2Z0Q
 
 | | Crystal structure of DH-PH domain of RhoGEF3(Xpln) | | Descriptor: | Rho guanine nucleotide exchange factor 3, SULFATE ION | | Authors: | Murayama, K, Kato-Murayama, M, Terada, T, Shirouzu, M, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | | Deposit date: | 2007-05-07 | | Release date: | 2008-05-13 | | Last modified: | 2012-12-12 | | Method: | X-RAY DIFFRACTION (1.79 Å) | | Cite: | Structure of the Rho-specific guanine nucleotide-exchange factor Xpln
Acta Crystallogr.,Sect.F, 68, 2012
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3A8Q
 | | Low-resolution crystal structure of the Tiam2 PHCCEx domain | | Descriptor: | T-lymphoma invasion and metastasis-inducing protein 2 | | Authors: | Terawaki, S, Kitano, K, Mori, T, Zhai, Y, Higuchi, Y, Itoh, N, Watanabe, T, Kaibuchi, K, Hakoshima, T. | | Deposit date: | 2009-10-07 | | Release date: | 2009-11-24 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | The PHCCEx domain of Tiam1/2 is a novel protein- and membrane-binding module
Embo J., 29, 2010
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3A8P
 | | Crystal structure of the Tiam2 PHCCEx domain | | Descriptor: | T-lymphoma invasion and metastasis-inducing protein 2 | | Authors: | Terawaki, S, Kitano, K, Mori, T, Zhai, Y, Higuchi, Y, Itoh, N, Watanabe, T, Kaibuchi, K, Hakoshima, T. | | Deposit date: | 2009-10-07 | | Release date: | 2009-11-24 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The PHCCEx domain of Tiam1/2 is a novel protein- and membrane-binding module
Embo J., 29, 2010
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3A8N
 | | Crystal structure of the Tiam1 PHCCEx domain | | Descriptor: | T-lymphoma invasion and metastasis-inducing protein 1 | | Authors: | Terawaki, S, Kitano, K, Mori, T, Zhai, Y, Higuchi, Y, Itoh, N, Watanabe, T, Kaibuchi, K, Hakoshima, T. | | Deposit date: | 2009-10-07 | | Release date: | 2009-11-24 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (4.5 Å) | | Cite: | The PHCCEx domain of Tiam1/2 is a novel protein- and membrane-binding module
Embo J., 29, 2010
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3CXB
 | | Crystal Structure of sifa and skip | | Descriptor: | Pleckstrin homology domain-containing family M member 2, Protein sifA | | Authors: | Huang, Z, Chai, J. | | Deposit date: | 2008-04-24 | | Release date: | 2008-12-02 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure and function of Salmonella SifA indicate that its interactions with SKIP, SseJ, and RhoA family GTPases induce endosomal tubulation
Cell Host Microbe, 4, 2008
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1QQG
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1RJ2
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2ELB
 | | Crystal Structure of the BAR-PH domain of human APPL1 | | Descriptor: | Adapter protein containing PH domain, PTB domain and leucine zipper motif 1 | | Authors: | Li, J, Mao, X, Dong, L.Q, Liu, F, Tong, L. | | Deposit date: | 2007-03-27 | | Release date: | 2007-05-29 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal Structures of the BAR-PH and PTB Domains of Human APPL1
Structure, 15, 2007
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7Z3J
 | | Structure of crystallisable rat Phospholipase C gamma 1 in complex with inositol 1,4,5-trisphosphate | | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, D-MYO-INOSITOL-1,4,5-TRIPHOSPHATE, ... | | Authors: | Pinotsis, N, Bunney, T.D, Katan, M. | | Deposit date: | 2022-03-02 | | Release date: | 2022-07-20 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Characterization of the membrane interactions of phospholipase C gamma reveals key features of the active enzyme.
Sci Adv, 8, 2022
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8GMB
 | | Crystal structure of the full-length Bruton's tyrosine kinase (PH-TH domain not visible) | | Descriptor: | 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 | | Authors: | Lin, D.Y, Andreotti, A.H. | | Deposit date: | 2023-03-24 | | Release date: | 2023-08-16 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Conformational heterogeneity of the BTK PHTH domain drives multiple regulatory states.
Elife, 12, 2024
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4PNK
 | | G protein-coupled receptor kinase 2 in complex with GSK180736A | | Descriptor: | (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, ... | | Authors: | Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G. | | Deposit date: | 2014-05-23 | | Release date: | 2014-10-08 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.56 Å) | | Cite: | Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors.
Acs Chem.Biol., 10, 2015
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7SJ4
 | | Human Trio residues 1284-1959 in complex with Rac1 | | Descriptor: | Ras-related C3 botulinum toxin substrate 1, Triple functional domain protein | | Authors: | Chen, C.-L, Ravala, S.K, Bandekar, S.J, Cash, J, Tesmer, J.J.G. | | Deposit date: | 2021-10-15 | | Release date: | 2022-07-06 | | Last modified: | 2022-08-24 | | Method: | ELECTRON MICROSCOPY (2.86 Å) | | Cite: | 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
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7T8T
 | | CryoEM structure of PLCg1 | | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma, CALCIUM ION | | Authors: | Endo-Streeter, S, Sondek, J. | | Deposit date: | 2021-12-17 | | Release date: | 2022-12-21 | | Method: | ELECTRON MICROSCOPY (3.68 Å) | | Cite: | CryoEM structure of PLCg1
To Be Published
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7NH5
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7NH4
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6PBC
 | | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations | | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma,1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, SODIUM ION | | Authors: | Hajicek, N, Sondek, J. | | Deposit date: | 2019-06-13 | | Release date: | 2020-01-08 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.46 Å) | | Cite: | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations.
Elife, 8, 2019
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7PWD
 | | Structure of an inhibited GRK2-G-beta and G-gamma complex | | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | | Deposit date: | 2021-10-06 | | Release date: | 2021-10-20 | | Last modified: | 2022-05-18 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Monatsh Chem, 2022
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6NFA
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6NEW
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6NF1
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7CSP
 | | Structure of Ephexin4 IDPSH | | Descriptor: | Rho guanine nucleotide exchange factor 16 | | Authors: | Zhang, M, Lin, L, Wang, C, Zhu, J. | | Deposit date: | 2020-08-15 | | Release date: | 2021-02-24 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Double inhibition and activation mechanisms of Ephexin family RhoGEFs.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7CSR
 | | Structure of Ephexin4 R676L | | Descriptor: | Rho guanine nucleotide exchange factor 16 | | Authors: | Zhang, M, Lin, L, Wang, C, Zhu, J. | | Deposit date: | 2020-08-17 | | Release date: | 2021-02-24 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Double inhibition and activation mechanisms of Ephexin family RhoGEFs.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7CSO
 | | Structure of Ephexin4 DH-PH-SH3 | | Descriptor: | Rho guanine nucleotide exchange factor 16, SULFATE ION | | Authors: | Zhang, M, Lin, L, Wang, C, Zhu, J. | | Deposit date: | 2020-08-15 | | Release date: | 2021-02-24 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (2.39 Å) | | Cite: | Double inhibition and activation mechanisms of Ephexin family RhoGEFs.
Proc.Natl.Acad.Sci.USA, 118, 2021
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5KCV
 | | Crystal structure of allosteric inhibitor, ARQ 092, in complex with autoinhibited form of AKT1 | | Descriptor: | 3-[3-[4-(1-azanylcyclobutyl)phenyl]-5-phenyl-imidazo[4,5-b]pyridin-2-yl]pyridin-2-amine, RAC-alpha serine/threonine-protein kinase | | Authors: | Eathiraj, S. | | Deposit date: | 2016-06-07 | | Release date: | 2016-06-29 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 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
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4XH9
 | | CRYSTAL STRUCTURE OF HUMAN RHOA IN COMPLEX WITH DH/PH FRAGMENT OF THE GUANINE NUCLEOTIDE EXCHANGE FACTOR NET1 | | Descriptor: | Neuroepithelial cell-transforming gene 1 protein, Transforming protein RhoA | | Authors: | Garcia, C, Petit, P, Boutin, J.A, Ferry, G, Vuillard, L. | | Deposit date: | 2015-01-05 | | Release date: | 2015-01-14 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | 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
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