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2YS3
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Solution structure of the PH domain of Kindlin-3 from human
分子名称: Unc-112-related protein 2
著者Li, H, Sato, M, Koshiba, S, Watanabe, S, Harada, T, Kigawa, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2007-04-03
公開日2007-10-09
最終更新日2024-05-29
実験手法SOLUTION NMR
主引用文献Solution structure of the PH domain of Kindlin-3 from human
To be Published
2Z0Q
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BU of 2z0q by Molmil
Crystal structure of DH-PH domain of RhoGEF3(Xpln)
分子名称: Rho guanine nucleotide exchange factor 3, SULFATE ION
著者Murayama, K, Kato-Murayama, M, Terada, T, Shirouzu, M, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2007-05-07
公開日2008-05-13
最終更新日2012-12-12
実験手法X-RAY DIFFRACTION (1.79 Å)
主引用文献Structure of the Rho-specific guanine nucleotide-exchange factor Xpln
Acta Crystallogr.,Sect.F, 68, 2012
3A8Q
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Low-resolution crystal structure of the Tiam2 PHCCEx domain
分子名称: T-lymphoma invasion and metastasis-inducing protein 2
著者Terawaki, S, Kitano, K, Mori, T, Zhai, Y, Higuchi, Y, Itoh, N, Watanabe, T, Kaibuchi, K, Hakoshima, T.
登録日2009-10-07
公開日2009-11-24
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (3.2 Å)
主引用文献The PHCCEx domain of Tiam1/2 is a novel protein- and membrane-binding module
Embo J., 29, 2010
3A8N
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Crystal structure of the Tiam1 PHCCEx domain
分子名称: T-lymphoma invasion and metastasis-inducing protein 1
著者Terawaki, S, Kitano, K, Mori, T, Zhai, Y, Higuchi, Y, Itoh, N, Watanabe, T, Kaibuchi, K, Hakoshima, T.
登録日2009-10-07
公開日2009-11-24
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (4.5 Å)
主引用文献The PHCCEx domain of Tiam1/2 is a novel protein- and membrane-binding module
Embo J., 29, 2010
3A8P
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BU of 3a8p by Molmil
Crystal structure of the Tiam2 PHCCEx domain
分子名称: T-lymphoma invasion and metastasis-inducing protein 2
著者Terawaki, S, Kitano, K, Mori, T, Zhai, Y, Higuchi, Y, Itoh, N, Watanabe, T, Kaibuchi, K, Hakoshima, T.
登録日2009-10-07
公開日2009-11-24
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献The PHCCEx domain of Tiam1/2 is a novel protein- and membrane-binding module
Embo J., 29, 2010
2Z0O
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BU of 2z0o by Molmil
Crystal structure of APPL1-BAR-PH domain
分子名称: DCC-interacting protein 13-alpha
著者Murayama, K, Kato-Murayama, M, Terada, T, Shirouzu, M, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2007-05-07
公開日2008-05-13
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.58 Å)
主引用文献Crystal structure of APPL1-BAR-PH domain
To be Published
1RJ2
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BU of 1rj2 by Molmil
Crystal structure of the DH/PH fragment of Dbs without bound GTPase
分子名称: Guanine nucleotide exchange factor DBS [Fragment]
著者Worthylake, D.K, Rossman, K.L, Sondek, J.
登録日2003-11-18
公開日2004-06-29
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献Crystal structure of the DH/PH fragment of Dbs without bound GTPase.
Structure, 12, 2004
2ELB
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BU of 2elb by Molmil
Crystal Structure of the BAR-PH domain of human APPL1
分子名称: Adapter protein containing PH domain, PTB domain and leucine zipper motif 1
著者Li, J, Mao, X, Dong, L.Q, Liu, F, Tong, L.
登録日2007-03-27
公開日2007-05-29
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Crystal Structures of the BAR-PH and PTB Domains of Human APPL1
Structure, 15, 2007
5WG3
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Human GRK2 in complex with Gbetagamma subunits and CCG258748
分子名称: 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(1H-pyrazol-3-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2017-07-13
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.896 Å)
主引用文献Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
7Z3J
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BU of 7z3j by Molmil
Structure of crystallisable rat Phospholipase C gamma 1 in complex with inositol 1,4,5-trisphosphate
分子名称: 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, D-MYO-INOSITOL-1,4,5-TRIPHOSPHATE, ...
著者Pinotsis, N, Bunney, T.D, Katan, M.
登録日2022-03-02
公開日2022-07-20
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Characterization of the membrane interactions of phospholipase C gamma reveals key features of the active enzyme.
Sci Adv, 8, 2022
7SJ4
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Human Trio residues 1284-1959 in complex with Rac1
分子名称: Ras-related C3 botulinum toxin substrate 1, Triple functional domain protein
著者Chen, C.-L, Ravala, S.K, Bandekar, S.J, Cash, J, Tesmer, J.J.G.
登録日2021-10-15
公開日2022-07-06
最終更新日2024-06-05
実験手法ELECTRON MICROSCOPY (2.86 Å)
主引用文献Structural/functional studies of Trio provide insights into its configuration and show that conserved linker elements enhance its activity for Rac1.
J.Biol.Chem., 298, 2022
6PBC
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BU of 6pbc by Molmil
Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations
分子名称: 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma,1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, SODIUM ION
著者Hajicek, N, Sondek, J.
登録日2019-06-13
公開日2020-01-08
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.46 Å)
主引用文献Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations.
Elife, 8, 2019
7T8T
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BU of 7t8t by Molmil
CryoEM structure of PLCg1
分子名称: 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma, CALCIUM ION
著者Endo-Streeter, S, Sondek, J.
登録日2021-12-17
公開日2022-12-21
最終更新日2024-06-05
実験手法ELECTRON MICROSCOPY (3.68 Å)
主引用文献CryoEM structure of PLCg1
To Be Published
7PWD
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BU of 7pwd by Molmil
Structure of an inhibited GRK2-G-beta and G-gamma complex
分子名称: 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ...
著者Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M.
登録日2021-10-06
公開日2021-10-20
最終更新日2022-05-18
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Monatsh Chem, 2022
8GMB
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BU of 8gmb by Molmil
Crystal structure of the full-length Bruton's tyrosine kinase (PH-TH domain not visible)
分子名称: 2-[3'-(hydroxymethyl)-1-methyl-5-({5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl}amino)-6-oxo[1,6-dihydro[3,4'-bipyridine]]-2'-yl]-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, Tyrosine-protein kinase BTK
著者Lin, D.Y, Andreotti, A.H.
登録日2023-03-24
公開日2023-08-16
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (3.4 Å)
主引用文献Conformational heterogeneity of the BTK PHTH domain drives multiple regulatory states.
Elife, 12, 2024
6U7C
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Human GRK2 in complex with Gbetagamma subunits and CCG258747
分子名称: 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-3-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2019-09-02
公開日2020-04-15
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.44 Å)
主引用文献A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor.
Mol.Pharmacol., 97, 2020
4XH9
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CRYSTAL STRUCTURE OF HUMAN RHOA IN COMPLEX WITH DH/PH FRAGMENT OF THE GUANINE NUCLEOTIDE EXCHANGE FACTOR NET1
分子名称: Neuroepithelial cell-transforming gene 1 protein, Transforming protein RhoA
著者Garcia, C, Petit, P, Boutin, J.A, Ferry, G, Vuillard, L.
登録日2015-01-05
公開日2015-01-14
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献A structural study of the complex between neuroepithelial cell transforming gene 1 (Net1) and RhoA reveals a potential anticancer drug hot spot.
J. Biol. Chem., 293, 2018
4PNK
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BU of 4pnk by Molmil
G protein-coupled receptor kinase 2 in complex with GSK180736A
分子名称: (4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G.
登録日2014-05-23
公開日2014-10-08
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.56 Å)
主引用文献Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors.
Acs Chem.Biol., 10, 2015
5KCV
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Crystal structure of allosteric inhibitor, ARQ 092, in complex with autoinhibited form of AKT1
分子名称: 3-[3-[4-(1-azanylcyclobutyl)phenyl]-5-phenyl-imidazo[4,5-b]pyridin-2-yl]pyridin-2-amine, RAC-alpha serine/threonine-protein kinase
著者Eathiraj, S.
登録日2016-06-07
公開日2016-06-29
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.
J.Med.Chem., 59, 2016
7NH5
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Co-Crystal Structure of Akt1 in Complex with Covalent-Allosteric Akt Inhibitor 6
分子名称: ACETATE ION, RAC-alpha serine/threonine-protein kinase, ~{N}-methyl-6-[4-[[4-[2-oxidanylidene-6-(propanoylamino)-3~{H}-benzimidazol-1-yl]piperidin-1-yl]methyl]phenyl]-5-phenyl-pyridine-3-carboxamide
著者Landel, I, Mueller, M.P, Rauh, D.
登録日2021-02-10
公開日2021-09-08
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Cellular model system to dissect the isoform-selectivity of Akt inhibitors.
Nat Commun, 12, 2021
7NH4
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Co-Crystal Structure of Akt1 in Complex with Covalent-Allosteric Akt Inhibitor 3
分子名称: ACETATE ION, RAC-alpha serine/threonine-protein kinase, ~{N}-[3-[1-[[4-[5-(hydroxymethyl)-3-phenyl-pyridin-2-yl]phenyl]methyl]piperidin-4-yl]-2-oxidanylidene-1~{H}-benzimidazol-5-yl]propanamide
著者Landel, I, Mueller, M.P, Rauh, D.
登録日2021-02-10
公開日2021-09-08
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Cellular model system to dissect the isoform-selectivity of Akt inhibitors.
Nat Commun, 12, 2021
1KZ7
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Crystal Structure of the DH/PH Fragment of Murine Dbs in Complex with the Placental Isoform of Human Cdc42
分子名称: CDC42 HOMOLOG, GUANINE NUCLEOTIDE EXCHANGE FACTOR DBS
著者Rossman, K.L, Worthylake, D.K, Snyder, J.T, Siderovski, D.P, Campbell, S.L, Sondek, J.
登録日2002-02-06
公開日2002-03-20
最終更新日2021-10-27
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献A crystallographic view of interactions between Dbs and Cdc42: PH domain-assisted guanine nucleotide exchange.
EMBO J., 21, 2002
1LB1
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Crystal Structure of the Dbl and Pleckstrin homology domains of Dbs in complex with RhoA
分子名称: Guanine nucleotide exchange factor DBS, Transforming protein RhoA
著者Snyder, J.T, Worthylake, D.K, Rossman, K.L, Betts, L, Pruitt, W.M, Siderovski, D.P, Der, C.J, Sondek, J.
登録日2002-04-01
公開日2002-05-29
最終更新日2023-08-16
実験手法X-RAY DIFFRACTION (2.81 Å)
主引用文献Structural basis for the selective activation of Rho GTPases by Dbl exchange factors.
Nat.Struct.Biol., 9, 2002
1KZG
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DbsCdc42(Y889F)
分子名称: CDC42 HOMOLOG, GUANINE NUCLEOTIDE EXCHANGE FACTOR DBS
著者Rossman, K.L, Worthylake, D.K, Snyder, J.T, Siderovski, D.P, Campbell, S.L, Sondek, J.
登録日2002-02-06
公開日2002-03-20
最終更新日2023-08-16
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献A crystallographic view of interactions between Dbs and Cdc42: PH domain-assisted guanine nucleotide exchange.
EMBO J., 21, 2002
3KRW
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BU of 3krw by Molmil
Human GRK2 in complex with Gbetgamma subunits and balanol (soak)
分子名称: BALANOL, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G, Tesmer, V.M.
登録日2009-11-19
公開日2010-02-16
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010

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