein kinase PAK 4
著者Park, S.
登録日2013-11-09
公開日2014-05-21
最終更新日2022-08-24
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Discovery and the structural basis of a novel p21-activated kinase 4 inhibitor.
Cancer Lett., 349, 2014
7CMB
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Crystal Structure of PAK4 in complex with inhibitor 41
分子名称: 1-(2-azanylpyrimidin-4-yl)-6-[2-(1-oxidanylcyclohexyl)ethynyl]indole-3-carboxamide, Serine/threonine-protein kinase PAK 4
著者Zhao, F, Li, H.
登録日2020-07-26
公開日2021-07-28
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.592 Å)
主引用文献Discovery of 6-ethynyl-1H-indole-3-carboxamide Derivatives as Highly Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors
to be published
4FIF
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Catalytic domain of human PAK4 with RPKPLVDP peptide
分子名称: PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine/threonine-protein kinase PAK 4
著者Ha, B.H, Boggon, T.J.
登録日2012-06-08
公開日2012-09-12
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Type II p21-activated kinases (PAKs) are regulated by an autoinhibitory pseudosubstrate.
Proc.Natl.Acad.Sci.USA, 109, 2012
5XVF
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Crystal Structure of PAK4 in complex with inhibitor CZH062
分子名称: 2-(4-azanylpiperidin-1-yl)-6-chloranyl-N-(1-methylimidazol-4-yl)quinazolin-4-amine, Serine/threonine-protein kinase PAK 4
著者Zhao, F, Li, H.
登録日2017-06-27
公開日2018-02-07
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2.655 Å)
主引用文献Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.
J. Med. Chem., 61, 2018
8AHI
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PAC-FragmentDEL: Photoactivated covalent capture of DNA encoded fragments for hit discovery
分子名称: Serine/threonine-protein kinase PAK 4, ~{N}-methyl-1,3-benzothiazole-6-carboxamide
著者Baker, L.M, Murray, J.B, Hubbard, R.E.
登録日2022-07-21
公開日2022-09-14
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (2.69 Å)
主引用文献PAC-FragmentDEL - photoactivated covalent capture of DNA-encoded fragments for hit discovery.
Rsc Med Chem, 13, 2022
4O0V
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Back pocket flexibility provides group-II PAK selectivity for type 1 kinase inhibitors
分子名称: 1-({1-(2-aminopyrimidin-4-yl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl}ethynyl)cyclohexanol, Serine/threonine-protein kinase PAK 4
著者Rouge, L, Tam, C, Wang, W.
登録日2013-12-14
公開日2014-02-12
最終更新日2014-02-26
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Back Pocket Flexibility Provides Group II p21-Activated Kinase (PAK) Selectivity for Type I 1/2 Kinase Inhibitors.
J.Med.Chem., 57, 2014
4L67
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Crystal Structure of Catalytic Domain of PAK4
分子名称: Serine/threonine-protein kinase PAK 4
著者Wang, W, Song, J.
登録日2013-06-12
公開日2013-08-14
最終更新日2023-11-08
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献NMR binding and crystal structure reveal that intrinsically-unstructured regulatory domain auto-inhibits PAK4 by a mechanism different for that of PAK1
Biochem.Biophys.Res.Commun., 438, 2013
7CP3
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Crystal Structure of PAK4 in complex with inhibitor 47
分子名称: Serine/threonine-protein kinase PAK 4, [(3R)-3-azanylpiperidin-1-yl]-[1-(2-azanylpyrimidin-4-yl)-6-[2-(1-oxidanylcyclohexyl)ethynyl]indol-3-yl]methanone
著者Zhao, F, Li, H.
登録日2020-08-05
公開日2021-08-11
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Discovery of 6-ethynyl-1H-indole-3-carboxamide Derivatives as Highly Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors
to be published
5BMS
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BU of 5bms by Molmil
Crystal structure of P21-activated kinase 4 in complex with an inhibitor compound 29
分子名称: N~2~-[(7-chloro-1H-benzimidazol-6-yl)methyl]-N~4~-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine, Serine/threonine-protein kinase PAK 4
著者Rouge, L, Wang, W.
登録日2015-05-22
公開日2015-07-01
最終更新日2015-07-15
実験手法X-RAY DIFFRACTION (2.903 Å)
主引用文献Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.
J.Med.Chem., 58, 2015
4XBR
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BU of 4xbr by Molmil
In cellulo Crystal Structure of PAK4 in complex with Inka
分子名称: ADENOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, Protein FAM212A,Serine/threonine-protein kinase PAK 4
著者Baskaran, Y, Ang, K.C, Anekal, P.V, Chan, W.L, Grimes, J.M, Manser, E, Robinson, R.C.
登録日2014-12-17
公開日2015-12-02
最終更新日2023-11-08
実験手法X-RAY DIFFRACTION (2.94 Å)
主引用文献An in cellulo-derived structure of PAK4 in complex with its inhibitor Inka1
Nat Commun, 6, 2015
5UPL
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CDC42 binds PAK4 via an extended GTPase-effector inteface - 2 peptide: PAK4FL, CDC42 - UNREFINED
分子名称: Cell division control protein 42 homolog, Serine/threonine-protein kinase PAK 4
著者Ha, B.H, Boggon, T.J.
登録日2017-02-03
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (3.003 Å)
主引用文献CDC42 binds PAK4 via an extended GTPase-effector interface.
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
4FIG
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Catalytic domain of human PAK4
分子名称: MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine/threonine-protein kinase PAK 4
著者Ha, B.H, Boggon, T.J.
登録日2012-06-08
公開日2012-09-12
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (3.01 Å)
主引用文献Type II p21-activated kinases (PAKs) are regulated by an autoinhibitory pseudosubstrate.
Proc.Natl.Acad.Sci.USA, 109, 2012
5I0B
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Structure of PAK4
分子名称: 6-bromo-2-[1-methyl-3-(propan-2-yl)-1H-pyrazol-4-yl]-1H-imidazo[4,5-b]pyridine, Serine/threonine-protein kinase PAK 4
著者Park, S.Y.
登録日2016-02-03
公開日2016-12-14
最終更新日2023-11-08
実験手法X-RAY DIFFRACTION (3.09 Å)
主引用文献The discovery and the structural basis of an imidazo[4,5-b]pyridine-based p21-activated kinase 4 inhibitor
Bioorg. Med. Chem. Lett., 26, 2016
4FIE
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Full-length human PAK4
分子名称: PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine/threonine-protein kinase PAK 4
著者Ha, B.H, Boggon, T.J.
登録日2012-06-08
公開日2012-09-12
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (3.11 Å)
主引用文献Type II p21-activated kinases (PAKs) are regulated by an autoinhibitory pseudosubstrate.
Proc.Natl.Acad.Sci.USA, 109, 2012
8YHK
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The Crystal Structure of P21-Activated Kinases Pak4 from Biortus
分子名称: Serine/threonine-protein kinase PAK 4, TRIETHYLENE GLYCOL
著者Wang, F, Cheng, W, Lv, Z, Qi, J, Wu, B.
登録日2024-02-28
公開日2024-03-13
実験手法X-RAY DIFFRACTION (3.3 Å)
主引用文献The Crystal Structure of P21-Activated Kinases Pak4 from Biortus
To Be Published
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